Click here to view all research publications from the Qi laboratory.
Selected Publications
2022
The FUS::DDIT3 fusion oncoprotein inhibits BAF complex targeting and activity in myxoid liposarcoma.
Zullow HJ, Sankar A, Ingram DR, Samé Guerra DD, D'Avino AR, Collings CK, Lazcano R, Wang WL, Liang Y, Qi J, Lazar AJ, Kadoch C.Mol Cell. 2022 Apr 4:S1097-2765(22)00257-X. doi: 10.1016/j.molcel.2022.03.019. Online ahead of print.PMID: 35390276
Exploring Methods of Targeting Histone Methyltransferases and Their Applications in Cancer Therapeutics.
Wang MY, Liow P, Guzman MIT, Qi J.ACS Chem Biol. 2022 Apr 1. doi: 10.1021/acschembio.2c00062. Online ahead of print.PMID: 35363464
BET-bromodomain and EZH2 inhibitor treated chronic GVHD mice have blunted germinal centers with distinct transcriptomes.
Zaiken MC, Flynn R, Paz KG, Rhee SY, Jin S, Mohamed FA, Saha A, Thangavelu G, Park PMC, Hemming ML, Sage PT, Sharpe AH, DuPage M, Bluestone JA, Panoskaltsis-Mortari A, Cutler CS, Koreth J, Antin JH, Soiffer RJ, Ritz J, Luznik L, Maillard I, Hill GR, MacDonald KP, Munn DH, Serody JS, Murphy WJ, Kean LS, Zhang Y, Bradner JE, Qi J, Blazar BR. Blood. 2022 Feb 28:blood.2021014557. doi: 10.1182/blood.2021014557. Online ahead of print.PMID: 35226736
A PRC2-Kdm5b axis sustains tumorigenicity of acute myeloid leukemia.
Ren Z, Kim A, Huang YT, Pi WC, Gong W, Yu X, Qi J, Jin J, Cai L, Roeder RG, Chen WY, Wang GG.Proc Natl Acad Sci U S A. 2022 Mar 1;119(9):e2122940119. doi: 10.1073/pnas.2122940119.PMID: 35217626
2021
EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma.
Durbin AD*#, Wang T*, Wimalasena VK, Zimmerman MW, Li D, Dharia NV, Mariani L, Shendy NAM, Nance S, Patel AG, Shao Y, Mundada M, Maxham L, Park PMC, Sigua LH, Morita K, Saur Conway A, Robichaud AL, Perez-Atayde AR, Bikowitz MJ, Quinn TR, Wiest OG, Easton J, Schonbrunn E, Bulyk ML, Abraham BJ, Stegmaier K#, Look AT#, Qi J.# Cancer Discovery. 2021 Nov 12:candisc.0385.2021. doi: 10.1158/2159-8290.CD-21-0385. Online ahead of print
Targeting an inducible SALL4-mediated cancer vulnerability with sequential therapy.
Yang J, Gao C, Liu M, Liu YC, Kwon J, Qi J, Tian X, Stein A, Liu YV, Kong NR, Wu Y, Yin S, Xi J, Chen Z, Kumari K, Wong H, Luo H, Silberstein LE, Thoms JAI, Unnikrishnan A, Pimanda JE, Tenen DG, Chai L.Cancer Res. 2021 Sep 30:canres.0030.2021. doi: 10.1158/0008-5472.CAN-21-0030. Online ahead of print.PMID: 34593523
Lysine Demethylase 5A Is Required for MYC-Driven Transcription in Multiple Myeloma
Ohguchi H, Park PMC, Wang T, Gryder BE, Ogiya D, Kurata K, Zhang X, Li D, Pei C, Masuda T, Johansson C, Wimalasena VK, Kim Y, Hino S, Usuki S, Kawano Y, Samur MK, Tai Y, Munshi NC, Matsuoka M, Ohtsuki S, Nakao M, Minami T, Lauberth S, Khan J, Oppermann U, Durbin AD, Anderson KC#, Hideshima T#, Qi J# (Lead Contact). Blood Cancer Discovery, In Press.
Bromodomain protein BRD4 directs and sustains CD8 T cell differentiation during infection.
Milner JJ, Toma C, Quon S, Omilusik K, Scharping NE, Dey A, Reina-Campos M, Nguyen H, Getzler AJ, Diao H, Yu B, Delpoux A, Yoshida TM, Li D, Qi J, Vincek A, Hedrick SM, Egawa T, Zhou MM, Crotty S, Ozato K, Pipkin ME, Goldrath AW.J Exp Med. 2021 Aug 2;218(8):e20202512. doi: 10.1084/jem.20202512. Epub 2021 May 26.PMID: 34037670
Reprogramming of the esophageal squamous carcinoma epigenome by SOX2 promotes ADAR1 dependence.
Wu Z, Zhou J, Zhang X, Zhang Z, Xie Y, Liu JB, Ho ZV, Panda A, Qiu X, Cejas P, Cañadas I, Akarca FG, McFarland JM, Nagaraja AK, Goss LB, Kesten N, Si L, Lim K, Liu Y, Zhang Y, Baek JY, Liu Y, Patil DT, Katz JP, Hai J, Bao C, Stachler M, Qi J, Ishizuka JJ, Nakagawa H, Rustgi AK, Wong KK, Meyerson M, Barbie DA, Brown M, Long H, Bass AJ.Nat Genet. 2021 May 10. doi: 10.1038/s41588-021-00859-2. Online ahead of print.PMID: 33972779
Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 Inhibitors.
Muthengi A,* Wimalasena VK,* Yosief HO,* Bikowitz MJ,* Sigua LH, Wang T, Li D, Gaieb Z, Dhawan G, Liu S, Erickson J, Amaro RE, Schönbrunn E#, Qi J#, Zhang W.# J Med Chem. 2021 Apr 19. doi: 10.1021/acs.jmedchem.0c02232. Online ahead of print. PMID: 33872011
Transcriptional programming drives Ibrutinib-resistance evolution in mantle cell lymphoma.
Zhao X, Wang MY, Jiang H, Lwin T, Park PM, Gao J, Meads MB, Ren Y, Li T, Sun J, Fahmi NA, Singh S, Sehgal L, Wang X, Silva AS, Sotomayor EM, Shain KH, Cleveland JL, Wang M, Zhang W, Qi J, Shah BD, Tao J. Cell Rep. 2021 Mar 16;34(11):108870. doi: 10.1016/j.celrep.2021.108870.PMID: 33730585 Free article.
Brd4 participates in epigenetic regulation of the extinction of remote auditory fear memory.
Huang FL, Li F, Zhang WJ, Li SJ, Yang ZH, Yang TL, Qi J, Duan Q, Li CQ. Neurobiol Learn Mem. 2021 Jan 15;179:107383. doi: 10.1016/j.nlm.2021.107383. Online ahead of print.PMID: 33460788
2020
Inhibition of Polo-like kinase 1 (PLK1) facilitates the elimination of HIV-1 viral reservoirs in CD4+ T cells ex vivo.
Zhou D, Hayashi T, Jean M, Kong W, Fiches G, Biswas A, Liu S, Yosief HO, Zhang X, Bradner J, Qi J, Zhang W, Santoso N, Zhu J. Sci Adv. 2020 Jul 15;6(29):eaba1941. doi: 10.1126/sciadv.aba1941. eCollection 2020 Jul.PMID: 32832623 Free PMC article.
The Folate Cycle Enzyme MTHFR is a Critical Regulator of Cell Response to MYC-Targeting Therapies.
Su A, Ling F, Vaganay C, Sodaro G, Benaksas C, Dal Bello R, Forget A, Pardieu B, Lin KH, Rutter JC, Bassil CF, Fortin G, Pasanisi J, Antony-Debre I, Alexe G, Benoist JF, Pruvost A, Pikman Y, Qi J, Schlageter MH, Micol JB, Roti G, Cluzeau T, Dombret H, Preudhomme C, Fenouille N, Benajiba L, Golan HM, Stegmaier K, Lobry C, Wood KC, Itzykson R, Puissant A.Cancer Discov. 2020 Aug 21:CD-19-0970. doi: 10.1158/2159-8290.CD-19-0970. Online ahead of print.PMID: 32826232
BET proteins inhibitor JQ-1 impaired the extinction of remote auditory fear memory: An effect mediated by insulin like growth factor 2.
Duan Q, Huang FL, Li SJ, Chen KZ, Gong L, Qi J, Yang ZH, Yang TL, Li F, Li CQ. Neuropharmacology. 2020 Oct 15;177:108255. doi: 10.1016/j.neuropharm.2020.108255. Epub 2020 Jul 28.
High-performance CRISPR-Cas12a genome editing for combinatorial genetic screening.
Gier RA, Budinich KA, Evitt NH, Cao Z, Freilich ES, Chen Q, Qi J, Lan Y, Kohli RM, Shi J.
Nat Commun. 2020 Jul 13;11(1):3455. doi: 10.1038/s41467-020-17209-1.
Epigenetic CRISPR screens identify Npm1 as a therapeutic vulnerability in non-small cell lung cancer.
Li F*, Ng WL*, Luster TA, Hu H, Sviderskiy VO, Dowling CM, Hollinshead KER, Zouitine P, Zhang H, Huang Q, Ranieri M, Wang W, Fang Z, Chen T, Deng J, Zhao K, So HC, Khodadadi-Jamayran A, Xu M, Karatza A, Pyon V, Li S, Pan Y, Labbe K, Almonte C, Poirier JT, Miller G, Possemato R, Qi J#, Wong KK#.
Cancer Res. 2020 Jul 9:canres.3782.2019. doi: 10.1158/0008-5472.CAN-19-3782. Online ahead of print.
BET bromodomain proteins regulate transcriptional reprogramming in genetic dilated cardiomyopathy.
Antolic A, Wakimoto H, Jiao Z, Gorham JM, DePalma SR, Lemieux ME, Conner DA, Lee DY, Qi J, Seidman JG, Bradner JE, Brown JD, Haldar SM, Seidman CE, Burke MA. JCI Insight. 2020 Jun 30:138687. doi: 10.1172/jci.insight.138687. Online ahead of print.
Peptide-Based PROTAC: The Predator of Pathological Proteins.
Au YZ, Wang T, Sigua LH, Qi J. Cell Chem Biol. 2020 Jun 18;27(6):637-639.
Selective Targeting of Different Bromodomains by Small Molecules.
Qi J, Shi Y.Cancer Cell. 2020 Jun 8;37(6):764-766.
Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer.
Shu S, Wu HJ, Ge JY, Zeid R, Harris IS, Jovanović B, Murphy K, Wang B, Qiu X, Endress JE, Reyes J, Lim K, Font-Tello A, Syamala S, Xiao T, Reddy Chilamakuri CS, Papachristou EK, D'Santos C, Anand J, Hinohara K, Li W, McDonald TO, Luoma A, Modiste RJ, Nguyen QD, Michel B, Cejas P, Kadoch C, Jaffe JD, Wucherpfennig KW, Qi J, Liu XS, Long H, Brown M, Carroll JS, Brugge JS, Bradner J, Michor F, Polyak K.Mol Cell. 2020 Jun 18;78(6):1096-1113.
Using Chemical Epigenetics to Target Cancer.
Wimalasena VK*, Wang T*, Sigua LH*, Durbin AD#, Qi J#.
Molecular Cell. 2020 May 5. pii: S1097-2765(20)30265-3. doi: 10.1016/j.molcel.2020.04.023. [Epub ahead of print] Review.
Acquired resistance to combined BET and CDK4/6 inhibition in triple-negative breast cancer.
Ge JY, Shu S, Kwon M, Jovanović B, Murphy K, Gulvady A, Fassl A, Trinh A, Kuang Y, Heavey GA, Luoma A, Paweletz C, Thorner AR, Wucherpfennig KW, Qi J, Brown M, Sicinski P, McDonald TO, Pellman D, Michor F, Polyak K.
Nature Communication. 2020 May 11;11(1):2350. doi: 10.1038/s41467-020-16170-3.
In vivo epigenetic CRISPR screen identifies Asf1a as an immunotherapeutic target in Kras-mutant lung adenocarcinoma.
Li F, Huang Q, Luster TA, Hu H, Zhang H, Ng WL, Khodadadi-Jamayran A, Wang W, Chen T, Deng J, Ranieri M, Fang Z, Pyon V, Dowling CM, Bagdatlioglu E, Almonte C, Labbe K, Silver H, Rabin AR, Jani K, Tsirigos A, Papagiannakopoulos T, Hammerman PS, Velcheti V, Freeman GJ, Qi J, Miller G, Wong KK.
Cancer Discovery. 2020 Feb;10(2):270-287. doi: 10.1158/2159-8290.CD-19-0780. Epub 2019 Nov 19.
BET bromodomain inhibition suppresses adipogenesis in mice.
Duan Q, Wu P, Liu Z, Xia F, Zhu L, Zheng Z, Yang T, Qi J.
Endocrine. 2020 Jan;67(1):264-267. doi: 10.1007/s12020-019-02115-4. Epub 2019 Nov 5.
2019
Diversified Application of Barcoded PLATO (PLATO-BC) Platform for Identification of Protein Interactions.
Kong W, Hayashi T, Fiches G, Xu Q, Li MZ, Que J, Liu S, Zhang W, Qi J, Santoso N, Elledge SJ, Zhu J.
Genomics Proteomics Bioinformatics. 2019 Jun;17(3):319-331. doi: 10.1016/j.gpb.2018.12.010. Epub 2019 Sep 5.
Dynamic Chromatin Targeting of BRD4 Stimulates Cardiac Fibroblast Activation.
Stratton MS, Bagchi RA, Felisbino MB, Hirsch RA, Smith HE, Riching AS, Enyart BY, Koch KA, Cavasin MA, Alexanian M, Song K, Qi J, Lemieux ME, Srivastava D, Lam MPY, Haldar SM, Lin CY, McKinsey TA.
Circulation Research. 2019 Sep 13;125(7):662-677. doi: 10.1161/CIRCRESAHA.119.315125. Epub 2019 Aug 14.
Chemical genomics reveals histone deacetylases are required for core regulatory transcription
Berkley E. Gryder*, Lei Wu*, Girma M. Woldemichael, Silvia Pomella, Taylor R. Quinn, Paul M. C. Park, Abigail Cleveland, Benjamin Z. Stanton, Young Song, Rossella Rota, Olaf Wiest, Marielle E. Yohe, Jack F. Shern, Jun Qi‡ & Javed Khan‡.
Nature Communications. 2019 July 08; doi: 10.1038/s41467-019-11046-7
Neuronal differentiation and cell-cycle programs mediate response to BET-bromodomain inhibition in MYC-driven medulloblastoma.
Bandopadhayay P, Piccioni F, O'Rourke R, Ho P, Gonzalez EM, Buchan G, Qian K, Gionet G, Girard E, Coxon M, Rees MG, Brenan L, Dubois F, Shapira O, Greenwald NF, Pages M, Balboni Iniguez A, Paolella BR, Meng A, Sinai C, Roti G, Dharia NV, Creech A, Tanenbaum B, Khadka P, Tracy A, Tiv HL, Hong AL, Coy S, Rashid R, Lin JR, Cowley GS, Lam FC, Goodale A, Lee Y, Schoolcraft K, Vazquez F, Hahn WC, Tsherniak A, Bradner JE, Yaffe MB, Milde T, Pfister SM, Qi J, Schenone M, Carr SA, Ligon KL, Kieran MW, Santagata S, Olson JM, Gokhale PC, Jaffe JD, Root DE, Stegmaier K, Johannessen CM, Beroukhim R.
Nature Communications. 2019 Jun 3;10(1):2400. doi: 10.1038/s41467-019-10307-9.
A large-scale drug screen identifies selective inhibitors of class I HDACs as a potential therapeutic option for SHH medulloblastoma.
Pak E, MacKenzie EL, Zhao X, Pazyra-Murphy MF, Park PMC, Wu L, Shaw DL, Addleson EC, Cayer SS, Lopez BG, Agar NYR, Rubin LL, Qi J, Merk DJ, Segal RA.
Neuro-Oncology. 2019 May 16. pii: noz089. doi: 10.1093/neuonc/noz089.
BCL2 Amplicon loss and transcriptional remodeling drives ABT-199 resistance in B-cell lymphoma models
Zhao X*, Ren Y*, Lawlor MA*, Shah BD, Park PMC, Lwin T, Wang X, Liu K, Wang M, Gao J, Li T, Xu M, Silva AS, Lee K, Zhang T, Koomen JM, Jiang H, Sudalagunta PR, Meads MB, Cheng F, Bi C, Fu K, Fan H, Dalton WS, Moscinski LC, Shain KH, Sotomayor EM, Wang GG, Gray NS, Cleveland JL, Qi J‡, Tao J‡.
Cancer Cell. 2019 May 13;35(5):752-766.e9. doi: 10.1016/j.ccell.2019.04.005. PMID: 31085176
Development and preclinical validation of a novel covalent ubiquitin receptor Rpn13 degrader in multiple myeloma
Song Y*, Park PMC*, Wu L, Ray A, Picaud S, Li D, Wimalasena VK, Du T, Filippakopoulos P, Anderson KC‡, Qi J‡, Chauhan D‡.
Leukemia. 2019 April 08; doi: 10.1038/s41375-019-0467-z. PMID:30962579
2018
Resistance to epigenetic-targeted therapy engenders tumor cell vulnerabilities associated with enhancer remodeling
Iniguez AB, Alexe G, Wang EJ, Roti G, Patel S, Chen L, Kitara S, Conway A, Robichaud AL, Stolte B, Bandopadhayay P, Goodale A, Pantel S, Lee Y, Cheff DM, Hall MD, Guha R, Davis MI, Menard M, Nasholm N, Weiss WA, Qi J, Beroukhim R, Piccioni F, Johannessen C, Stegmaier K.
Cancer Cell. 2018 Dec 10;34(6):922-938.e7. doi: 10.1016/j.ccell.2018.11.005. PMID:30537514
YAP1 enhances NF-KB-depedent and independent effects on clock-mediated unfolded protein responses and autophagy in sarcoma
Rivera-Reyes A, Ye S, Marino G, Egolf S, Ciotti G, Chor S, Liu Y, Posimo J, Park PMC, Pak K, Babichev Y, Sostre-Colon J, Tameire F, Leli N, Koumenis C, Brady D, Mancuso A, Weber K, Gladdy R, Qi J, Eisinger-Mathanson TSK.
Cell Death Dis. 2018 Oct 31;9(11):1108. doi: 10.1038/s41419-018-1142-4. PMID:30382078
Small-molecule BCL6 inhibitor effectively treats mice with nonsclerodermatous chronice graft-versus-host disease
Paz K, Flynn R, Du J, Qi J, Luznik L, Maillard I, MacDonald KP, Hill GR, Serody JS, Murphy WJ, Sage PT, Sharpe AH, Miklos D, Cutler CS, Koreth J, Antin JH, Soiffer RJ, Ritz J, Bradner JE, Melnick AM, Blazar BR.
Blood. 2018 Oct 2. doi: 10.1182/blood-2018-03-839993. [Epub ahead of print] PMID: 30279226
Structural and atropisomeric factors governing the selectivity of pyrimido-benzodiazipinones as inhibitors of kinases and bromodomains
Wang J, Erazo T, Ferguson FM, Buckley DL, Gomez N, Muñoz-Guardiola P, Diéguez-Martinez N, Deng X, Hao M, Massefski W, Fedorov O, Offei-Addo NK, Park PM, Dai L, DiBona A, Becht K, Kim ND, McKeown MR, Roberts JM, Zhang J, Sim T, Alessi DR, Bradner JE, Lizcano JM, Blacklow SC, Qi J, Xu X, Gray NS.
ACS Chem Biol. 2018 Sep 21;13(9):2438-2448. doi: 10.1021/acschembio.7b00638. Epub 2018 Aug 31. PMID:30102854
Structure-guided design and development of potent and selective dual bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) inhibitors
Liu S, Yosief HO, Dai L, Huang H, Dhawan G, Zhang X, Muthengi AM, Roberts J, Buckley DL, Perry JA, Wu L, Bradner JE, Qi J‡, Zhang W‡.
J Med Chem. 2018 Sep 13;61(17):7785-7795. doi: 10.1021/acs.jmedchem.8b00765. Epub 2018 Aug 30. PMID:30125504
The dTAG system for immediate and target-specific protein degradation
Nabet B, Roberts JM, Buckley DL, Paulk J, Dastjerdi S, Yang A, Leggett AL, Erb MA, Lawlor MA, Souza A, Scott TG, Vittori S, Perry JA, Qi J, Winter GE, Wong KK, Gray NS, Bradner JE.
Nat Chem Biol. 2018 May;14(5):431-441. doi: 10.1038/s41589-018-0021-8. Epub 2018 Mar 26. PMID:29581585
YAP1-mediated suppression of USP31 enhances NFKB activity to promote sarcomagenesis
Ye S, Lawlor MA, Rivera-Reyes A, Egolf S, Chor S, Pak K, Ciotti GE, Lee AC, Marino G, Shah J, Niedzwicki D, Weber K, Park PMC, Alam MZ, Grazioli A, Haldar M, Xu M, Perry JA, Qi J‡, Eisinger-Mathason TSK‡.
Cancer Res. 2018 May 15;78(10):2705-2720. doi: 10.1158/0008-5472.CAN-17-4052. Epub 2018 Feb 28. PMID:29490948
Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms
Kleppe M, Koche R, Zou L, van Galen P, Hill CE, Dong L, De Groote S, Papalexi E, Hanasoge Somasundara AV, Cordner K, Keller M, Farnoud N, Medina J, McGovern E, Reyes J, Roberts J, Witkin M, Rapaport F, Teruya-Feldstein J, Qi J, Rampal R, Bernstein BE, Bradner JE, Levine RL.
Cancer Cell. 2018 Jan 8;33(1):29-43.e7. doi: 10.1016/j.ccell.2017.11.009. Epub 2017 Dec 14. PMID:29249691
Leukemia-specific delivery of mutant NOTCH1 targeted therapy
Roti G*, Qi J*, Kitara S, Sanchez-Martin M, Saur Conway A, Varca AC, Su A, Wu L, Ferrando AA, Brander JE, Stegmaier K.
J Exp Med. 2018 Jan 2;215(1):197-216. doi: 10.1084/jem.20151778. Epub 2017 Nov 20. PMID:29158376
2017
Synthetic transcription elongation factors license transcription across repressive chromatin
Erwin GS, Grieshop MP, Ali A, Qi J, Lawlor M, Kumar D, Ahmad I, McNally A, Teider N, Worringer K, Sivasankaran R, Syed DN, Eguchi A, Ashraf M, Jeffery J, Xu M, Park PMC, Mukhtar H, Srivastava AK, Faruq M, Bradner JE, Ansari AZ.
Science. 2017 Dec 22;358(6370):1617-1622. doi: 10.1126/science.aan6414. Epub 2017 Nov 30. PMID:29192133
HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer
Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KC.
Oncotarget. 2017 Jul 5;8(46):80109-80123. doi: 10.18632/oncotarget.19019. eCollection 2017 Oct 6. PMID:29113288
Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4
Dai X, Gan W, Li X, Wang S, Zhang W, Huang L, Liu S, Zhong Q, Guo J, Zhang J, Chen T, Shimizu K, Beca F, Blattner M, Vasudevan D, Buckley DL, Qi J, Buser L, Liu P, Inuzuka H, Beck AH, Wang L, Wild PJ, Garraway LA, Rubin MA, Barbieri CE, Wong KK, Muthuswamy SK, Huang J, Chen Y, Bradner JE, Wei W.
Nat Med. 2017 Sep;23(9):1063-1071. doi: 10.1038/nm.4378. Epub 2017 Aug 14. PMID:28805820
HIF activation causes synthetic lethality between the VHL tumor suppressor and the EZH1 histone methyltransferase
Chakraborty AA, Nakamura E, Qi J, Creech A, Jaffe JD, Paulk J, Novak JS, Nagulapalli K, McBrayer SK, Cowley GS, Pineda J, Song J, Wang YE, Carr SA, Root DE, Signoretti S, Bradner JE, Kaelin WG Jr.
Sci Transl Med. 2017 Jul 12;9(398). pii: eaal5272. doi: 10.1126/scitranslmed.aal5272. PMID:28701475
Bromodomain and Extraterminal Protein Inhibitor JQ1 Suppresses Thyroid Tumor Growth in a Mouse Model
Zhu X, Enomoto K, Zhao L, Zhu YJ, Willingham MC, Meltzer P, Qi J, Cheng SY.
Clin Cancer Res. 2017 Jan 15;23(2):430-440. doi: 10.1158/1078-0432.CCR-16-0914. Epub 2016 Jul 20. PMID:27440272
2016
Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma
Hideshima T*, Qi J*, Paranal RM, Tang W, Greenberg E, West N, Colling ME, Estiu G, Mazitschek R, Perry JA, Ohguchi H, Cottini F, Mimura N, Görgün G, Tai YT, Richardson PG, Carrasco RD, Wiest O, Schreiber SL, Anderson KC, Bradner JE.
Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167. Epub 2016 Oct 31. PMID:27799547
Chronic Myelogenous Leukemia- Initiating Cells Require Polycomb Group Protein EZH2
Xie H, Peng C, Huang J, Li BE, Kim W, Smith EC, Fujiwara Y, Qi J, Cheloni G, Das PP, Nguyen M, Li S, Bradner JE, Orkin SH.
Cancer Discov. 2016 Nov;6(11):1237-1247. Epub 2016 Sep 14. PMID:27630126
Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer
Zhang H*, Qi J*, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK.
Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID:27312177
An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation
Souroullas GP, Jeck WR, Parker JS, Simon JM, Liu JY, Paulk J, Xiong J, Clark KS, Fedoriw Y, Qi J, Burd CE, Bradner JE, Sharpless NE.
Nat Med. 2016 Jun;22(6):632-40. doi: 10.1038/nm.4092. Epub 2016 May 2. PMID:27135738
An oncogenic MYB feedback loop drives alternate cell fates in adenoid cystic carcinoma
Drier Y, Cotton MJ, Williamson KE, Gillespie SM, Ryan RJ, Kluk MJ, Carey CD, Rodig SJ, Sholl LM, Afrogheh AH, Faquin WC, Queimado L, Qi J, Wick MJ, El-Naggar AK, Bradner JE, Moskaluk CA, Aster JC, Knoechel B, Bernstein BE.
Nat Genet. 2016 Mar;48(3):265-72. doi: 10.1038/ng.3502. Epub 2016 Feb 1. PMID:26829750
- 2015
Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib
Sun B, Shah B, Fiskus W, Qi J, Rajapakshe K, Coarfa C, Li L, Devaraj SG, Sharma S, Zhang L, Wang ML, Saenz DT, Krieger S, Bradner JE, Bhalla KN.
Blood. 2015 Sep 24;126(13):1565-74. doi: 10.1182/blood-2015-04-639542. Epub 2015 Aug 7. PMID:26254443
Structure-guided DOT1L probe optimization by label-free ligand displacement
Yi JS*, Federation AJ*, Qi J*, Dhe-Paganon S, Hadler M, Xu X, St Pierre R, Varca AC, Wu L, Marineau JJ, Smith WB, Souza A, Chory EJ, Armstrong SA, Bradner JE.
ACS Chem Biol. 2015 Mar 20;10(3):667-74. doi: 10.1021/cb500796d. Epub 2015 Jan 15. PMID:25397901
Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects
Chan CT, Qi J, Smith W, Paranol R, Mazitschek R, West N, Reeves R, Chiosis G, Schreiber SL, Bradner JE, Paulmurugan R, Gambhir SS.
Cancer Res. 2014 Dec 15;74(24):7475-86. doi: 10.1158/0008-5472.CAN-14-0197. Epub 2014 Oct 15. PMID:25320008
Biased multicomponent reactions to develop novel bromodomain inhibitors
McKeown MR, Shaw DL, Fu H, Liu S, Xu X, Marineau JJ, Huang Y, Zhang X, Buckley DL, Kadam A, Zhang Z, Blacklow SC, Qi J, Zhang W, Bradner JE.
J Med Chem. 2014 Nov 13;57(21):9019-27. doi: 10.1021/jm501120z. Epub 2014 Oct 31. PMID:25314271
Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition
Tang Y, Gholamin S, Schubert S, Willardson MI, Lee A, Bandopadhayay P, Bergthold G, Masoud S, Nguyen B, Vue N, Balansay B, Yu F, Oh S, Woo P, Chen S, Ponnuswami A, Monje M, Atwood SX, Whitson RJ, Mitra S, Cheshier SH, Qi J, Beroukhim R, Tang JY, Wechsler-Reya R, Oro AE, Link BA, Bradner JE, Cho YJ.
Nat Med. 2014 Jul;20(7):732-40. doi: 10.1038/nm.3613. Epub 2014 Jun 29. PMID:24973920
c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells
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BET bromodomains mediate transcriptional pause release in heart failure
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Cell. 2013 Aug 1;154(3):569-82. doi: 10.1016/j.cell.2013.07.013. PMID:23911322
Small-molecule inhibition of BRDT for male contraception
Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, Lemieux ME, Picaud S, Yu RN, Qi J, Knapp S, Bradner JE.
Cell. 2012 Aug 17;150(4):673-84. PMID:22901802
BET bromodomain inhibition as a therapeutic strategy to target c-Myc
Delmore JE, Issa GC, Lemieux ME, Rahl PB, Shi J, Jacobs HM, Kastritis E, Gilpatrick T, Paranal RM, Qi J, Chesi M, Schinzel AC, McKeown MR, Heffernan TP, Vakoc CR, Bergsagel PL, Ghobrial IM, Richardson PG, Young RA, Hahn WC, Anderson KC, Kung AL, Bradner JE, Mitsiades CS.
Cell. 2011 Sep 16;146(6):904-17. doi: 10.1016/j.cell.2011.08.017. Epub 2011 Sep 1. PMID:21889194
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia
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Nature. 2011 Aug 3;478(7370):524-8. doi: 10.1038/nature10334. PMID:21814200
Selective inhibition of BET bromodomains
Filippakopoulos P*, Qi J*, Picaud S*, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE.
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Total synthesis of (-)-himandrine
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Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer.Shu S, Wu HJ, Ge JY, Zeid R, Harris IS, Jovanović B, Murphy K, Wang B, Qiu X, Endress JE, Reyes J, Lim K, Font-Tello A, Syamala S, Xiao T, Reddy Chilamakuri CS, Papachristou EK, D'Santos C, Anand J, Hinohara K, Li W, McDonald TO, Luoma A, Modiste RJ, Nguyen QD, Michel B, Cejas P, Kadoch C, Jaffe JD, Wucherpfennig KW, Qi J, Liu XS, Long H, Brown M, Carroll JS, Brugge JS, Bradner J, Michor F, Polyak K.Mol Cell. 2020 Jun 18;78(6):1096-1113.e8. doi: 10.1016/j.molcel.2020.04.027. Epub 2020 May 15.EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma.Durbin AD, Wang T, Wimalasena VK, Zimmerman MW, Li D, Dharia NV, Mariani L, Shendy NAM, Nance S, Patel AG, Shao Y, Mundada M, Maxham L, Park PMC, Sigua LH, Morita K, Saur Conway A, Robichaud AL, Perez-Atayde AR, Bikowitz MJ, Quinn TR, Wiest OG, Easton J, Schonbrunn E, Bulyk ML, Abraham BJ, Stegmaier K, Look AT, Qi J.Cancer Discov. 2021 Nov 12:candisc.0385.2021. doi: 10.1158/2159-8290.CD-21-0385. Online ahead of print.
The FUS::DDIT3 fusion oncoprotein inhibits BAF complex targeting and activity in myxoid liposarcoma.
Zullow HJ, Sankar A, Ingram DR, Samé Guerra DD, D'Avino AR, Collings CK, Lazcano R, Wang WL, Liang Y, Qi J, Lazar AJ, Kadoch C.Mol Cell. 2022 Apr 4:S1097-2765(22)00257-X. doi: 10.1016/j.molcel.2022.03.019. Online ahead of print.PMID: 35390276
Exploring Methods of Targeting Histone Methyltransferases and Their Applications in Cancer Therapeutics.
Wang MY, Liow P, Guzman MIT, Qi J.ACS Chem Biol. 2022 Apr 1. doi: 10.1021/acschembio.2c00062. Online ahead of print.PMID: 35363464
BET-bromodomain and EZH2 inhibitor treated chronic GVHD mice have blunted germinal centers with distinct transcriptomes.
Zaiken MC, Flynn R, Paz KG, Rhee SY, Jin S, Mohamed FA, Saha A, Thangavelu G, Park PMC, Hemming ML, Sage PT, Sharpe AH, DuPage M, Bluestone JA, Panoskaltsis-Mortari A, Cutler CS, Koreth J, Antin JH, Soiffer RJ, Ritz J, Luznik L, Maillard I, Hill GR, MacDonald KP, Munn DH, Serody JS, Murphy WJ, Kean LS, Zhang Y, Bradner JE, Qi J, Blazar BR. Blood. 2022 Feb 28:blood.2021014557. doi: 10.1182/blood.2021014557. Online ahead of print.PMID: 35226736
A PRC2-Kdm5b axis sustains tumorigenicity of acute myeloid leukemia.
Ren Z, Kim A, Huang YT, Pi WC, Gong W, Yu X, Qi J, Jin J, Cai L, Roeder RG, Chen WY, Wang GG.Proc Natl Acad Sci U S A. 2022 Mar 1;119(9):e2122940119. doi: 10.1073/pnas.2122940119.PMID: 35217626
2021
EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma.
Durbin AD*#, Wang T*, Wimalasena VK, Zimmerman MW, Li D, Dharia NV, Mariani L, Shendy NAM, Nance S, Patel AG, Shao Y, Mundada M, Maxham L, Park PMC, Sigua LH, Morita K, Saur Conway A, Robichaud AL, Perez-Atayde AR, Bikowitz MJ, Quinn TR, Wiest OG, Easton J, Schonbrunn E, Bulyk ML, Abraham BJ, Stegmaier K#, Look AT#, Qi J.# Cancer Discovery. 2021 Nov 12:candisc.0385.2021. doi: 10.1158/2159-8290.CD-21-0385. Online ahead of print
Targeting an inducible SALL4-mediated cancer vulnerability with sequential therapy.
Yang J, Gao C, Liu M, Liu YC, Kwon J, Qi J, Tian X, Stein A, Liu YV, Kong NR, Wu Y, Yin S, Xi J, Chen Z, Kumari K, Wong H, Luo H, Silberstein LE, Thoms JAI, Unnikrishnan A, Pimanda JE, Tenen DG, Chai L.Cancer Res. 2021 Sep 30:canres.0030.2021. doi: 10.1158/0008-5472.CAN-21-0030. Online ahead of print.PMID: 34593523
Lysine Demethylase 5A Is Required for MYC-Driven Transcription in Multiple Myeloma
Ohguchi H, Park PMC, Wang T, Gryder BE, Ogiya D, Kurata K, Zhang X, Li D, Pei C, Masuda T, Johansson C, Wimalasena VK, Kim Y, Hino S, Usuki S, Kawano Y, Samur MK, Tai Y, Munshi NC, Matsuoka M, Ohtsuki S, Nakao M, Minami T, Lauberth S, Khan J, Oppermann U, Durbin AD, Anderson KC#, Hideshima T#, Qi J# (Lead Contact). Blood Cancer Discovery, In Press.
Bromodomain protein BRD4 directs and sustains CD8 T cell differentiation during infection.
Milner JJ, Toma C, Quon S, Omilusik K, Scharping NE, Dey A, Reina-Campos M, Nguyen H, Getzler AJ, Diao H, Yu B, Delpoux A, Yoshida TM, Li D, Qi J, Vincek A, Hedrick SM, Egawa T, Zhou MM, Crotty S, Ozato K, Pipkin ME, Goldrath AW.J Exp Med. 2021 Aug 2;218(8):e20202512. doi: 10.1084/jem.20202512. Epub 2021 May 26.PMID: 34037670
Reprogramming of the esophageal squamous carcinoma epigenome by SOX2 promotes ADAR1 dependence.
Wu Z, Zhou J, Zhang X, Zhang Z, Xie Y, Liu JB, Ho ZV, Panda A, Qiu X, Cejas P, Cañadas I, Akarca FG, McFarland JM, Nagaraja AK, Goss LB, Kesten N, Si L, Lim K, Liu Y, Zhang Y, Baek JY, Liu Y, Patil DT, Katz JP, Hai J, Bao C, Stachler M, Qi J, Ishizuka JJ, Nakagawa H, Rustgi AK, Wong KK, Meyerson M, Barbie DA, Brown M, Long H, Bass AJ.Nat Genet. 2021 May 10. doi: 10.1038/s41588-021-00859-2. Online ahead of print.PMID: 33972779
Development of Dimethylisoxazole-Attached Imidazo[1,2-a]pyridines as Potent and Selective CBP/P300 Inhibitors.
Muthengi A,* Wimalasena VK,* Yosief HO,* Bikowitz MJ,* Sigua LH, Wang T, Li D, Gaieb Z, Dhawan G, Liu S, Erickson J, Amaro RE, Schönbrunn E#, Qi J#, Zhang W.# J Med Chem. 2021 Apr 19. doi: 10.1021/acs.jmedchem.0c02232. Online ahead of print. PMID: 33872011
Transcriptional programming drives Ibrutinib-resistance evolution in mantle cell lymphoma.
Zhao X, Wang MY, Jiang H, Lwin T, Park PM, Gao J, Meads MB, Ren Y, Li T, Sun J, Fahmi NA, Singh S, Sehgal L, Wang X, Silva AS, Sotomayor EM, Shain KH, Cleveland JL, Wang M, Zhang W, Qi J, Shah BD, Tao J. Cell Rep. 2021 Mar 16;34(11):108870. doi: 10.1016/j.celrep.2021.108870.PMID: 33730585 Free article.
Brd4 participates in epigenetic regulation of the extinction of remote auditory fear memory.
Huang FL, Li F, Zhang WJ, Li SJ, Yang ZH, Yang TL, Qi J, Duan Q, Li CQ. Neurobiol Learn Mem. 2021 Jan 15;179:107383. doi: 10.1016/j.nlm.2021.107383. Online ahead of print.PMID: 33460788
2020
Inhibition of Polo-like kinase 1 (PLK1) facilitates the elimination of HIV-1 viral reservoirs in CD4+ T cells ex vivo.
Zhou D, Hayashi T, Jean M, Kong W, Fiches G, Biswas A, Liu S, Yosief HO, Zhang X, Bradner J, Qi J, Zhang W, Santoso N, Zhu J. Sci Adv. 2020 Jul 15;6(29):eaba1941. doi: 10.1126/sciadv.aba1941. eCollection 2020 Jul.PMID: 32832623 Free PMC article.
The Folate Cycle Enzyme MTHFR is a Critical Regulator of Cell Response to MYC-Targeting Therapies.
Su A, Ling F, Vaganay C, Sodaro G, Benaksas C, Dal Bello R, Forget A, Pardieu B, Lin KH, Rutter JC, Bassil CF, Fortin G, Pasanisi J, Antony-Debre I, Alexe G, Benoist JF, Pruvost A, Pikman Y, Qi J, Schlageter MH, Micol JB, Roti G, Cluzeau T, Dombret H, Preudhomme C, Fenouille N, Benajiba L, Golan HM, Stegmaier K, Lobry C, Wood KC, Itzykson R, Puissant A.Cancer Discov. 2020 Aug 21:CD-19-0970. doi: 10.1158/2159-8290.CD-19-0970. Online ahead of print.PMID: 32826232
BET proteins inhibitor JQ-1 impaired the extinction of remote auditory fear memory: An effect mediated by insulin like growth factor 2.
Duan Q, Huang FL, Li SJ, Chen KZ, Gong L, Qi J, Yang ZH, Yang TL, Li F, Li CQ. Neuropharmacology. 2020 Oct 15;177:108255. doi: 10.1016/j.neuropharm.2020.108255. Epub 2020 Jul 28.
High-performance CRISPR-Cas12a genome editing for combinatorial genetic screening.
Gier RA, Budinich KA, Evitt NH, Cao Z, Freilich ES, Chen Q, Qi J, Lan Y, Kohli RM, Shi J.
Nat Commun. 2020 Jul 13;11(1):3455. doi: 10.1038/s41467-020-17209-1.
Epigenetic CRISPR screens identify Npm1 as a therapeutic vulnerability in non-small cell lung cancer.
Li F*, Ng WL*, Luster TA, Hu H, Sviderskiy VO, Dowling CM, Hollinshead KER, Zouitine P, Zhang H, Huang Q, Ranieri M, Wang W, Fang Z, Chen T, Deng J, Zhao K, So HC, Khodadadi-Jamayran A, Xu M, Karatza A, Pyon V, Li S, Pan Y, Labbe K, Almonte C, Poirier JT, Miller G, Possemato R, Qi J#, Wong KK#.
Cancer Res. 2020 Jul 9:canres.3782.2019. doi: 10.1158/0008-5472.CAN-19-3782. Online ahead of print.
BET bromodomain proteins regulate transcriptional reprogramming in genetic dilated cardiomyopathy.
Antolic A, Wakimoto H, Jiao Z, Gorham JM, DePalma SR, Lemieux ME, Conner DA, Lee DY, Qi J, Seidman JG, Bradner JE, Brown JD, Haldar SM, Seidman CE, Burke MA. JCI Insight. 2020 Jun 30:138687. doi: 10.1172/jci.insight.138687. Online ahead of print.
Peptide-Based PROTAC: The Predator of Pathological Proteins.
Au YZ, Wang T, Sigua LH, Qi J. Cell Chem Biol. 2020 Jun 18;27(6):637-639.
Selective Targeting of Different Bromodomains by Small Molecules.
Qi J, Shi Y.Cancer Cell. 2020 Jun 8;37(6):764-766.
Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer.
Shu S, Wu HJ, Ge JY, Zeid R, Harris IS, Jovanović B, Murphy K, Wang B, Qiu X, Endress JE, Reyes J, Lim K, Font-Tello A, Syamala S, Xiao T, Reddy Chilamakuri CS, Papachristou EK, D'Santos C, Anand J, Hinohara K, Li W, McDonald TO, Luoma A, Modiste RJ, Nguyen QD, Michel B, Cejas P, Kadoch C, Jaffe JD, Wucherpfennig KW, Qi J, Liu XS, Long H, Brown M, Carroll JS, Brugge JS, Bradner J, Michor F, Polyak K.Mol Cell. 2020 Jun 18;78(6):1096-1113.
Using Chemical Epigenetics to Target Cancer.
Wimalasena VK*, Wang T*, Sigua LH*, Durbin AD#, Qi J#.
Molecular Cell. 2020 May 5. pii: S1097-2765(20)30265-3. doi: 10.1016/j.molcel.2020.04.023. [Epub ahead of print] Review.
Acquired resistance to combined BET and CDK4/6 inhibition in triple-negative breast cancer.
Ge JY, Shu S, Kwon M, Jovanović B, Murphy K, Gulvady A, Fassl A, Trinh A, Kuang Y, Heavey GA, Luoma A, Paweletz C, Thorner AR, Wucherpfennig KW, Qi J, Brown M, Sicinski P, McDonald TO, Pellman D, Michor F, Polyak K.
Nature Communication. 2020 May 11;11(1):2350. doi: 10.1038/s41467-020-16170-3.
In vivo epigenetic CRISPR screen identifies Asf1a as an immunotherapeutic target in Kras-mutant lung adenocarcinoma.
Li F, Huang Q, Luster TA, Hu H, Zhang H, Ng WL, Khodadadi-Jamayran A, Wang W, Chen T, Deng J, Ranieri M, Fang Z, Pyon V, Dowling CM, Bagdatlioglu E, Almonte C, Labbe K, Silver H, Rabin AR, Jani K, Tsirigos A, Papagiannakopoulos T, Hammerman PS, Velcheti V, Freeman GJ, Qi J, Miller G, Wong KK.
Cancer Discovery. 2020 Feb;10(2):270-287. doi: 10.1158/2159-8290.CD-19-0780. Epub 2019 Nov 19.
BET bromodomain inhibition suppresses adipogenesis in mice.
Duan Q, Wu P, Liu Z, Xia F, Zhu L, Zheng Z, Yang T, Qi J.
Endocrine. 2020 Jan;67(1):264-267. doi: 10.1007/s12020-019-02115-4. Epub 2019 Nov 5.
2019
Diversified Application of Barcoded PLATO (PLATO-BC) Platform for Identification of Protein Interactions.
Kong W, Hayashi T, Fiches G, Xu Q, Li MZ, Que J, Liu S, Zhang W, Qi J, Santoso N, Elledge SJ, Zhu J.
Genomics Proteomics Bioinformatics. 2019 Jun;17(3):319-331. doi: 10.1016/j.gpb.2018.12.010. Epub 2019 Sep 5.
Dynamic Chromatin Targeting of BRD4 Stimulates Cardiac Fibroblast Activation.
Stratton MS, Bagchi RA, Felisbino MB, Hirsch RA, Smith HE, Riching AS, Enyart BY, Koch KA, Cavasin MA, Alexanian M, Song K, Qi J, Lemieux ME, Srivastava D, Lam MPY, Haldar SM, Lin CY, McKinsey TA.
Circulation Research. 2019 Sep 13;125(7):662-677. doi: 10.1161/CIRCRESAHA.119.315125. Epub 2019 Aug 14.
Chemical genomics reveals histone deacetylases are required for core regulatory transcription
Berkley E. Gryder*, Lei Wu*, Girma M. Woldemichael, Silvia Pomella, Taylor R. Quinn, Paul M. C. Park, Abigail Cleveland, Benjamin Z. Stanton, Young Song, Rossella Rota, Olaf Wiest, Marielle E. Yohe, Jack F. Shern, Jun Qi‡ & Javed Khan‡.
Nature Communications. 2019 July 08; doi: 10.1038/s41467-019-11046-7
Neuronal differentiation and cell-cycle programs mediate response to BET-bromodomain inhibition in MYC-driven medulloblastoma.
Bandopadhayay P, Piccioni F, O'Rourke R, Ho P, Gonzalez EM, Buchan G, Qian K, Gionet G, Girard E, Coxon M, Rees MG, Brenan L, Dubois F, Shapira O, Greenwald NF, Pages M, Balboni Iniguez A, Paolella BR, Meng A, Sinai C, Roti G, Dharia NV, Creech A, Tanenbaum B, Khadka P, Tracy A, Tiv HL, Hong AL, Coy S, Rashid R, Lin JR, Cowley GS, Lam FC, Goodale A, Lee Y, Schoolcraft K, Vazquez F, Hahn WC, Tsherniak A, Bradner JE, Yaffe MB, Milde T, Pfister SM, Qi J, Schenone M, Carr SA, Ligon KL, Kieran MW, Santagata S, Olson JM, Gokhale PC, Jaffe JD, Root DE, Stegmaier K, Johannessen CM, Beroukhim R.
Nature Communications. 2019 Jun 3;10(1):2400. doi: 10.1038/s41467-019-10307-9.
A large-scale drug screen identifies selective inhibitors of class I HDACs as a potential therapeutic option for SHH medulloblastoma.
Pak E, MacKenzie EL, Zhao X, Pazyra-Murphy MF, Park PMC, Wu L, Shaw DL, Addleson EC, Cayer SS, Lopez BG, Agar NYR, Rubin LL, Qi J, Merk DJ, Segal RA.
Neuro-Oncology. 2019 May 16. pii: noz089. doi: 10.1093/neuonc/noz089.
BCL2 Amplicon loss and transcriptional remodeling drives ABT-199 resistance in B-cell lymphoma models
Zhao X*, Ren Y*, Lawlor MA*, Shah BD, Park PMC, Lwin T, Wang X, Liu K, Wang M, Gao J, Li T, Xu M, Silva AS, Lee K, Zhang T, Koomen JM, Jiang H, Sudalagunta PR, Meads MB, Cheng F, Bi C, Fu K, Fan H, Dalton WS, Moscinski LC, Shain KH, Sotomayor EM, Wang GG, Gray NS, Cleveland JL, Qi J‡, Tao J‡.
Cancer Cell. 2019 May 13;35(5):752-766.e9. doi: 10.1016/j.ccell.2019.04.005. PMID: 31085176
Development and preclinical validation of a novel covalent ubiquitin receptor Rpn13 degrader in multiple myeloma
Song Y*, Park PMC*, Wu L, Ray A, Picaud S, Li D, Wimalasena VK, Du T, Filippakopoulos P, Anderson KC‡, Qi J‡, Chauhan D‡.
Leukemia. 2019 April 08; doi: 10.1038/s41375-019-0467-z. PMID:30962579
2018
Resistance to epigenetic-targeted therapy engenders tumor cell vulnerabilities associated with enhancer remodeling
Iniguez AB, Alexe G, Wang EJ, Roti G, Patel S, Chen L, Kitara S, Conway A, Robichaud AL, Stolte B, Bandopadhayay P, Goodale A, Pantel S, Lee Y, Cheff DM, Hall MD, Guha R, Davis MI, Menard M, Nasholm N, Weiss WA, Qi J, Beroukhim R, Piccioni F, Johannessen C, Stegmaier K.
Cancer Cell. 2018 Dec 10;34(6):922-938.e7. doi: 10.1016/j.ccell.2018.11.005. PMID:30537514
YAP1 enhances NF-KB-depedent and independent effects on clock-mediated unfolded protein responses and autophagy in sarcoma
Rivera-Reyes A, Ye S, Marino G, Egolf S, Ciotti G, Chor S, Liu Y, Posimo J, Park PMC, Pak K, Babichev Y, Sostre-Colon J, Tameire F, Leli N, Koumenis C, Brady D, Mancuso A, Weber K, Gladdy R, Qi J, Eisinger-Mathanson TSK.
Cell Death Dis. 2018 Oct 31;9(11):1108. doi: 10.1038/s41419-018-1142-4. PMID:30382078
Small-molecule BCL6 inhibitor effectively treats mice with nonsclerodermatous chronice graft-versus-host disease
Paz K, Flynn R, Du J, Qi J, Luznik L, Maillard I, MacDonald KP, Hill GR, Serody JS, Murphy WJ, Sage PT, Sharpe AH, Miklos D, Cutler CS, Koreth J, Antin JH, Soiffer RJ, Ritz J, Bradner JE, Melnick AM, Blazar BR.
Blood. 2018 Oct 2. doi: 10.1182/blood-2018-03-839993. [Epub ahead of print] PMID: 30279226
Structural and atropisomeric factors governing the selectivity of pyrimido-benzodiazipinones as inhibitors of kinases and bromodomains
Wang J, Erazo T, Ferguson FM, Buckley DL, Gomez N, Muñoz-Guardiola P, Diéguez-Martinez N, Deng X, Hao M, Massefski W, Fedorov O, Offei-Addo NK, Park PM, Dai L, DiBona A, Becht K, Kim ND, McKeown MR, Roberts JM, Zhang J, Sim T, Alessi DR, Bradner JE, Lizcano JM, Blacklow SC, Qi J, Xu X, Gray NS.
ACS Chem Biol. 2018 Sep 21;13(9):2438-2448. doi: 10.1021/acschembio.7b00638. Epub 2018 Aug 31. PMID:30102854
Structure-guided design and development of potent and selective dual bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) inhibitors
Liu S, Yosief HO, Dai L, Huang H, Dhawan G, Zhang X, Muthengi AM, Roberts J, Buckley DL, Perry JA, Wu L, Bradner JE, Qi J‡, Zhang W‡.
J Med Chem. 2018 Sep 13;61(17):7785-7795. doi: 10.1021/acs.jmedchem.8b00765. Epub 2018 Aug 30. PMID:30125504
The dTAG system for immediate and target-specific protein degradation
Nabet B, Roberts JM, Buckley DL, Paulk J, Dastjerdi S, Yang A, Leggett AL, Erb MA, Lawlor MA, Souza A, Scott TG, Vittori S, Perry JA, Qi J, Winter GE, Wong KK, Gray NS, Bradner JE.
Nat Chem Biol. 2018 May;14(5):431-441. doi: 10.1038/s41589-018-0021-8. Epub 2018 Mar 26. PMID:29581585
YAP1-mediated suppression of USP31 enhances NFKB activity to promote sarcomagenesis
Ye S, Lawlor MA, Rivera-Reyes A, Egolf S, Chor S, Pak K, Ciotti GE, Lee AC, Marino G, Shah J, Niedzwicki D, Weber K, Park PMC, Alam MZ, Grazioli A, Haldar M, Xu M, Perry JA, Qi J‡, Eisinger-Mathason TSK‡.
Cancer Res. 2018 May 15;78(10):2705-2720. doi: 10.1158/0008-5472.CAN-17-4052. Epub 2018 Feb 28. PMID:29490948
Dual Targeting of Oncogenic Activation and Inflammatory Signaling Increases Therapeutic Efficacy in Myeloproliferative Neoplasms
Kleppe M, Koche R, Zou L, van Galen P, Hill CE, Dong L, De Groote S, Papalexi E, Hanasoge Somasundara AV, Cordner K, Keller M, Farnoud N, Medina J, McGovern E, Reyes J, Roberts J, Witkin M, Rapaport F, Teruya-Feldstein J, Qi J, Rampal R, Bernstein BE, Bradner JE, Levine RL.
Cancer Cell. 2018 Jan 8;33(1):29-43.e7. doi: 10.1016/j.ccell.2017.11.009. Epub 2017 Dec 14. PMID:29249691
Leukemia-specific delivery of mutant NOTCH1 targeted therapy
Roti G*, Qi J*, Kitara S, Sanchez-Martin M, Saur Conway A, Varca AC, Su A, Wu L, Ferrando AA, Brander JE, Stegmaier K.
J Exp Med. 2018 Jan 2;215(1):197-216. doi: 10.1084/jem.20151778. Epub 2017 Nov 20. PMID:29158376
2017
Synthetic transcription elongation factors license transcription across repressive chromatin
Erwin GS, Grieshop MP, Ali A, Qi J, Lawlor M, Kumar D, Ahmad I, McNally A, Teider N, Worringer K, Sivasankaran R, Syed DN, Eguchi A, Ashraf M, Jeffery J, Xu M, Park PMC, Mukhtar H, Srivastava AK, Faruq M, Bradner JE, Ansari AZ.
Science. 2017 Dec 22;358(6370):1617-1622. doi: 10.1126/science.aan6414. Epub 2017 Nov 30. PMID:29192133
HDAC6 inhibitor WT161 downregulates growth factor receptors in breast cancer
Hideshima T, Mazitschek R, Qi J, Mimura N, Tseng JC, Kung AL, Bradner JE, Anderson KC.
Oncotarget. 2017 Jul 5;8(46):80109-80123. doi: 10.18632/oncotarget.19019. eCollection 2017 Oct 6. PMID:29113288
Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4
Dai X, Gan W, Li X, Wang S, Zhang W, Huang L, Liu S, Zhong Q, Guo J, Zhang J, Chen T, Shimizu K, Beca F, Blattner M, Vasudevan D, Buckley DL, Qi J, Buser L, Liu P, Inuzuka H, Beck AH, Wang L, Wild PJ, Garraway LA, Rubin MA, Barbieri CE, Wong KK, Muthuswamy SK, Huang J, Chen Y, Bradner JE, Wei W.
Nat Med. 2017 Sep;23(9):1063-1071. doi: 10.1038/nm.4378. Epub 2017 Aug 14. PMID:28805820
HIF activation causes synthetic lethality between the VHL tumor suppressor and the EZH1 histone methyltransferase
Chakraborty AA, Nakamura E, Qi J, Creech A, Jaffe JD, Paulk J, Novak JS, Nagulapalli K, McBrayer SK, Cowley GS, Pineda J, Song J, Wang YE, Carr SA, Root DE, Signoretti S, Bradner JE, Kaelin WG Jr.
Sci Transl Med. 2017 Jul 12;9(398). pii: eaal5272. doi: 10.1126/scitranslmed.aal5272. PMID:28701475
Bromodomain and Extraterminal Protein Inhibitor JQ1 Suppresses Thyroid Tumor Growth in a Mouse Model
Zhu X, Enomoto K, Zhao L, Zhu YJ, Willingham MC, Meltzer P, Qi J, Cheng SY.
Clin Cancer Res. 2017 Jan 15;23(2):430-440. doi: 10.1158/1078-0432.CCR-16-0914. Epub 2016 Jul 20. PMID:27440272
2016
Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma
Hideshima T*, Qi J*, Paranal RM, Tang W, Greenberg E, West N, Colling ME, Estiu G, Mazitschek R, Perry JA, Ohguchi H, Cottini F, Mimura N, Görgün G, Tai YT, Richardson PG, Carrasco RD, Wiest O, Schreiber SL, Anderson KC, Bradner JE.
Proc Natl Acad Sci U S A. 2016 Nov 15;113(46):13162-13167. Epub 2016 Oct 31. PMID:27799547
Chronic Myelogenous Leukemia- Initiating Cells Require Polycomb Group Protein EZH2
Xie H, Peng C, Huang J, Li BE, Kim W, Smith EC, Fujiwara Y, Qi J, Cheloni G, Das PP, Nguyen M, Li S, Bradner JE, Orkin SH.
Cancer Discov. 2016 Nov;6(11):1237-1247. Epub 2016 Sep 14. PMID:27630126
Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer
Zhang H*, Qi J*, Reyes JM, Li L, Rao PK, Li F, Lin CY, Perry JA, Lawlor MA, Federation A, De Raedt T, Li YY, Liu Y, Duarte MA, Zhang Y, Herter-Sprie GS, Kikuchi E, Carretero J, Perou CM, Reibel JB, Paulk J, Bronson RT, Watanabe H, Brainson CF, Kim CF, Hammerman PS, Brown M, Cichowski K, Long H, Bradner JE, Wong KK.
Cancer Discov. 2016 Sep;6(9):1006-21. doi: 10.1158/2159-8290.CD-16-0164. Epub 2016 Jun 16. PMID:27312177
An oncogenic Ezh2 mutation induces tumors through global redistribution of histone 3 lysine 27 trimethylation
Souroullas GP, Jeck WR, Parker JS, Simon JM, Liu JY, Paulk J, Xiong J, Clark KS, Fedoriw Y, Qi J, Burd CE, Bradner JE, Sharpless NE.
Nat Med. 2016 Jun;22(6):632-40. doi: 10.1038/nm.4092. Epub 2016 May 2. PMID:27135738
An oncogenic MYB feedback loop drives alternate cell fates in adenoid cystic carcinoma
Drier Y, Cotton MJ, Williamson KE, Gillespie SM, Ryan RJ, Kluk MJ, Carey CD, Rodig SJ, Sholl LM, Afrogheh AH, Faquin WC, Queimado L, Qi J, Wick MJ, El-Naggar AK, Bradner JE, Moskaluk CA, Aster JC, Knoechel B, Bernstein BE.
Nat Genet. 2016 Mar;48(3):265-72. doi: 10.1038/ng.3502. Epub 2016 Feb 1. PMID:26829750
- 2015
Synergistic activity of BET protein antagonist-based combinations in mantle cell lymphoma cells sensitive or resistant to ibrutinib
Sun B, Shah B, Fiskus W, Qi J, Rajapakshe K, Coarfa C, Li L, Devaraj SG, Sharma S, Zhang L, Wang ML, Saenz DT, Krieger S, Bradner JE, Bhalla KN.
Blood. 2015 Sep 24;126(13):1565-74. doi: 10.1182/blood-2015-04-639542. Epub 2015 Aug 7. PMID:26254443
Structure-guided DOT1L probe optimization by label-free ligand displacement
Yi JS*, Federation AJ*, Qi J*, Dhe-Paganon S, Hadler M, Xu X, St Pierre R, Varca AC, Wu L, Marineau JJ, Smith WB, Souza A, Chory EJ, Armstrong SA, Bradner JE.
ACS Chem Biol. 2015 Mar 20;10(3):667-74. doi: 10.1021/cb500796d. Epub 2015 Jan 15. PMID:25397901
Syntheses and discovery of a novel class of cinnamic hydroxamates as histone deacetylase inhibitors by multimodality molecular imaging in living subjects
Chan CT, Qi J, Smith W, Paranol R, Mazitschek R, West N, Reeves R, Chiosis G, Schreiber SL, Bradner JE, Paulmurugan R, Gambhir SS.
Cancer Res. 2014 Dec 15;74(24):7475-86. doi: 10.1158/0008-5472.CAN-14-0197. Epub 2014 Oct 15. PMID:25320008
Biased multicomponent reactions to develop novel bromodomain inhibitors
McKeown MR, Shaw DL, Fu H, Liu S, Xu X, Marineau JJ, Huang Y, Zhang X, Buckley DL, Kadam A, Zhang Z, Blacklow SC, Qi J, Zhang W, Bradner JE.
J Med Chem. 2014 Nov 13;57(21):9019-27. doi: 10.1021/jm501120z. Epub 2014 Oct 31. PMID:25314271
Epigenetic targeting of Hedgehog pathway transcriptional output through BET bromodomain inhibition
Tang Y, Gholamin S, Schubert S, Willardson MI, Lee A, Bandopadhayay P, Bergthold G, Masoud S, Nguyen B, Vue N, Balansay B, Yu F, Oh S, Woo P, Chen S, Ponnuswami A, Monje M, Atwood SX, Whitson RJ, Mitra S, Cheshier SH, Qi J, Beroukhim R, Tang JY, Wechsler-Reya R, Oro AE, Link BA, Bradner JE, Cho YJ.
Nat Med. 2014 Jul;20(7):732-40. doi: 10.1038/nm.3613. Epub 2014 Jun 29. PMID:24973920
c-Myc inhibition prevents leukemia initiation in mice and impairs the growth of relapsed and induction failure pediatric T-ALL cells
Roderick JE, Tesell J, Shultz LD, Brehm MA, Greiner DL, Harris MH, Silverman LB, Sallan SE, Gutierrez A, Look AT, Qi J, Bradner JE, Kelliher MA.
Blood. 2014 Feb 13;123(7):1040-50. doi: 10.1182/blood-2013-08-522698. Epub 2014 Jan 6. PMID:24394663
Genome-wide localization of small molecules
Anders L, Guenther MG, Qi J, Fan ZP, Marineau JJ, Rahl PB, Lovén J, Sigova AA, Smith WB, Lee TI, Bradner JE, Young RA.
Nat Biotechnol. 2014 Jan;32(1):92-6. doi: 10.1038/nbt.2776. Epub 2013 Dec 15. PMID:24336317
BET bromodomains mediate transcriptional pause release in heart failure
Anand P, Brown JD, Lin CY, Qi J, Zhang R, Artero PC, Alaiti MA, Bullard J, Alazem K, Margulies KB, Cappola TP, Lemieux M, Plutzky J, Bradner JE, Haldar SM.
Cell. 2013 Aug 1;154(3):569-82. doi: 10.1016/j.cell.2013.07.013. PMID:23911322
Small-molecule inhibition of BRDT for male contraception
Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, Lemieux ME, Picaud S, Yu RN, Qi J, Knapp S, Bradner JE.
Cell. 2012 Aug 17;150(4):673-84. PMID:22901802
BET bromodomain inhibition as a therapeutic strategy to target c-Myc
Delmore JE, Issa GC, Lemieux ME, Rahl PB, Shi J, Jacobs HM, Kastritis E, Gilpatrick T, Paranal RM, Qi J, Chesi M, Schinzel AC, McKeown MR, Heffernan TP, Vakoc CR, Bergsagel PL, Ghobrial IM, Richardson PG, Young RA, Hahn WC, Anderson KC, Kung AL, Bradner JE, Mitsiades CS.
Cell. 2011 Sep 16;146(6):904-17. doi: 10.1016/j.cell.2011.08.017. Epub 2011 Sep 1. PMID:21889194
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia
Zuber J, Shi J, Wang E, Rappaport AR, Herrmann H, Sison EA, Magoon D, Qi J, Blatt K, Wunderlich M, Taylor MJ, Johns C, Chicas A, Mulloy JC, Kogan SC, Brown P, Valent P, Bradner JE, Lowe SW, Vakoc CR.
Nature. 2011 Aug 3;478(7370):524-8. doi: 10.1038/nature10334. PMID:21814200
Selective inhibition of BET bromodomains
Filippakopoulos P*, Qi J*, Picaud S*, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE.
Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. PMID:20871596
Total synthesis of (-)-himandrine
Movassaghi M, Tjandra M, Qi J.
J Am Chem Soc. 2009 Jul 22;131(28):9648-50. doi: 10.1021/ja903790y. PMID:19555115
* equal contribution
‡ shared corresponding authors
Synthetic Lethal and Resistance Interactions with BET Bromodomain Inhibitors in Triple-Negative Breast Cancer.Shu S, Wu HJ, Ge JY, Zeid R, Harris IS, Jovanović B, Murphy K, Wang B, Qiu X, Endress JE, Reyes J, Lim K, Font-Tello A, Syamala S, Xiao T, Reddy Chilamakuri CS, Papachristou EK, D'Santos C, Anand J, Hinohara K, Li W, McDonald TO, Luoma A, Modiste RJ, Nguyen QD, Michel B, Cejas P, Kadoch C, Jaffe JD, Wucherpfennig KW, Qi J, Liu XS, Long H, Brown M, Carroll JS, Brugge JS, Bradner J, Michor F, Polyak K.Mol Cell. 2020 Jun 18;78(6):1096-1113.e8. doi: 10.1016/j.molcel.2020.04.027. Epub 2020 May 15.EP300 selectively controls the enhancer landscape of MYCN-amplified neuroblastoma.Durbin AD, Wang T, Wimalasena VK, Zimmerman MW, Li D, Dharia NV, Mariani L, Shendy NAM, Nance S, Patel AG, Shao Y, Mundada M, Maxham L, Park PMC, Sigua LH, Morita K, Saur Conway A, Robichaud AL, Perez-Atayde AR, Bikowitz MJ, Quinn TR, Wiest OG, Easton J, Schonbrunn E, Bulyk ML, Abraham BJ, Stegmaier K, Look AT, Qi J.Cancer Discov. 2021 Nov 12:candisc.0385.2021. doi: 10.1158/2159-8290.CD-21-0385. Online ahead of print.