Click here to view all research publications from the Qi laboratory.
Selected Publications
2019
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
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
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
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