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Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma.
Poon E, Liang T, Jamin Y, Walz S, Kwok C, Hakkert A, Barker K, Urban Z, Thway K, Zeid R, Hallsworth A, Box G, Ebus ME, Licciardello MP, Sbirkov Y, Lazaro G, Calton E, Costa BM, Valenti M, De Haven Brandon A, Webber H, Tardif N, Almeida GS, Christova R, Boysen G, Richards MW, Barone G, Ford A, Bayliss R, Clarke PA, De Bono J, Gray NS, Blagg J, Robinson SP, Eccles SA, Zheleva D, Bradner JE, Molenaar J, Vivanco I, Eilers M, Workman P, Lin CY, Chesler L. Poon E, et al. Among authors: gray ns. J Clin Invest. 2020 Nov 2;130(11):5875-5892. doi: 10.1172/JCI134132. J Clin Invest. 2020. PMID: 33016930 Free PMC article.
The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma.
Berry T, Luther W, Bhatnagar N, Jamin Y, Poon E, Sanda T, Pei D, Sharma B, Vetharoy WR, Hallsworth A, Ahmad Z, Barker K, Moreau L, Webber H, Wang W, Liu Q, Perez-Atayde A, Rodig S, Cheung NK, Raynaud F, Hallberg B, Robinson SP, Gray NS, Pearson AD, Eccles SA, Chesler L, George RE. Berry T, et al. Among authors: gray ns. Cancer Cell. 2012 Jul 10;22(1):117-30. doi: 10.1016/j.ccr.2012.06.001. Cancer Cell. 2012. PMID: 22789543 Free PMC article.
A public-private partnership to unlock the untargeted kinome.
Knapp S, Arruda P, Blagg J, Burley S, Drewry DH, Edwards A, Fabbro D, Gillespie P, Gray NS, Kuster B, Lackey KE, Mazzafera P, Tomkinson NC, Willson TM, Workman P, Zuercher WJ. Knapp S, et al. Among authors: gray ns. Nat Chem Biol. 2013 Jan;9(1):3-6. doi: 10.1038/nchembio.1113. Nat Chem Biol. 2013. PMID: 23238671 No abstract available.
CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer.
Chipumuro E, Marco E, Christensen CL, Kwiatkowski N, Zhang T, Hatheway CM, Abraham BJ, Sharma B, Yeung C, Altabef A, Perez-Atayde A, Wong KK, Yuan GC, Gray NS, Young RA, George RE. Chipumuro E, et al. Among authors: gray ns. Cell. 2014 Nov 20;159(5):1126-1139. doi: 10.1016/j.cell.2014.10.024. Epub 2014 Nov 6. Cell. 2014. PMID: 25416950 Free PMC article.
Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor.
Christensen CL, Kwiatkowski N, Abraham BJ, Carretero J, Al-Shahrour F, Zhang T, Chipumuro E, Herter-Sprie GS, Akbay EA, Altabef A, Zhang J, Shimamura T, Capelletti M, Reibel JB, Cavanaugh JD, Gao P, Liu Y, Michaelsen SR, Poulsen HS, Aref AR, Barbie DA, Bradner JE, George RE, Gray NS, Young RA, Wong KK. Christensen CL, et al. Among authors: gray ns. Cancer Cell. 2014 Dec 8;26(6):909-922. doi: 10.1016/j.ccell.2014.10.019. Cancer Cell. 2014. PMID: 25490451 Free PMC article.
Inhibiting the oncogenic translation program is an effective therapeutic strategy in multiple myeloma.
Manier S, Huynh D, Shen YJ, Zhou J, Yusufzai T, Salem KZ, Ebright RY, Shi J, Park J, Glavey SV, Devine WG, Liu CJ, Leleu X, Quesnel B, Roche-Lestienne C, Snyder JK, Brown LE, Gray N, Bradner J, Whitesell L, Porco JA Jr, Ghobrial IM. Manier S, et al. Sci Transl Med. 2017 May 10;9(389):eaal2668. doi: 10.1126/scitranslmed.aal2668. Sci Transl Med. 2017. PMID: 28490664 Free PMC article.
BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.
Winter GE, Mayer A, Buckley DL, Erb MA, Roderick JE, Vittori S, Reyes JM, di Iulio J, Souza A, Ott CJ, Roberts JM, Zeid R, Scott TG, Paulk J, Lachance K, Olson CM, Dastjerdi S, Bauer S, Lin CY, Gray NS, Kelliher MA, Churchman LS, Bradner JE. Winter GE, et al. Among authors: gray ns. Mol Cell. 2017 Jul 6;67(1):5-18.e19. doi: 10.1016/j.molcel.2017.06.004. Epub 2017 Jun 29. Mol Cell. 2017. PMID: 28673542 Free PMC article.
MELK is not necessary for the proliferation of basal-like breast cancer cells.
Huang HT, Seo HS, Zhang T, Wang Y, Jiang B, Li Q, Buckley DL, Nabet B, Roberts JM, Paulk J, Dastjerdi S, Winter GE, McLauchlan H, Moran J, Bradner JE, Eck MJ, Dhe-Paganon S, Zhao JJ, Gray NS. Huang HT, et al. Among authors: gray ns. Elife. 2017 Sep 19;6:e26693. doi: 10.7554/eLife.26693. Elife. 2017. PMID: 28926338 Free PMC article.
560 results