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Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7.
Marineau JJ, Hamman KB, Hu S, Alnemy S, Mihalich J, Kabro A, Whitmore KM, Winter DK, Roy S, Ciblat S, Ke N, Savinainen A, Wilsily A, Malojcic G, Zahler R, Schmidt D, Bradley MJ, Waters NJ, Chuaqui C. Marineau JJ, et al. J Med Chem. 2022 Jan 27;65(2):1458-1480. doi: 10.1021/acs.jmedchem.1c01171. Epub 2021 Nov 2. J Med Chem. 2022. PMID: 34726887 Free article.
Discovery and Characterization of SY-1365, a Selective, Covalent Inhibitor of CDK7.
Hu S, Marineau JJ, Rajagopal N, Hamman KB, Choi YJ, Schmidt DR, Ke N, Johannessen L, Bradley MJ, Orlando DA, Alnemy SR, Ren Y, Ciblat S, Winter DK, Kabro A, Sprott KT, Hodgson JG, Fritz CC, Carulli JP, di Tomaso E, Olson ER. Hu S, et al. Among authors: marineau jj. Cancer Res. 2019 Jul 1;79(13):3479-3491. doi: 10.1158/0008-5472.CAN-19-0119. Epub 2019 May 7. Cancer Res. 2019. PMID: 31064851
Selective inhibition of CDK7 reveals high-confidence targets and new models for TFIIH function in transcription.
Rimel JK, Poss ZC, Erickson B, Maas ZL, Ebmeier CC, Johnson JL, Decker TM, Yaron TM, Bradley MJ, Hamman KB, Hu S, Malojcic G, Marineau JJ, White PW, Brault M, Tao L, DeRoy P, Clavette C, Nayak S, Damon LJ, Kaltheuner IH, Bunch H, Cantley LC, Geyer M, Iwasa J, Dowell RD, Bentley DL, Old WM, Taatjes DJ. Rimel JK, et al. Among authors: marineau jj. Genes Dev. 2020 Nov 1;34(21-22):1452-1473. doi: 10.1101/gad.341545.120. Epub 2020 Oct 15. Genes Dev. 2020. PMID: 33060135 Free PMC article.
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. McKeown MR, et al. Among authors: marineau jj. J Med Chem. 2014 Nov 13;57(21):9019-27. doi: 10.1021/jm501120z. Epub 2014 Oct 31. J Med Chem. 2014. PMID: 25314271 Free PMC article.
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Yu W, et al. Among authors: marineau jj. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304. Nat Commun. 2012. PMID: 23250418 Free article.
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. Yi JS, et al. Among authors: marineau jj. ACS Chem Biol. 2015 Mar 20;10(3):667-74. doi: 10.1021/cb500796d. Epub 2015 Jan 15. ACS Chem Biol. 2015. PMID: 25397901 Free PMC article.
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. Anders L, et al. Among authors: marineau jj. Nat Biotechnol. 2014 Jan;32(1):92-6. doi: 10.1038/nbt.2776. Epub 2013 Dec 15. Nat Biotechnol. 2014. PMID: 24336317 Free PMC article.
Phenothiazines induce PP2A-mediated apoptosis in T cell acute lymphoblastic leukemia.
Gutierrez A, Pan L, Groen RW, Baleydier F, Kentsis A, Marineau J, Grebliunaite R, Kozakewich E, Reed C, Pflumio F, Poglio S, Uzan B, Clemons P, VerPlank L, An F, Burbank J, Norton S, Tolliday N, Steen H, Weng AP, Yuan H, Bradner JE, Mitsiades C, Look AT, Aster JC. Gutierrez A, et al. J Clin Invest. 2014 Feb;124(2):644-55. doi: 10.1172/JCI65093. Epub 2014 Jan 9. J Clin Invest. 2014. PMID: 24401270 Free PMC article.
12 results