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Page 1
Discovery of Potent Azetidine-Benzoxazole MerTK Inhibitors with In Vivo Target Engagement.
Frey RR, Jana N, Gorman JV, Wang J, Smith HA, Bromberg KD, Thakur A, Doktor SZ, Indulkar AS, Jakob CG, Upadhyay AK, Qiu W, Manaves V, Gambino F Jr, Valentino SA, Montgomery D, Zhou Y, Li T, Buchanan FG, Ferguson DC, Kurnick MD, Kapecki N, Lai A, Michaelides MR, Penning TD. Frey RR, et al. Among authors: michaelides mr. J Med Chem. 2024 Oct 10;67(19):17033-17052. doi: 10.1021/acs.jmedchem.4c01451. Epub 2024 Sep 30. J Med Chem. 2024. PMID: 39350472
Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases.
Ji Z, Clark RF, Bhat V, Matthew Hansen T, Lasko LM, Bromberg KD, Manaves V, Algire M, Martin R, Qiu W, Torrent M, Jakob CG, Liu H, Cole PA, Marmorstein R, Kesicki EA, Lai A, Michaelides MR. Ji Z, et al. Among authors: michaelides mr. Bioorg Med Chem Lett. 2021 May 1;39:127854. doi: 10.1016/j.bmcl.2021.127854. Epub 2021 Feb 23. Bioorg Med Chem Lett. 2021. PMID: 33631370 Free PMC article.
Discovery of a Potent and Selective Covalent p300/CBP Inhibitor.
Mastracchio A, Lai C, Digiammarino E, Ready DB, Lasko LM, Bromberg KD, McClellan WJ, Montgomery D, Manaves V, Shaw B, Algire M, Patterson MJ, Sun CC, Rosenberg S, Lai A, Michaelides MR. Mastracchio A, et al. Among authors: michaelides mr. ACS Med Chem Lett. 2021 Apr 5;12(5):726-731. doi: 10.1021/acsmedchemlett.0c00654. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055218 Free PMC article.
Discovery of A-910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor.
Yu Y, Jang M, Miyashiro J, Clark RF, Zhu GD, Gong J, Dai Y, Frey RR, Penning TD, Kim H, Lee HK, Kim JK, Ryu KM, Park SJ, Yoon T, Li T, Kurnick MD, Kapecki NJ, Li L, Gorman JV, Montgomery DA, Manaves V, Bromberg KD, Doktor SZ, Thakur A, Wang J, Smith HA, Buchanan FG, Ferguson DC, Torrent M, Jakob CG, Qiu W, Upadhyay AK, Martin RL, Lai A, Michaelides MR. Yu Y, et al. Among authors: michaelides mr. J Med Chem. 2024 Oct 10;67(19):17000-17032. doi: 10.1021/acs.jmedchem.4c01450. Epub 2024 Sep 16. J Med Chem. 2024. PMID: 39283694
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Van Drie JH, McElligott D, Kesicki E, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD. Lasko LM, et al. Among authors: michaelides mr. Nature. 2017 Oct 5;550(7674):128-132. doi: 10.1038/nature24028. Epub 2017 Sep 27. Nature. 2017. PMID: 28953875 Free PMC article.
Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases.
Michaelides MR, Kluge A, Patane M, Van Drie JH, Wang C, Hansen TM, Risi RM, Mantei R, Hertel C, Karukurichi K, Nesterov A, McElligott D, de Vries P, Langston JW, Cole PA, Marmorstein R, Liu H, Lasko L, Bromberg KD, Lai A, Kesicki EA. Michaelides MR, et al. ACS Med Chem Lett. 2017 Dec 13;9(1):28-33. doi: 10.1021/acsmedchemlett.7b00395. eCollection 2018 Jan 11. ACS Med Chem Lett. 2017. PMID: 29348807 Free PMC article.
SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.
Curtin ML, Pliushchev MA, Li HQ, Torrent M, Dietrich JD, Jakob CG, Zhu H, Zhao H, Wang Y, Ji Z, Clark RF, Sarris KA, Selvaraju S, Shaw B, Algire MA, He Y, Richardson PL, Sweis RF, Sun C, Chiang GG, Michaelides MR. Curtin ML, et al. Among authors: michaelides mr. Bioorg Med Chem Lett. 2017 Apr 1;27(7):1576-1583. doi: 10.1016/j.bmcl.2017.02.030. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28254486
Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.
Dai Y, Hartandi K, Soni NB, Pease LJ, Reuter DR, Olson AM, Osterling DJ, Doktor SZ, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Stewart KD, Davidsen SK, Michaelides MR. Dai Y, et al. Among authors: michaelides mr. Bioorg Med Chem Lett. 2008 Jan 1;18(1):386-90. doi: 10.1016/j.bmcl.2007.10.018. Epub 2007 Oct 17. Bioorg Med Chem Lett. 2008. PMID: 18023347
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).
Curtin ML, Heyman HR, Clark RF, Sorensen BK, Doherty GA, Hansen TM, Frey RR, Sarris KA, Aguirre AL, Shrestha A, Tu N, Woller K, Pliushchev MA, Sweis RF, Cheng M, Wilsbacher JL, Kovar PJ, Guo J, Cheng D, Longenecker KL, Raich D, Korepanova AV, Soni NB, Algire MA, Richardson PL, Marin VL, Badagnani I, Vasudevan A, Buchanan FG, Maag D, Chiang GG, Tse C, Michaelides MR. Curtin ML, et al. Among authors: michaelides mr. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3317-3325. doi: 10.1016/j.bmcl.2017.06.018. Epub 2017 Jun 14. Bioorg Med Chem Lett. 2017. PMID: 28610984
58 results