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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: doktor sz. 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 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: doktor sz. 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
AhR activation underlies the CYP1A autoinduction by A-998679 in rats.
Liguori MJ, Lee CH, Liu H, Ciurlionis R, Ditewig AC, Doktor S, Andracki ME, Gagne GD, Waring JF, Marsh KC, Gopalakrishnan M, Blomme EA, Yang Y. Liguori MJ, et al. Among authors: doktor s. Front Genet. 2012 Oct 26;3:213. doi: 10.3389/fgene.2012.00213. eCollection 2012. Front Genet. 2012. PMID: 23112805 Free PMC article.
Liver-specific knockdown of JNK1 up-regulates proliferator-activated receptor gamma coactivator 1 beta and increases plasma triglyceride despite reduced glucose and insulin levels in diet-induced obese mice.
Yang R, Wilcox DM, Haasch DL, Jung PM, Nguyen PT, Voorbach MJ, Doktor S, Brodjian S, Bush EN, Lin E, Jacobson PB, Collins CA, Landschulz KT, Trevillyan JM, Rondinone CM, Surowy TK. Yang R, et al. Among authors: doktor s. J Biol Chem. 2007 Aug 3;282(31):22765-74. doi: 10.1074/jbc.M700790200. Epub 2007 Jun 5. J Biol Chem. 2007. PMID: 17550900 Free article.
22 results