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Page 1
Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).
Axten JM, Medina JR, Feng Y, Shu A, Romeril SP, Grant SW, Li WH, Heerding DA, Minthorn E, Mencken T, Atkins C, Liu Q, Rabindran S, Kumar R, Hong X, Goetz A, Stanley T, Taylor JD, Sigethy SD, Tomberlin GH, Hassell AM, Kahler KM, Shewchuk LM, Gampe RT. Axten JM, et al. Among authors: shu a. J Med Chem. 2012 Aug 23;55(16):7193-207. doi: 10.1021/jm300713s. Epub 2012 Aug 8. J Med Chem. 2012. PMID: 22827572
Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.
Medina JR, Becker CJ, Blackledge CW, Duquenne C, Feng Y, Grant SW, Heerding D, Li WH, Miller WH, Romeril SP, Scherzer D, Shu A, Bobko MA, Chadderton AR, Dumble M, Gardiner CM, Gilbert S, Liu Q, Rabindran SK, Sudakin V, Xiang H, Brady PG, Campobasso N, Ward P, Axten JM. Medina JR, et al. Among authors: shu a. J Med Chem. 2011 Mar 24;54(6):1871-95. doi: 10.1021/jm101527u. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341675
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
Axten JM, Romeril SP, Shu A, Ralph J, Medina JR, Feng Y, Li WH, Grant SW, Heerding DA, Minthorn E, Mencken T, Gaul N, Goetz A, Stanley T, Hassell AM, Gampe RT, Atkins C, Kumar R. Axten JM, et al. Among authors: shu a. ACS Med Chem Lett. 2013 Aug 12;4(10):964-8. doi: 10.1021/ml400228e. eCollection 2013 Oct 10. ACS Med Chem Lett. 2013. PMID: 24900593 Free PMC article.
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH. Verma SK, et al. Among authors: shu a. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13. ACS Med Chem Lett. 2012. PMID: 24900432 Free PMC article.
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors.
Haffner CD, Charnley AK, Aquino CJ, Casillas L, Convery MA, Cox JA, Elban MA, Goodwin NC, Gough PJ, Haile PA, Hughes TV, Knapp-Reed B, Kreatsoulas C, Lakdawala AS, Li H, Lian Y, Lipshutz D, Mehlmann JF, Ouellette M, Romano J, Shewchuk L, Shu A, Votta BJ, Zhou H, Bertin J, Marquis RW. Haffner CD, et al. Among authors: shu a. ACS Med Chem Lett. 2019 Oct 11;10(11):1518-1523. doi: 10.1021/acsmedchemlett.9b00141. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749904 Free PMC article.
Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).
Brnardic EJ, Ye G, Brooks C, Donatelli C, Barton L, McAtee J, Sanchez RM, Shu A, Erhard K, Terrell L, Graczyk-Millbrandt G, He Y, Costell MH, Behm DJ, Roethke T, Stoy P, Holt DA, Lawhorn BG. Brnardic EJ, et al. Among authors: shu a. J Med Chem. 2018 Nov 8;61(21):9738-9755. doi: 10.1021/acs.jmedchem.8b01317. Epub 2018 Oct 18. J Med Chem. 2018. PMID: 30335378
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.
Samanen JM, Ali FE, Barton LS, Bondinell WE, Burgess JL, Callahan JF, Calvo RR, Chen W, Chen L, Erhard K, Feuerstein G, Heys R, Hwang SM, Jakas DR, Keenan RM, Ku TW, Kwon C, Lee CP, Miller WH, Newlander KA, Nichols A, Parker M, Peishoff CE, Rhodes G, Ross S, Shu A, Simpson R, Takata D, Yellin TO, Uzsinskas I, Venslavsky JW, Yuan CK, Huffman WF. Samanen JM, et al. Among authors: shu a. J Med Chem. 1996 Dec 6;39(25):4867-70. doi: 10.1021/jm960558a. J Med Chem. 1996. PMID: 8960544 No abstract available.
Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.
Pero JE, Matthews JM, Behm DJ, Brnardic EJ, Brooks C, Budzik BW, Costell MH, Donatelli CA, Eisennagel SH, Erhard K, Fischer MC, Holt DA, Jolivette LJ, Li H, Li P, McAtee JJ, McCleland BW, Pendrak I, Posobiec LM, Rivera KLK, Rivero RA, Roethke TJ, Sender MR, Shu A, Terrell LR, Vaidya K, Xu X, Lawhorn BG. Pero JE, et al. Among authors: shu a. J Med Chem. 2018 Dec 27;61(24):11209-11220. doi: 10.1021/acs.jmedchem.8b01344. Epub 2018 Dec 12. J Med Chem. 2018. PMID: 30500190
132 results