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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: grant sw. 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: grant sw. J Med Chem. 2011 Mar 24;54(6):1871-95. doi: 10.1021/jm101527u. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341675
Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity.
Axten JM, Medina JR, Blackledge CW, Duquenne C, Grant SW, Bobko MA, Peng T, Miller WH, Pinckney T, Gallagher TF, Kulkarni S, Lewandowski T, Van Aller GS, Zonis R, Ward P, Campobasso N. Axten JM, et al. Among authors: grant sw. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4028-32. doi: 10.1016/j.bmcl.2012.04.086. Epub 2012 Apr 25. Bioorg Med Chem Lett. 2012. PMID: 22579486
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: grant sw. 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.
Discovery of a new series of Aurora inhibitors through truncation of GSK1070916.
Medina JR, Grant SW, Axten JM, Miller WH, Donatelli CA, Hardwicke MA, Oleykowski CA, Liao Q, Plant R, Xiang H. Medina JR, et al. Among authors: grant sw. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2552-5. doi: 10.1016/j.bmcl.2010.02.091. Epub 2010 Mar 1. Bioorg Med Chem Lett. 2010. PMID: 20335034
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: grant sw. 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.
Association between kidney function, frailty and receipt of invasive management after acute coronary syndrome.
Scott JK, Johnson T, Caskey FJ, Bailey P, Selman LE, Mulla A, Glampson B, Davies J, Papdimitriou D, Woods K, O'Gallagher K, Williams B, Asselbergs FW, Mayer EK, Lee R, Herbert C, Grant SW, Curzen N, Squire I, Kharbanda R, Shah A, Perera D, Patel RS, Channon K, Mayet J, Kaura A, Ben-Shlomo Y. Scott JK, et al. Among authors: grant sw. Open Heart. 2024 Oct 9;11(2):e002875. doi: 10.1136/openhrt-2024-002875. Open Heart. 2024. PMID: 39384342 Free PMC article.
Composite end points and competing risks analysis.
Dayan V, Grant SW, Brophy JM, Barili F, Freemantle N. Dayan V, et al. Among authors: grant sw. Interdiscip Cardiovasc Thorac Surg. 2024 Jul 3;39(1):ivae126. doi: 10.1093/icvts/ivae126. Interdiscip Cardiovasc Thorac Surg. 2024. PMID: 38954830 Free PMC article.
97 results