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Page 1
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction.
Gilmartin AG, Faitg TH, Richter M, Groy A, Seefeld MA, Darcy MG, Peng X, Federowicz K, Yang J, Zhang SY, Minthorn E, Jaworski JP, Schaber M, Martens S, McNulty DE, Sinnamon RH, Zhang H, Kirkpatrick RB, Nevins N, Cui G, Pietrak B, Diaz E, Jones A, Brandt M, Schwartz B, Heerding DA, Kumar R. Gilmartin AG, et al. Nat Chem Biol. 2014 Mar;10(3):181-7. doi: 10.1038/nchembio.1427. Epub 2014 Jan 5. Nat Chem Biol. 2014. PMID: 24390428
Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity.
Concha NO, Smallwood A, Bonnette W, Totoritis R, Zhang G, Federowicz K, Yang J, Qi H, Chen S, Campobasso N, Choudhry AE, Shuster LE, Evans KA, Ralph J, Sweitzer S, Heerding DA, Buser CA, Su DS, DeYoung MP. Concha NO, et al. Among authors: heerding da. Mol Pharmacol. 2015 Dec;88(6):1011-23. doi: 10.1124/mol.115.100917. Epub 2015 Oct 5. Mol Pharmacol. 2015. PMID: 26438213
Aminofurazans as potent inhibitors of AKT kinase.
Rouse MB, Seefeld MA, Leber JD, McNulty KC, Sun L, Miller WH, Zhang S, Minthorn EA, Concha NO, Choudhry AE, Schaber MD, Heerding DA. Rouse MB, et al. Among authors: heerding da. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1508-11. doi: 10.1016/j.bmcl.2009.01.002. Epub 2009 Jan 9. Bioorg Med Chem Lett. 2009. PMID: 19179070
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: heerding da. J Med Chem. 2012 Aug 23;55(16):7193-207. doi: 10.1021/jm300713s. Epub 2012 Aug 8. J Med Chem. 2012. PMID: 22827572
Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI).
Miller WH, Seefeld MA, Newlander KA, Uzinskas IN, Burgess WJ, Heerding DA, Yuan CC, Head MS, Payne DJ, Rittenhouse SF, Moore TD, Pearson SC, Berry V, DeWolf WE Jr, Keller PM, Polizzi BJ, Qiu X, Janson CA, Huffman WF. Miller WH, et al. Among authors: heerding da. J Med Chem. 2002 Jul 18;45(15):3246-56. doi: 10.1021/jm020050+. J Med Chem. 2002. PMID: 12109908
2,3,5-Trisubstituted pyridines as selective AKT inhibitors-Part I: Substitution at 2-position of the core pyridine for ROCK1 selectivity.
Lin H, Yamashita DS, Zeng J, Xie R, Wang W, Nidarmarthy S, Luengo JI, Rhodes N, Knick VB, Choudhry AE, Lai Z, Minthorn EA, Strum SL, Wood ER, Elkins PA, Concha NO, Heerding DA. Lin H, et al. Bioorg Med Chem Lett. 2010 Jan 15;20(2):673-8. doi: 10.1016/j.bmcl.2009.11.064. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 20006497
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: heerding d. J Med Chem. 2011 Mar 24;54(6):1871-95. doi: 10.1021/jm101527u. Epub 2011 Feb 22. J Med Chem. 2011. PMID: 21341675
31 results