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Page 1
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.
Rudolph J, Aliagas I, Crawford JJ, Mathieu S, Lee W, Chao Q, Dong P, Rouge L, Wang W, Heise C, Murray LJ, La H, Liu Y, Manning G, Diederich F, Hoeflich KP. Rudolph J, et al. Among authors: heise c. ACS Med Chem Lett. 2015 May 20;6(6):711-5. doi: 10.1021/acsmedchemlett.5b00151. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101579 Free PMC article.
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H, DiPasquale AG, Friedman LS, Heise C, Koeppen H, Kotey A, Mintzer R, Oh A, Roberts DA, Rouge L, Rudolph J, Tam C, Wang W, Xiao Y, Young A, Zhang Y, Hoeflich KP. Staben ST, et al. Among authors: heise c. J Med Chem. 2014 Feb 13;57(3):1033-45. doi: 10.1021/jm401768t. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24432870
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.
Ndubaku CO, Crawford JJ, Drobnick J, Aliagas I, Campbell D, Dong P, Dornan LM, Duron S, Epler J, Gazzard L, Heise CE, Hoeflich KP, Jakubiak D, La H, Lee W, Lin B, Lyssikatos JP, Maksimoska J, Marmorstein R, Murray LJ, O'Brien T, Oh A, Ramaswamy S, Wang W, Zhao X, Zhong Y, Blackwood E, Rudolph J. Ndubaku CO, et al. ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6. doi: 10.1021/acsmedchemlett.5b00398. eCollection 2015 Dec 10. ACS Med Chem Lett. 2015. PMID: 26713112 Free PMC article.
Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window.
Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood E, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, Zhang H, Heise CE, Oh A, Ong CC, La H, Chakravarty P, Chan C, Jakubiak D, Epler J, Ramaswamy S, Vega R, Cain G, Diaz D, Zhong Y. Rudolph J, et al. Among authors: heise ce. J Med Chem. 2016 Jun 9;59(11):5520-41. doi: 10.1021/acs.jmedchem.6b00638. Epub 2016 May 24. J Med Chem. 2016. PMID: 27167326
Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.
Crawford JJ, Lee W, Aliagas I, Mathieu S, Hoeflich KP, Zhou W, Wang W, Rouge L, Murray L, La H, Liu N, Fan PW, Cheong J, Heise CE, Ramaswamy S, Mintzer R, Liu Y, Chao Q, Rudolph J. Crawford JJ, et al. J Med Chem. 2015 Jun 25;58(12):5121-36. doi: 10.1021/acs.jmedchem.5b00572. Epub 2015 Jun 12. J Med Chem. 2015. PMID: 26030457
A therapeutic antibody targeting BACE1 inhibits amyloid-β production in vivo.
Atwal JK, Chen Y, Chiu C, Mortensen DL, Meilandt WJ, Liu Y, Heise CE, Hoyte K, Luk W, Lu Y, Peng K, Wu P, Rouge L, Zhang Y, Lazarus RA, Scearce-Levie K, Wang W, Wu Y, Tessier-Lavigne M, Watts RJ. Atwal JK, et al. Among authors: heise ce. Sci Transl Med. 2011 May 25;3(84):84ra43. doi: 10.1126/scitranslmed.3002254. Sci Transl Med. 2011. PMID: 21613622
Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.
Burdick DJ, Wang S, Heise C, Pan B, Drummond J, Yin J, Goeser L, Magnuson S, Blaney J, Moffat J, Wang W, Chen H. Burdick DJ, et al. Among authors: heise c. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4728-4732. doi: 10.1016/j.bmcl.2015.08.048. Epub 2015 Aug 22. Bioorg Med Chem Lett. 2015. PMID: 26338362
Optimized arylomycins are a new class of Gram-negative antibiotics.
Smith PA, Koehler MFT, Girgis HS, Yan D, Chen Y, Chen Y, Crawford JJ, Durk MR, Higuchi RI, Kang J, Murray J, Paraselli P, Park S, Phung W, Quinn JG, Roberts TC, Rougé L, Schwarz JB, Skippington E, Wai J, Xu M, Yu Z, Zhang H, Tan MW, Heise CE. Smith PA, et al. Among authors: heise ce. Nature. 2018 Sep;561(7722):189-194. doi: 10.1038/s41586-018-0483-6. Epub 2018 Sep 12. Nature. 2018. PMID: 30209367
Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6.
Heise CE, Murray J, Augustyn KE, Bravo B, Chugha P, Cohen F, Giannetti AM, Gibbons P, Hannoush RN, Hearn BR, Jaishankar P, Ly CQ, Shah K, Stanger K, Steffek M, Tang Y, Zhao X, Lewcock JW, Renslo AR, Flygare J, Arkin MR. Heise CE, et al. PLoS One. 2012;7(12):e50864. doi: 10.1371/journal.pone.0050864. Epub 2012 Dec 5. PLoS One. 2012. PMID: 23227217 Free PMC article.
328 results