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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: crawford jj. 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
p21-Activated kinase inhibitors: a patent review.
Crawford JJ, Hoeflich KP, Rudolph J. Crawford JJ, et al. Expert Opin Ther Pat. 2012 Mar;22(3):293-310. doi: 10.1517/13543776.2012.668758. Epub 2012 Mar 11. Expert Opin Ther Pat. 2012. PMID: 22404134 Review.
Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors.
Crawford JJ, Kenny PW, Bowyer J, Cook CR, Finlayson JE, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Martin S, Macfaul PA, McDermott BP, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Dossetter AG. Crawford JJ, et al. J Med Chem. 2012 Oct 25;55(20):8827-37. doi: 10.1021/jm301119s. Epub 2012 Oct 11. J Med Chem. 2012. PMID: 22984809
p21-activated kinase inhibitors.
Rudolph J, Crawford JJ, Hoeflich KP, Chernoff J. Rudolph J, et al. Among authors: crawford jj. Enzymes. 2013;34 Pt. B:157-80. doi: 10.1016/B978-0-12-420146-0.00007-X. Epub 2013 Nov 7. Enzymes. 2013. PMID: 25034104 Review.
Inhibitors of p21-activated kinases (PAKs).
Rudolph J, Crawford JJ, Hoeflich KP, Wang W. Rudolph J, et al. Among authors: crawford jj. J Med Chem. 2015 Jan 8;58(1):111-29. doi: 10.1021/jm501613q. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25415869
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
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: crawford jj. 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.
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. Among authors: crawford jj. 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.
Rate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat.
Fan PW, Chen JZ, Allan Jaochico M, La H, Liu N, Mulder T, Cass RT, Durk M, Messick K, Valle N, Liu S, Lee W, Crawford JJ, Rudolf J, Murray LJ, Cyrus Khojasteh S, Wright M. Fan PW, et al. Among authors: crawford jj. Drug Metab Lett. 2016;10(2):91-100. doi: 10.2174/1872312810666160411144358. Drug Metab Lett. 2016. PMID: 27063863 Free PMC article.
129 results