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745 results

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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. 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
Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Mathieu S, Gradl SN, Ren L, Wen Z, Aliagas I, Gunzner-Toste J, Lee W, Pulk R, Zhao G, Alicke B, Boggs JW, Buckmelter AJ, Choo EF, Dinkel V, Gloor SL, Gould SE, Hansen JD, Hastings G, Hatzivassiliou G, Laird ER, Moreno D, Ran Y, Voegtli WC, Wenglowsky S, Grina J, Rudolph J. Mathieu S, et al. Among authors: rudolph j. J Med Chem. 2012 Mar 22;55(6):2869-81. doi: 10.1021/jm300016v. Epub 2012 Feb 29. J Med Chem. 2012. PMID: 22335519
p21-Activated kinase inhibitors: a patent review.
Crawford JJ, Hoeflich KP, Rudolph J. Crawford JJ, et al. Among authors: rudolph j. 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.
Ras inhibition via direct Ras binding--is there a path forward?
Wang W, Fang G, Rudolph J. Wang W, et al. Among authors: rudolph j. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5766-76. doi: 10.1016/j.bmcl.2012.07.082. Epub 2012 Aug 2. Bioorg Med Chem Lett. 2012. PMID: 22902659 Free article.
P21-activated kinase 1 (PAK1) as a therapeutic target in BRAF wild-type melanoma.
Ong CC, Jubb AM, Jakubiak D, Zhou W, Rudolph J, Haverty PM, Kowanetz M, Yan Y, Tremayne J, Lisle R, Harris AL, Friedman LS, Belvin M, Middleton MR, Blackwood EM, Koeppen H, Hoeflich KP. Ong CC, et al. Among authors: rudolph j. J Natl Cancer Inst. 2013 May 1;105(9):606-7. doi: 10.1093/jnci/djt054. Epub 2013 Mar 27. J Natl Cancer Inst. 2013. PMID: 23535073
Imidazo[4,5-b]pyridine inhibitors of B-Raf kinase.
Newhouse BJ, Wenglowsky S, Grina J, Laird ER, Voegtli WC, Ren L, Ahrendt K, Buckmelter A, Gloor SL, Klopfenstein N, Rudolph J, Wen Z, Li X, Feng B. Newhouse BJ, et al. Among authors: rudolph j. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5896-9. doi: 10.1016/j.bmcl.2013.08.086. Epub 2013 Aug 29. Bioorg Med Chem Lett. 2013. PMID: 24042006
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: rudolph j. J Med Chem. 2014 Feb 13;57(3):1033-45. doi: 10.1021/jm401768t. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24432870
p21-activated kinase inhibitors.
Rudolph J, Crawford JJ, Hoeflich KP, Chernoff J. Rudolph J, et al. 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. J Med Chem. 2015 Jan 8;58(1):111-29. doi: 10.1021/jm501613q. Epub 2014 Dec 3. J Med Chem. 2015. PMID: 25415869
Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents.
Ong CC, Gierke S, Pitt C, Sagolla M, Cheng CK, Zhou W, Jubb AM, Strickland L, Schmidt M, Duron SG, Campbell DA, Zheng W, Dehdashti S, Shen M, Yang N, Behnke ML, Huang W, McKew JC, Chernoff J, Forrest WF, Haverty PM, Chin SF, Rakha EA, Green AR, Ellis IO, Caldas C, O'Brien T, Friedman LS, Koeppen H, Rudolph J, Hoeflich KP. Ong CC, et al. Among authors: rudolph j. Breast Cancer Res. 2015 Apr 23;17(1):59. doi: 10.1186/s13058-015-0564-5. Breast Cancer Res. 2015. PMID: 25902869 Free PMC article.
745 results