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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
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
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.
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
Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.
Beveridge RE, Wallweber HA, Ashkenazi A, Beresini M, Clark KR, Gibbons P, Ghiro E, Kaufman S, Larivée A, Leblanc M, Leclerc JP, Lemire A, Ly C, Rudolph J, Schwarz JB, Srivastava S, Wang W, Zhao L, Braun MG. Beveridge RE, et al. Among authors: rudolph j. ACS Med Chem Lett. 2020 Oct 16;11(12):2389-2396. doi: 10.1021/acsmedchemlett.0c00344. eCollection 2020 Dec 10. ACS Med Chem Lett. 2020. PMID: 33335661 Free PMC article.
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
Huestis MP, Dela Cruz D, DiPasquale AG, Durk MR, Eigenbrot C, Gibbons P, Gobbi A, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Siu M, Rudolph J. Huestis MP, et al. Among authors: rudolph j. J Med Chem. 2021 Apr 8;64(7):3940-3955. doi: 10.1021/acs.jmedchem.0c02085. Epub 2021 Mar 29. J Med Chem. 2021. PMID: 33780623
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
Huestis MP, Durk MR, Eigenbrot C, Gibbons P, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Rudolph J, Siu M. Huestis MP, et al. Among authors: rudolph j. ACS Med Chem Lett. 2021 Apr 21;12(5):791-797. doi: 10.1021/acsmedchemlett.1c00063. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055227 Free PMC article.
746 results