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743 results

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Conformation-locking antibodies for the discovery and characterization of KRAS inhibitors.
Davies CW, Oh AJ, Mroue R, Steffek M, Bruning JM, Xiao Y, Feng S, Jayakar S, Chan E, Arumugam V, Uribe SC, Drummond J, Frommlet A, Lu C, Franke Y, Merchant M, Koeppen H, Quinn JG, Malhotra S, Do S, Gazzard L, Purkey HE, Rudolph J, Mulvihill MM, Koerber JT, Wang W, Evangelista M. Davies CW, et al. Among authors: rudolph j. Nat Biotechnol. 2022 May;40(5):769-778. doi: 10.1038/s41587-021-01126-9. Epub 2022 Jan 6. Nat Biotechnol. 2022. PMID: 34992247
Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity.
Maurer T, Garrenton LS, Oh A, Pitts K, Anderson DJ, Skelton NJ, Fauber BP, Pan B, Malek S, Stokoe D, Ludlam MJ, Bowman KK, Wu J, Giannetti AM, Starovasnik MA, Mellman I, Jackson PK, Rudolph J, Wang W, Fang G. Maurer T, et al. Among authors: rudolph j. Proc Natl Acad Sci U S A. 2012 Apr 3;109(14):5299-304. doi: 10.1073/pnas.1116510109. Epub 2012 Mar 19. Proc Natl Acad Sci U S A. 2012. PMID: 22431598 Free PMC article.
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
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
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
Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors.
Yen I, Shanahan F, Merchant M, Orr C, Hunsaker T, Durk M, La H, Zhang X, Martin SE, Lin E, Chan J, Yu Y, Amin D, Neve RM, Gustafson A, Venkatanarayan A, Foster SA, Rudolph J, Klijn C, Malek S. Yen I, et al. Among authors: rudolph j. Cancer Cell. 2018 Oct 8;34(4):611-625.e7. doi: 10.1016/j.ccell.2018.09.002. Cancer Cell. 2018. PMID: 30300582 Free article.
IRE1α Disruption in Triple-Negative Breast Cancer Cooperates with Antiangiogenic Therapy by Reversing ER Stress Adaptation and Remodeling the Tumor Microenvironment.
Harnoss JM, Le Thomas A, Reichelt M, Guttman O, Wu TD, Marsters SA, Shemorry A, Lawrence DA, Kan D, Segal E, Merchant M, Totpal K, Crocker LM, Mesh K, Dohse M, Solon M, Modrusan Z, Rudolph J, Koeppen H, Walter P, Ashkenazi A. Harnoss JM, et al. Among authors: rudolph j. Cancer Res. 2020 Jun 1;80(11):2368-2379. doi: 10.1158/0008-5472.CAN-19-3108. Epub 2020 Apr 7. Cancer Res. 2020. PMID: 32265225 Free PMC article.
743 results