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Page 1
Discovery of Potent and Selective Antibody-Drug Conjugates with Eg5 Inhibitors through Linker and Payload Optimization.
Karpov AS, Nieto-Oberhuber CM, Abrams T, Beng-Louka E, Blanco E, Chamoin S, Chene P, Dacquignies I, Daniel D, Dillon MP, Doumampouom-Metoul L, Drosos N, Fedoseev P, Furegati M, Granda B, Grotzfeld RM, Hess Clark S, Joly E, Jones D, Lacaud-Baumlin M, Lagasse-Guerro S, Lorenzana EG, Mallet W, Martyniuk P, Marzinzik AL, Mesrouze Y, Nocito S, Oei Y, Perruccio F, Piizzi G, Richard E, Rudewicz PJ, Schindler P, Velay M, Venstrom K, Wang P, Zurini M, Lafrance M. Karpov AS, et al. Among authors: grotzfeld rm. ACS Med Chem Lett. 2019 Dec 3;10(12):1674-1679. doi: 10.1021/acsmedchemlett.9b00468. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857845 Free PMC article.
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P. Schoepfer J, et al. Among authors: grotzfeld rm. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. J Med Chem. 2018. PMID: 30137981
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J. Fabbro D, et al. Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009. Biochim Biophys Acta. 2010. PMID: 20152788
Arylcarboxyamino-substituted diaryl ureas as potent and selective FLT3 inhibitors.
Patel HK, Grotzfeld RM, Lai AG, Mehta SA, Milanov ZV, Chao Q, Sprankle KG, Carter TA, Velasco AM, Fabian MA, James J, Treiber DK, Lockhart DJ, Zarrinkar PP, Bhagwat SS. Patel HK, et al. Among authors: grotzfeld rm. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5182-5. doi: 10.1016/j.bmcl.2009.07.024. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19646870
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Chao Q, Sprankle KG, Grotzfeld RM, Lai AG, Carter TA, Velasco AM, Gunawardane RN, Cramer MD, Gardner MF, James J, Zarrinkar PP, Patel HK, Bhagwat SS. Chao Q, et al. Among authors: grotzfeld rm. J Med Chem. 2009 Dec 10;52(23):7808-16. doi: 10.1021/jm9007533. J Med Chem. 2009. PMID: 19754199
A small molecule-kinase interaction map for clinical kinase inhibitors.
Fabian MA, Biggs WH 3rd, Treiber DK, Atteridge CE, Azimioara MD, Benedetti MG, Carter TA, Ciceri P, Edeen PT, Floyd M, Ford JM, Galvin M, Gerlach JL, Grotzfeld RM, Herrgard S, Insko DE, Insko MA, Lai AG, Lélias JM, Mehta SA, Milanov ZV, Velasco AM, Wodicka LM, Patel HK, Zarrinkar PP, Lockhart DJ. Fabian MA, et al. Among authors: grotzfeld rm. Nat Biotechnol. 2005 Mar;23(3):329-36. doi: 10.1038/nbt1068. Epub 2005 Feb 13. Nat Biotechnol. 2005. PMID: 15711537 Free article.
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.
Carter TA, Wodicka LM, Shah NP, Velasco AM, Fabian MA, Treiber DK, Milanov ZV, Atteridge CE, Biggs WH 3rd, Edeen PT, Floyd M, Ford JM, Grotzfeld RM, Herrgard S, Insko DE, Mehta SA, Patel HK, Pao W, Sawyers CL, Varmus H, Zarrinkar PP, Lockhart DJ. Carter TA, et al. Among authors: grotzfeld rm. Proc Natl Acad Sci U S A. 2005 Aug 2;102(31):11011-6. doi: 10.1073/pnas.0504952102. Epub 2005 Jul 26. Proc Natl Acad Sci U S A. 2005. PMID: 16046538 Free PMC article.
11 results