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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: chene p. 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.
2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Gerspacher M, Furet P, Pissot-Soldermann C, Gaul C, Holzer P, Vangrevelinghe E, Lang M, Erdmann D, Radimerski T, Regnier CH, Chene P, De Pover A, Hofmann F, Baffert F, Buhl T, Aichholz R, Blasco F, Endres R, Trappe J, Drueckes P. Gerspacher M, et al. Among authors: chene p. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138510
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F. Holzer P, et al. Among authors: chene p. J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810. Epub 2015 Aug 5. J Med Chem. 2015. PMID: 26181851
Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.
Furet P, Masuya K, Kallen J, Stachyra-Valat T, Ruetz S, Guagnano V, Holzer P, Mah R, Stutz S, Vaupel A, Chène P, Jeay S, Schlapbach A. Furet P, et al. Among authors: chene p. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-4841. doi: 10.1016/j.bmcl.2016.08.010. Epub 2016 Aug 9. Bioorg Med Chem Lett. 2016. PMID: 27542305
197 results