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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: mallet w. 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.
Nicotinamide Phosphoribosyltransferase Inhibitor as a Novel Payload for Antibody-Drug Conjugates.
Karpov AS, Abrams T, Clark S, Raikar A, D'Alessio JA, Dillon MP, Gesner TG, Jones D, Lacaud M, Mallet W, Martyniuk P, Meredith E, Mohseni M, Nieto-Oberhuber CM, Palacios D, Perruccio F, Piizzi G, Zurini M, Bialucha CU. Karpov AS, et al. Among authors: mallet w. ACS Med Chem Lett. 2018 Jun 28;9(8):838-842. doi: 10.1021/acsmedchemlett.8b00254. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128077 Free PMC article.
Efficient Preparation of Site-Specific Antibody-Drug Conjugates Using Phosphopantetheinyl Transferases.
Grünewald J, Klock HE, Cellitti SE, Bursulaya B, McMullan D, Jones DH, Chiu HP, Wang X, Patterson P, Zhou H, Vance J, Nigoghossian E, Tong H, Daniel D, Mallet W, Ou W, Uno T, Brock A, Lesley SA, Geierstanger BH. Grünewald J, et al. Among authors: mallet w. Bioconjug Chem. 2015 Dec 16;26(12):2554-62. doi: 10.1021/acs.bioconjchem.5b00558. Epub 2015 Dec 4. Bioconjug Chem. 2015. PMID: 26588668
Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index.
Junutula JR, Raab H, Clark S, Bhakta S, Leipold DD, Weir S, Chen Y, Simpson M, Tsai SP, Dennis MS, Lu Y, Meng YG, Ng C, Yang J, Lee CC, Duenas E, Gorrell J, Katta V, Kim A, McDorman K, Flagella K, Venook R, Ross S, Spencer SD, Lee Wong W, Lowman HB, Vandlen R, Sliwkowski MX, Scheller RH, Polakis P, Mallet W. Junutula JR, et al. Among authors: mallet w. Nat Biotechnol. 2008 Aug;26(8):925-32. doi: 10.1038/nbt.1480. Epub 2008 Jul 20. Nat Biotechnol. 2008. PMID: 18641636
Nonclinical evaluation of the serum pharmacodynamic biomarkers HGF and shed MET following dosing with the anti-MET monovalent monoclonal antibody onartuzumab.
Mai E, Zheng Z, Chen Y, Peng J, Severin C, Filvaroff E, Romero M, Mallet W, Kaur S, Gelzleichter T, Nijem I, Merchant M, Young JC. Mai E, et al. Among authors: mallet w. Mol Cancer Ther. 2014 Feb;13(2):540-52. doi: 10.1158/1535-7163.MCT-13-0494. Epub 2013 Nov 20. Mol Cancer Ther. 2014. PMID: 24258345
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