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Page 1
Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing.
Pissot Soldermann C, Simic O, Renatus M, Erbel P, Melkko S, Wartmann M, Bigaud M, Weiss A, McSheehy P, Endres R, Santos P, Blank J, Schuffenhauer A, Bold G, Buschmann N, Zoller T, Altmann E, Manley PW, Dix I, Buchdunger E, Scesa J, Quancard J, Schlapbach A, Bornancin F, Radimerski T, Régnier CH. Pissot Soldermann C, et al. Among authors: weiss a. J Med Chem. 2020 Dec 10;63(23):14576-14593. doi: 10.1021/acs.jmedchem.0c01245. Epub 2020 Nov 30. J Med Chem. 2020. PMID: 33252239
Targeted inhibition of the COP9 signalosome for treatment of cancer.
Schlierf A, Altmann E, Quancard J, Jefferson AB, Assenberg R, Renatus M, Jones M, Hassiepen U, Schaefer M, Kiffe M, Weiss A, Wiesmann C, Sedrani R, Eder J, Martoglio B. Schlierf A, et al. Among authors: weiss a. Nat Commun. 2016 Oct 24;7:13166. doi: 10.1038/ncomms13166. Nat Commun. 2016. PMID: 27774986 Free PMC article.
FGF401, A First-In-Class Highly Selective and Potent FGFR4 Inhibitor for the Treatment of FGF19-Driven Hepatocellular Cancer.
Weiss A, Adler F, Buhles A, Stamm C, Fairhurst RA, Kiffe M, Sterker D, Centeleghe M, Wartmann M, Kinyamu-Akunda J, Schadt HS, Couttet P, Wolf A, Wang Y, Barzaghi-Rinaudo P, Murakami M, Kauffmann A, Knoepfel T, Buschmann N, Leblanc C, Mah R, Furet P, Blank J, Hofmann F, Sellers WR, Graus Porta D. Weiss A, et al. Mol Cancer Ther. 2019 Dec;18(12):2194-2206. doi: 10.1158/1535-7163.MCT-18-1291. Epub 2019 Aug 13. Mol Cancer Ther. 2019. PMID: 31409633
New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse.
Stauffer F, Weiss A, Scheufler C, Möbitz H, Ragot C, Beyer KS, Calkins K, Guthy D, Kiffe M, Van Eerdenbrugh B, Tiedt R, Gaul C. Stauffer F, et al. Among authors: weiss a. ACS Med Chem Lett. 2019 Dec 4;10(12):1655-1660. doi: 10.1021/acsmedchemlett.9b00452. eCollection 2019 Dec 12. ACS Med Chem Lett. 2019. PMID: 31857842 Free PMC article.
Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4.
Fairhurst RA, Knoepfel T, Buschmann N, Leblanc C, Mah R, Todorov M, Nimsgern P, Ripoche S, Niklaus M, Warin N, Luu VH, Madoerin M, Wirth J, Graus-Porta D, Weiss A, Kiffe M, Wartmann M, Kinyamu-Akunda J, Sterker D, Stamm C, Adler F, Buhles A, Schadt H, Couttet P, Blank J, Galuba I, Trappe J, Voshol J, Ostermann N, Zou C, Berghausen J, Del Rio Espinola A, Jahnke W, Furet P. Fairhurst RA, et al. Among authors: weiss a. J Med Chem. 2020 Nov 12;63(21):12542-12573. doi: 10.1021/acs.jmedchem.0c01019. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32930584
Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood.
Quancard J, Simic O, Pissot Soldermann C, Aichholz R, Blatter M, Renatus M, Erbel P, Melkko S, Endres R, Sorge M, Kieffer L, Wagner T, Beltz K, Mcsheehy P, Wartmann M, Régnier CH, Calzascia T, Radimerski T, Bigaud M, Weiss A, Bornancin F, Schlapbach A. Quancard J, et al. Among authors: weiss a. J Med Chem. 2020 Dec 10;63(23):14594-14608. doi: 10.1021/acs.jmedchem.0c01246. Epub 2020 Nov 20. J Med Chem. 2020. PMID: 33216547
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Huang Y, Sendzik M, Zhang J, Gao Z, Sun Y, Wang L, Gu J, Zhao K, Yu Z, Zhang L, Zhang Q, Blanz J, Chen Z, Dubost V, Fang D, Feng L, Fu X, Kiffe M, Li L, Luo F, Luo X, Mi Y, Mistry P, Pearson D, Piaia A, Scheufler C, Terranova R, Weiss A, Zeng J, Zhang H, Zhang J, Zhao M, Dillon MP, Jeay S, Qi W, Moggs J, Pissot-Soldermann C, Li E, Atadja P, Lingel A, Oyang C. Huang Y, et al. Among authors: weiss a. J Med Chem. 2022 Apr 14;65(7):5317-5333. doi: 10.1021/acs.jmedchem.1c02148. Epub 2022 Mar 30. J Med Chem. 2022. PMID: 35352560
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. Lorthiois E, et al. Among authors: weiss a. J Med Chem. 2022 Dec 22;65(24):16173-16203. doi: 10.1021/acs.jmedchem.2c01438. Epub 2022 Nov 18. J Med Chem. 2022. PMID: 36399068
Transient Inhibition of the JAK/STAT Pathway Prevents B-ALL Development in Genetically Predisposed Mice.
Casado-García A, Isidro-Hernández M, Oak N, Mayado A, Mann-Ran C, Raboso-Gallego J, Alemán-Arteaga S, Buhles A, Sterker D, Sánchez EG, Martínez-Cano J, Blanco O, Orfao A, Alonso-López D, De Las Rivas J, Riesco S, Prieto-Matos P, González-Murillo Á, García Criado FJ, García Cenador MB, Radimerski T, Ramírez-Orellana M, Cobaleda C, Yang JJ, Vicente-Dueñas C, Weiss A, Nichols KE, Sánchez-García I. Casado-García A, et al. Among authors: weiss a. Cancer Res. 2022 Mar 15;82(6):1098-1109. doi: 10.1158/0008-5472.CAN-21-3386. Cancer Res. 2022. PMID: 35131871 Free PMC article.
3,735 results