Identification of novel TACE inhibitors compatible with topical application

Autor:	Arnaud Reitz, Corinne Millois, Marilyne Bourotte, Feriel Hacini-Rachinel, Carine Rosignoli, Arnaud Mathieu, Sandrine Chambon, Denis Duvert, Anne-Pascale Luzy, Laetitia Bonnary, Gwenaëlle Duvert, Gilles Ouvry, Jonathan Pascau, Craig S. Harris, Benoit Deprez, Laurent F. Hennequin, Catherine Comino, Yushma Bhurruth-Alcor, Yaël Berton, Nathalie Taquet, Claire Bouix-Peter, Gaëlle Polge, Kevin Reverse, Artur Pinto, Karine Bouquet
Rok vydání:	2017
Předmět:	0301 basic medicine Cellular activity Side effect Administration Topical Clinical Biochemistry Pharmaceutical Science Context (language use) ADAM17 Protein Pharmacology Hydroxamic Acids 01 natural sciences Biochemistry 03 medical and health sciences Psoriasis Drug Discovery medicine Humans Enzyme Inhibitors Molecular Biology Tumor necrosis factor α ADME chemistry.chemical_classification 010405 organic chemistry Organic Chemistry medicine.disease 0104 chemical sciences 030104 developmental biology Enzyme chemistry Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 27:1848-1853
ISSN:	0960-894X
Popis:	Targeting the Tumor Necrosis Factor α signalling with antibodies has led to a revolution in the treatment of psoriasis. Locally inhibiting Tumor Necrosis Factor α Converting Enzyme (TACE or ADAM17) could potentially mimic those effects and help treat mild to moderate psoriasis, without the reported side effect of systemic TACE inhibitors. Efforts to identify new TACE inhibitors are presented here. Enzymatic SAR as well as ADME and physico-chemistry data are presented. This study culminated in the identification of potent enzymatic inhibitors. Suboptimal cellular activity of this series is discussed in the context of previously published results.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fb6d576b781466f2d73bb18129c36d97 https://doi.org/10.1016/j.bmcl.2017.02.035 Zobrazit plný text záznamu Full Text from ScienceDirect