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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Discovery of a new isomannide-based peptidomimetic synthetized by Ugi multicomponent reaction as human tissue kallikrein 1 inhibitor

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Barros, Thalita G. ; Santos, Jorge A. N. ; de Souza, Bruno E. G. ; Sodero, Ana Carolina R. ; de Souza, Alessandra M. T. ; da Silva, Dayane P. ; Rodrigues, Carlos Rangel ; Pinheiro, Sergio ; Dias, Luiza R. S. ; Abrahim-Vieira, Barbara ; Puzer, Luciano ; Muri, Estela M. F.
Total Authors: 12
Document type: Journal article
Source: Bioorganic & Medicinal Chemistry Letters; v. 27, n. 2, p. 314-318, JAN 15 2017.
Web of Science Citations: 4

Human kallikrein 1 (KLK1) is the most extensively studied member of this family and plays a major role in inflammation processes. From Ugi multicomponent reactions, isomannide-based peptidomimetic 10 and 13 where synthesized and showed low micromolar values of IC50 for KLK1 The most active compound (10) presented competitive mechanism, with three structural modifications important to interact with active site residues which corroborates its KLK1 inhibition. Finally, the most active compound also showed good ADMET profile, which indicates compound 10 as a potential hit in the search for new KLK1 inhibitors with low side effects. (C) 2016 Elsevier Ltd. All rights reserved. (AU)

FAPESP's process: 13/10548-3 - Development of mutant serpins for inhibition of human tissue kallikreins
Grantee:Luciano Puzer
Support Opportunities: Regular Research Grants