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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.)

Protein-protein interaction inhibitors: advances in anticancer drug design

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Ferreira, Leonardo G. ; Oliva, Glaucius ; Andricopulo, Adriano D.
Total Authors: 3
Document type: Review article
Source: EXPERT OPINION ON DRUG DISCOVERY; v. 11, n. 10, p. 957-968, OCT 2016.
Web of Science Citations: 7

Introduction: Pocket-based drug design has contributed to major scientific breakthroughs in pharmaceutical research and development (R\&D). The integrated use of experimental and computational methods, primarily during the early phases of drug discovery, has enabled the development of highly potent and selective small-molecule ligands. In this scenario, the targeting of protein-protein interactions (PPIs) has emerged as an attractive strategy for designing innovative drugs for highly complex diseases, such as cancer. Areas covered: This article focuses on the use of experimental and computational approaches with a diversity of PPI classes and discusses the relevant advances in the field, primarily for oncological applications. Analyses of the target binding pockets and medicinal chemistry approaches used to develop promising PPI inhibitors are provided, with an emphasis on data reported over the past 2 years. Expert opinion: PPI drug discovery is a challenging field that depends completely on accurate structural data. The integration of molecular docking, nuclear magnetic resonance and X-ray crystallography is a cornerstone for the current development of effective PPI inhibitors. Although this field has not reached its peak, several compounds have entered clinical trials over the past few years, providing promising perspectives for novel therapies for highly prevalent and life-threatening conditions. (AU)

FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
Grantee:Glaucius Oliva
Support type: Research Grants - Research, Innovation and Dissemination Centers - RIDC
FAPESP's process: 13/25658-9 - Design and development of drug candidates for Chagas Disease
Grantee:Leonardo Luiz Gomes Ferreira
Support type: Scholarships in Brazil - Post-Doctorate