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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

From Protein Structure to Small-Molecules: Recent Advances and Applications to Fragment-Based Drug Discovery

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Autor(es):
Ferreira, Leonardo G. ; Andricopulo, Adriano D.
Número total de Autores: 2
Tipo de documento: Artigo de Revisão
Fonte: CURRENT TOPICS IN MEDICINAL CHEMISTRY; v. 17, n. 20, p. 2260-2270, 2017.
Citações Web of Science: 3
Resumo

Fragment-based drug discovery (FBDD) is a broadly used strategy in structure-guided ligand design, whereby low-molecular weight hits move from lead-like to drug-like compounds. Over the past 15 years, an increasingly important role of the integration of these strategies into industrial and academic research platforms has been successfully established, allowing outstanding contributions to drug discovery. One important factor for the current prominence of FBDD is the better coverage of the chemical space provided by fragment-like libraries. The development of the field relies on two features: (i) the growing number of structurally characterized drug targets and (ii) the enormous chemical diversity available for experimental and virtual screenings. Indeed, fragment-based campaigns have contributed to address major challenges in lead optimization, such as the appropriate physicochemical profile of clinical candidates. This perspective paper outlines the usefulness and applications of FBDD approaches in medicinal chemistry and drug design. (AU)

Processo FAPESP: 13/07600-3 - CIBFar - Centro de Inovação em Biodiversidade e Fármacos
Beneficiário:Glaucius Oliva
Linha de fomento: Auxílio à Pesquisa - Centros de Pesquisa, Inovação e Difusão - CEPIDs
Processo FAPESP: 13/25658-9 - Planejamento e desenvolvimento de candidatos a fármacos para a Doença de Chagas
Beneficiário:Leonardo Luiz Gomes Ferreira
Linha de fomento: Bolsas no Brasil - Pós-Doutorado