期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 204, 期 -, 页码 -出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112631
关键词
Cystic fibrosis; Cystic fibrosis transmembrane conductance regulator; CFTR; CFTR potentiators; VX-770
资金
- Fondazione Italiana per la Ricerca sulla Fibrosi Cistica [4/2018]
Cystic fibrosis (CF) is a genetic disorder produced by the loss of function of CFTR, a main chloride channel involved in transepithelial salt and water transport. CFTR function can be rescued by small molecules called potentiators which increase gating activity of CFTR on epithelial surfaces. High throughput screening (HTS) assays allowed the identification of new chemical entities endowed with potentiator properties, further improved through medicinal chemistry optimization. In this review, the most relevant classes of CFTR potentiators developed in the last decade were explored, focusing on structure-activity relationships (SAR) of the different chemical entities, as a useful tool for the improvement of their pharmacological activity. (C) 2020 Elsevier Masson SAS. All rights reserved.
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