The Potential of 19F NMR Application in GPCR Biased Drug Discovery.
 

The Potential of 19F NMR Application in GPCR Biased Drug Discovery.

http://www.bionmr.com//www.ncbi.nlm....es-cellhub.gif Related Articles The Potential of 19F NMR Application in GPCR Biased Drug Discovery.

Trends Pharmacol Sci. 2020 Nov 26;:

Authors: Wang X, McFarland A, Madsen JJ, Aalo E, Ye L

Abstract
Although structure-based virtual drug discovery is revolutionizing the conventional high-throughput cell-based screening system, its limitation is obvious, together with other critical challenges. In particular, the resolved static snapshots fail to represent a full free-energy landscape due to homogenization in structural determination processing. The loss of conformational heterogeneity and related functional diversity emphasize the necessity of developing an approach that can fill this space. In this regard, NMR holds undeniable potential. However, outstanding questions regarding the NMR application remain. This review summarizes the limitations of current drug discovery and explores the potential of 19F NMR in establishing a conformation-guided drug screening system, advancing the cell- and structure-based discovery strategy for G protein-coupled receptor (GPCR) biased drug screening.


PMID: 33250272 [PubMed - as supplied by publisher]



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