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Recent Advances in Structure-Based Drug Design Targeting Class A G Protein-Coupled Receptors Utilizing Crystal Structures and Computational Simulations

Title
Recent Advances in Structure-Based Drug Design Targeting Class A G Protein-Coupled Receptors Utilizing Crystal Structures and Computational Simulations
Authors
Lee, YoonjiBasith, ShaherinChoi, Sun
Ewha Authors
최선이윤지
SCOPUS Author ID
최선scopus; 이윤지scopus
Issue Date
2018
Journal Title
JOURNAL OF MEDICINAL CHEMISTRY
ISSN
0022-2623JCR Link1520-4804JCR Link
Citation
vol. 61, no. 1, pp. 1 - 46
Publisher
AMER CHEMICAL SOC
Indexed
SCI; SCIE; SCOPUS WOS
Abstract
G protein-coupled receptors (GPCRs) represent the largest and most physiologically important integral membrane protein family, and these receptors respond to a wide variety of physiological and environmental stimuli. GPCRs are among the most critical therapeutic targets for numerous human diseases, and approximately one-third of the currently marketed drugs target this receptor family.The recent breakthroughs in GPCR structural biology have significantly contributed to our understanding of GPCR function, ligand binding, and pharmacological action as well as to the design of new drugs. This perspective highlights the latest advances in GPCR structures with a focus on the receptor ligand interactions of each receptor family in class A nonrhodopsin GPCRs as well as the structural features for their activation, biased :signaling, and allosteric mechanisms. The current state-of-the-art methodologies of structure-based drug design (ODD) approaches in the GPCR research field are also discussed.
DOI
10.1021/acs.jmedchem.6b01453
Appears in Collections:
약학대학 > 약학과 > Journal papers
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