Please use this identifier to cite or link to this item: https://doi.org/10.3390/ph15010012
Title: Recent Advances in Structure, Function, and Pharmacology of Class A Lipid GPCRs: Opportunities and Challenges for Drug Discovery
Authors: Krishna Deepak, RNV
Verma, Ravi Kumar
Hartono, Yossa Dwi 
Yew, Wen Shan 
Fan, Hao 
Keywords: Science & Technology
Life Sciences & Biomedicine
Chemistry, Medicinal
Pharmacology & Pharmacy
lipid GPCR
ligand access
orthosteric and allosteric binding sites
drug discovery
antibody
computational methods
prostaglandin receptor
platelet-activating factor receptor
sphingosine-1-phosphate receptor
lysophosphatidic acid receptor
leukotriene receptor
free fatty acid receptor
cannabinoid receptor
PROTEIN-COUPLED RECEPTOR
STABILIZED ACTIVE STATE
CRYO-EM STRUCTURE
CRYSTAL-STRUCTURE
ALLOSTERIC MODULATION
LIGAND-BINDING
ACTIVATION
MECHANISMS
INSIGHTS
SITES
Issue Date: 1-Jan-2022
Publisher: MDPI
Citation: Krishna Deepak, RNV, Verma, Ravi Kumar, Hartono, Yossa Dwi, Yew, Wen Shan, Fan, Hao (2022-01-01). Recent Advances in Structure, Function, and Pharmacology of Class A Lipid GPCRs: Opportunities and Challenges for Drug Discovery. PHARMACEUTICALS 15 (1). ScholarBank@NUS Repository. https://doi.org/10.3390/ph15010012
Abstract: Great progress has been made over the past decade in understanding the structural, functional, and pharmacological diversity of lipid GPCRs. From the first determination of the crystal structure of bovine rhodopsin in 2000, much progress has been made in the field of GPCR structural biology. The extraordinary progress in structural biology and pharmacology of GPCRs, coupled with rapid advances in computational approaches to study receptor dynamics and receptorligand interactions, has broadened our comprehension of the structural and functional facets of the receptor family members and has helped usher in a modern age of structure-based drug design and development. First, we provide a primer on lipid mediators and lipid GPCRs and their role in physiology and diseases as well as their value as drug targets. Second, we summarize the current advancements in the understanding of structural features of lipid GPCRs, such as the structural variation of their extracellular domains, diversity of their orthosteric and allosteric ligand binding sites, and molecular mechanisms of ligand binding. Third, we close by collating the emerging paradigms and opportunities in targeting lipid GPCRs, including a brief discussion on current strategies, challenges, and the future outlook.
Source Title: PHARMACEUTICALS
URI: https://scholarbank.nus.edu.sg/handle/10635/218856
ISSN: 14248247
DOI: 10.3390/ph15010012
Appears in Collections:Staff Publications
Elements

Show full item record
Files in This Item:
File Description SizeFormatAccess SettingsVersion 
Recent Advances in Structure, Function, and Pharmacology of Class A Lipid GPCRs Opportunities and Challenges for Drug Discov.pdf6.87 MBAdobe PDF

OPEN

PublishedView/Download

SCOPUSTM   
Citations

3
checked on Sep 23, 2022

Page view(s)

39
checked on Sep 22, 2022

Download(s)

29
checked on Sep 22, 2022

Google ScholarTM

Check

Altmetric


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.