Recent Advances in Structure, Function, and Pharmacology of Class A Lipid GPCRs: Opportunities and Challenges for Drug Discovery
| Autor: | R. N. V. Krishna Deepak, Ravi Kumar Verma, Yossa Dwi Hartono, Wen Shan Yew, Hao Fan |
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| Jazyk: | angličtina |
| Rok vydání: | 2022 |
| Předmět: |
lysophosphatidic acid receptor
platelet-activating factor receptor Pharmaceutical Science ligand access cannabinoid receptor Review drug discovery lipid GPCR RS1-441 leukotriene receptor computational methods Pharmacy and materia medica antibody prostaglandin receptor sphingosine-1-phosphate receptor orthosteric and allosteric binding sites Molecular Medicine Medicine free fatty acid receptor |
| Zdroj: | Pharmaceuticals, Vol 15, Iss 12, p 12 (2022) Pharmaceuticals |
| ISSN: | 1424-8247 |
| Popis: | 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 receptor-ligand 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. |
| Databáze: | OpenAIRE |
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