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From Proteopedia
Cryo-EM structure of human galanin receptor 2
Structural highlights
Function[GALR2_HUMAN] Receptor for the hormone galanin and GALP. Receptor for the hormone spexin-1 (PubMed:24517231). The activity of this receptor is mediated by G proteins that activate the phospholipase C/protein kinase C pathway (via G(q)) and that inhibit adenylyl cyclase (via G(i)).[1] [2] [3] [4] [5] [6] Publication Abstract from PubMedGalanin is a neuropeptide expressed in the central and peripheral nervous systems, where it regulates various processes including neuroendocrine release, cognition, and nerve regeneration. Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts to treat diseases including Alzheimer's disease, anxiety, and addiction. To understand the basis of the ligand preferences of the receptors and to assist structure-based drug design, we used cryo-electron microscopy (cryo-EM) to solve the molecular structure of GALR2 bound to galanin and a cognate heterotrimeric G-protein, providing a molecular view of the neuropeptide binding site. Mutant proteins were assayed to help reveal the basis of ligand specificity, and structural comparison between the activated GALR2 and inactive hbeta2AR was used to relate galanin binding to the movements of transmembrane (TM) helices and the G-protein interface. Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand specificity and how binding affects the G-protein interface.,Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY PLoS Biol. 2022 Aug 1;20(8):e3001714. doi: 10.1371/journal.pbio.3001714., eCollection 2022 Aug. PMID:35913979[7] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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