The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW

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• 作者：Anne Cathrine Nø ; hr^a ; Mohamed A. Shehata^a ; Alexander S. Hauser^a ; Vignir Isberg^a ; Jacek Mokrosinski^b ; Kirsten B. Andersen^a ; I. Sadaf Farooqi^b ; Daniel Sejer Pedersen^a ; David E. Gloriam^a ; ¹ ; ^{david.goriam@sund.ku.dk} ; Hans Brä ; uner-Osborne^a ; ¹ ; ^{hbo@sund.ku.dk}
• 关键词：Orphan GPCR ; GPR139 ; Pro-opiomelanocortin (POMC) ; Adrenocorticotropic hormone (ACTH) ; Melanocyte stimulating hormone (MSH) ; Peptide receptor
• 刊名：Neurochemistry International
• 出版年：2017
• 出版时间：January 2017
• 年：2017
• 卷：102
• 期：Complete
• 页码：105-113
• 全文大小：2076 K
• 卷排序：102

文摘

Using GPCRdb we found that the binding cavity of GPR139 is 49% similar to MC4R. ACTH, α-MSH and β-MSH activate GPR139 in the low μM-range. We predicted a novel possible cleavage site in POMC leading to the peptide α-MSH1-9. α-MSH1-9 activates GPR139 in the high nM range.