Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects
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چکیده
منابع مشابه
Effects of selective dopamine receptor (Dl and D2) agonists on stress-induced gastric ulcer in rat
It has been revealed that dopamine (DA) modulates gastro-duodenal responses to stress. Several investigations have been made to identify the mechanisms and/or receptors by which DA or its promoters exert their gastroprotective function against stress, however there are many discrepancies in this respect. In order to clarify the relative contribution and/or interaction of two DA receptor subty...
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Lactate is an important metabolic intermediate released by skeletal muscle and other organs including the adipose tissue, which converts glucose into lactate under the influence of insulin. Here we show that lactate activates the G protein-coupled receptor GPR81, which is expressed in adipocytes and mediates antilipolytic effects through G(i)-dependent inhibition of adenylyl cyclase. Using GPR8...
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Receptors from distant species may have conserved functions despite significant differences in protein sequences. Whereas the noncritical residues are often changed in distant species, the amino acids critical in receptor functions are often conserved. Studying the conserved residues between receptors from distant species offers valuable information to probe the roles of residues in receptor fu...
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Background: In this study, the effects of three structural analogues of adenosine upon proliferation of human tumor cells were investigated. Previous research showed a cytotoxic effect of adenosine via A3 receptor and A1 receptor and sometimes this effect was receptor independent. The researches showed a differential cytotoxic effect of adenosine and its A3 agonists on cancerous cells, while ot...
متن کاملLactate inhibits lipolysis in fat cells through activation of an orphan G-protein-coupled receptor, GPR81.
Lactic acid is a well known metabolic by-product of intense exercise, particularly under anaerobic conditions. Lactate is also a key source of energy and an important metabolic substrate, and it has also been hypothesized to be a signaling molecule directing metabolic activity. Here we show that GPR81, an orphan G-protein-coupled receptor highly expressed in fat, is in fact a sensor for lactate...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2012
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml3000676