Two ligands for a GPCR, proton vs lysolipid.
Recently, two different chemicals have been matched as ligands with the same G-protein-coupled receptor (GPCR). Double-pairing of OGR1 family GPCRs with proton and lysolipid raises several questions. First, whether both are the real ligands for the GPCRs. Second, whether modulation of a GPCR by two chemicals could be possible. Third, one of the chemicals is proton. Proton-sensing not only is a new action mode of GPCR activation, but also it could be generalized in other GPCRs. In this review, I would like to summarize the issue and discuss questions with pharmacological criteria.
Im
Dong-Soon
DS
Laboratory of Pharmacology and Research Institute of Drug Development, College of Pharmacy, Pusan National University, Busan 609-735, Republic of Korea. imds@pusan.ac.kr
D000595:Amino Acid Sequence; D000818:Animals; D018797:Cell Cycle Proteins / Q000819:agonists / Q000737:chemistry / Q000378:metabolism / Q000502:physiology; D006801:Humans; D008024:Ligands; D008244:Lysophosphatidylcholines / Q000737:chemistry / Q000378:metabolism; D008969:Molecular Sequence Data; D010767:Phosphorylcholine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D011522:Protons; D011609:Psychosine / Q000737:chemistry / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000737:chemistry / Q000378:metabolism / Q000502:physiology*; D016415:Sequence Alignment; D015398:Signal Transduction; D013110:Sphingosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism
D018797:Cell Cycle Proteins; C115270:G2A receptor; C091670:GPR4 protein, human; C513334:GPR65 protein, human; C486281:GPR68 protein, human; D008024:Ligands; D008244:Lysophosphatidylcholines; D011522:Protons; D043562:Receptors, G-Protein-Coupled; C005356:sphingosine phosphorylcholine; D010767:Phosphorylcholine; D011609:Psychosine; D013110:Sphingosine