Adiponectin receptor 2
Adiponectin receptor 2 (AdipoR2) is a protein which in humans is encoded by the ADIPOR2 gene.[1]
Structure
Similar to G protein-coupled receptors (GPCRs), AdipoR2 also possesses 7 transmembrane domains. However, AdipoR2 is orientated oppositely to GPCRs in the membrane (i.e., cytoplasmic N-terminus, extracellular C-terminus) and does not associate with G proteins.[1]
Function
The adiponectin receptors, AdipoR1 and AdipoR2, serve as receptors for globular and full-length adiponectin and mediate increased AMPK and PPAR-α ligand activities, as well as fatty acid oxidation and glucose uptake by adiponectin.[1]
Ligands
Agonists
Peptide
- Adiponectin
- ADP-355[2]
- ADP-399[2]
Non-peptide
Antagonists
Peptide
- ADP-400[2]
See also
References
- 1 2 3 Yamauchi T, Kamon J, Ito Y, Tsuchida A, Yokomizo T, Kita S, Sugiyama T, Miyagishi M, Hara K, Tsunoda M, Murakami K, Ohteki T, Uchida S, Takekawa S, Waki H, Tsuno NH, Shibata Y, Terauchi Y, Froguel P, Tobe K, Koyasu S, Taira K, Kitamura T, Shimizu T, Nagai R, Kadowaki T (June 2003). "Cloning of adiponectin receptors that mediate antidiabetic metabolic effects". Nature 423 (6941): 762–9. doi:10.1038/nature01705. PMID 12802337.
- 1 2 3 Otvos L, Knappe D, Hoffmann R, Kovalszky I, Olah J, Hewitson TD, Stawikowska R, Stawikowski M, Cudic P, Lin F, Wade JD, Surmacz E, Lovas S (2014). "Development of second generation peptides modulating cellular adiponectin receptor responses". Front Chem 2: 93. doi:10.3389/fchem.2014.00093. PMC 4201147. PMID 25368867.
- ↑ Okada-Iwabu M, Yamauchi T, Iwabu M, Honma T, Hamagami K, Matsuda K, Yamaguchi M, Tanabe H, Kimura-Someya T, Shirouzu M, Ogata H, Tokuyama K, Ueki K, Nagano T, Tanaka A, Yokoyama S, Kadowaki T (2013). "A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity". Nature 503 (7477): 493–9. doi:10.1038/nature12656. PMID 24172895.
- 1 2 3 4 Sun Y, Zang Z, Zhong L, Wu M, Su Q, Gao X, Zan W, Lin D, Zhao Y, Zhang Z (2013). "Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay". PLoS ONE 8 (5): e63354. doi:10.1371/journal.pone.0063354. PMC 3653934. PMID 23691032.
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