S1PR5 explained

Sphingosine-1-phosphate receptor 5 also known as S1PR5 is a human gene which encodes a G protein-coupled receptor which binds the lipid signaling molecule sphingosine 1-phosphate (S1P). Hence this receptor is also known as S1P₅.^[1]

Agonists

• A-971432^[2]
• Sphingosine 1-phosphate receptor agonists: a patent review (2010-2012)^[3]

Evolution

Paralogues for S1PR5 Gene ^[4]

• S1PR1
• S1PR3
• S1PR2
• S1PR4
• LPAR1
• LPAR2
• GPR3
• LPAR3
• GPR12
• CNR1
• GPR6
• CNR2
• MC4R
• MC3R
• MC5R
• GPR119
• MC1R
• MC2R

See also

• Lysophospholipid receptor

Further reading

• Im DS, Heise CE, Ancellin N, O'Dowd BF, Shei GJ, Heavens RP, Rigby MR, Hla T, Mandala S, McAllister G, George SR, Lynch KR . Characterization of a novel sphingosine 1-phosphate receptor, Edg-8 . The Journal of Biological Chemistry . 275 . 19 . 14281–6 . May 2000 . 10799507 . 10.1074/jbc.275.19.14281 . free .
• Malek RL, Toman RE, Edsall LC, Wong S, Chiu J, Letterle CA, Van Brocklyn JR, Milstien S, Spiegel S, Lee NH . Nrg-1 belongs to the endothelial differentiation gene family of G protein-coupled sphingosine-1-phosphate receptors . The Journal of Biological Chemistry . 276 . 8 . 5692–9 . Feb 2001 . 11069896 . 10.1074/jbc.M003964200 . free .
• Hla T . Sphingosine 1-phosphate receptors . Prostaglandins . 64 . 1–4 . 135–142 . Apr 2001 . 11331101 . 10.1016/s0090-6980(01)00109-5 .
• Im DS, Clemens J, Macdonald TL, Lynch KR . Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors . Biochemistry . 40 . 46 . 14053–60 . Nov 2001 . 11705398 . 10.1021/bi011606i .
• Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S . Identification of G protein-coupled receptor genes from the human genome sequence . FEBS Letters . 520 . 1–3 . 97–101 . Jun 2002 . 12044878 . 10.1016/S0014-5793(02)02775-8 . 7116392 . free .
• Niedernberg A, Scherer CR, Busch AE, Kostenis E . Comparative analysis of human and rat S1P(5) (edg8): differential expression profiles and sensitivities to antagonists . Biochemical Pharmacology . 64 . 8 . 1243–50 . Oct 2002 . 12234605 . 10.1016/S0006-2952(02)01289-3 .
• Kothapalli R, Kusmartseva I, Loughran TP . Characterization of a human sphingosine-1-phosphate receptor gene (S1P5) and its differential expression in LGL leukemia . Biochimica et Biophysica Acta (BBA) - Gene Structure and Expression . 1579 . 2–3 . 117–23 . Dec 2002 . 12427546 . 10.1016/S0167-4781(02)00529-8 .
• Vogler R, Sauer B, Kim DS, Schäfer-Korting M, Kleuser B . Sphingosine-1-phosphate and its potentially paradoxical effects on critical parameters of cutaneous wound healing . The Journal of Investigative Dermatology . 120 . 4 . 693–700 . Apr 2003 . 12648236 . 10.1046/j.1523-1747.2003.12096.x . free .
• Ulfig N, Briese M . Evidence for the presence of the sphingosine-1-phosphate receptor Edg-8 in human radial glial fibers . Acta Histochemica . 106 . 5 . 373–8 . 2005 . 15530552 . 10.1016/j.acthis.2004.08.002 .
• Huda Zoghbi . Rual JF, Venkatesan K, Hao T, Hirozane-Kishikawa T, Dricot A, Li N, Berriz GF, Gibbons FD, Dreze M, Ayivi-Guedehoussou N, Klitgord N, Simon C, Boxem M, Milstein S, Rosenberg J, Goldberg DS, Zhang LV, Wong SL, Franklin G, Li S, Albala JS, Lim J, Fraughton C, Llamosas E, Cevik S, Bex C, Lamesch P, Sikorski RS, Vandenhaute J, Zoghbi HY, Smolyar A, Bosak S, Sequerra R, Doucette-Stamm L, Cusick ME, Hill DE, Roth FP, Vidal M . Towards a proteome-scale map of the human protein-protein interaction network . Nature . 437 . 7062 . 1173–8 . Oct 2005 . 16189514 . 10.1038/nature04209 . 2005Natur.437.1173R . 4427026 .
• Otsuki T, Ota T, Nishikawa T, Hayashi K, Suzuki Y, Yamamoto J, Wakamatsu A, Kimura K, Sakamoto K, Hatano N, Kawai Y, Ishii S, Saito K, Kojima S, Sugiyama T, Ono T, Okano K, Yoshikawa Y, Aotsuka S, Sasaki N, Hattori A, Okumura K, Nagai K, Sugano S, Isogai T . Signal sequence and keyword trap in silico for selection of full-length human cDNAs encoding secretion or membrane proteins from oligo-capped cDNA libraries . DNA Research . 12 . 2 . 117–26 . 2007 . 16303743 . 10.1093/dnares/12.2.117 . free .
• Van der Kam E, Turner S, van Bergeij J, Mueller R, Mezler M, Bespalov A, Hobson A, Harris CM, Rendenbach-Mueller B, Schoemaker H . The use of selective sphingosine-1-phosphate receptor 5 agonists for the treatment of neurodegenerative disorders such as alzheimer's disease and lysosomal storage diseases such as niemann-pick c disease . Alzheimer's & Dementia . Jun 2014 . 10.1016/j.jalz.2014.07.153 . 10 . P281. 54386805 .
• Jenne CN, Enders A, Rivera R, Watson SR, Bankovich AJ, Pereira JP, Xu Y, Roots CM, Beilke JN, Banerjee A, Reiner SL, Miller SA, Weinmann AS, Goodnow CC, Lanier LL, Cyster JG, Chun J . T-bet-dependent S1P5 expression in NK cells promotes egress from lymph nodes and bone marrow . J Exp Med . Oct 2009 . 19808259 . 10.1084/jem.20090525 . 206 . 11 . 2768857 . 2469–81.

External links

• Web site: Lysophospholipid Receptors: S₁P₅ . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology .

Notes and References

1. Web site: Entrez Gene: S1PR5 Sphingosine-1-phosphate receptor 5 .
2. Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G, Kim Y, Larson K, Maull JW, Moore NS, Shi D, Shrestha A, Tang X, Zhang P, Sarris KK . Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders . Journal of Medicinal Chemistry . Nov 2015 . 26509640 . 10.1021/acs.jmedchem.5b00928 . 58 . 23 . 9154–70.
3. Roberts E, Guerrero M, Urbano M, Rosen H . Sphingosine 1-phosphate receptor agonists: a patent review (2010-2012) . Expert Opin Ther Pat . Jul 2013 . 23541049 . 10.1517/13543776.2013.783022 . 23 . 7 . 817–41. 24421259 .
4. Web site: GeneCards®: The Human Gene Database .