PDGFRA

PDGFRA
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
Aliases PDGFRA, CD140A, PDGFR-2, PDGFR2, RHEGAS9, platelet derived growth factor receptor alpha
External IDs MGI: 97530 HomoloGene: 31361 GeneCards: PDGFRA
Genetically Related Diseases
astigmatism[1]
Targeted by Drug
cediranib, crenolanib, masitinib, nintedanib[2]
RNA expression pattern
More reference expression data
Orthologs
Species Human Mouse
Entrez

5156

18595

Ensembl

ENSG00000134853

ENSMUSG00000029231

UniProt

P16234

P26618

RefSeq (mRNA)

NM_006206

NM_001083316
NM_011058

RefSeq (protein)

NP_006197.1

NP_001076785.1
NP_035188.2

Location (UCSC) Chr 4: 54.23 – 54.3 Mb Chr 5: 75.15 – 75.2 Mb
PubMed search [3] [4]
Wikidata
View/Edit HumanView/Edit Mouse

Platelet-derived growth factor receptor, alpha polypeptide is a protein that in humans is encoded by the PDGFRA gene.

Function

This gene encodes a cell surface tyrosine kinase receptor for members of the platelet-derived growth factor family. These growth factors are mitogens for cells of mesenchymal origin. The identity of the growth factor bound to a receptor monomer determines whether the functional receptor is a homodimer or a heterodimer, composed of both platelet-derived growth factor receptor alpha and beta polypeptides. Studies in knockout mice, where homozygosity is lethal, indicate that the alpha form of the platelet-derived growth factor receptor is particularly important for kidney development since mice heterozygous for the receptor exhibit defective kidney phenotypes.[5]

Interactions

PDGFRA has been shown to interact with:

Monoclonal Antibody

Lilly has developed Olaratumab, (LY3012207) a human IgG1 monoclonal antibody designed to bind to human PDGFRα with high affinity and block PDGF-AA, PDGF-BB, and PDGF-CC ligands from binding to the receptor and is conducting clinical trials (2016) in patients with soft-tissue sarcoma.[15]

See also

References

  1. ↑ "Diseases that are genetically associated with PDGFRA view/edit references on wikidata".
  2. ↑ "Drugs that physically interact with Platelet-derived growth factor receptor alpha view/edit references on wikidata".
  3. ↑ "Human PubMed Reference:".
  4. ↑ "Mouse PubMed Reference:".
  5. ↑ "Entrez Gene: PDGFRA platelet-derived growth factor receptor, alpha polypeptide".
  6. ↑ Yokote K, Hellman U, Ekman S, Saito Y, Rönnstrand L, Saito Y, Heldin CH, Mori S (March 1998). "Identification of Tyr-762 in the platelet-derived growth factor alpha-receptor as the binding site for Crk proteins". Oncogene. 16 (10): 1229–39. doi:10.1038/sj.onc.1201641. PMID 9546424.
  7. ↑ Matsumoto T, Yokote K, Take A, Takemoto M, Asaumi S, Hashimoto Y, Matsuda M, Saito Y, Mori S (April 2000). "Differential interaction of CrkII adaptor protein with platelet-derived growth factor alpha- and beta-receptors is determined by its internal tyrosine phosphorylation". Biochem. Biophys. Res. Commun. 270 (1): 28–33. doi:10.1006/bbrc.2000.2374. PMID 10733900.
  8. ↑ Yamamoto M, Toya Y, Jensen RA, Ishikawa Y (March 1999). "Caveolin is an inhibitor of platelet-derived growth factor receptor signaling". Exp. Cell Res. 247 (2): 380–8. doi:10.1006/excr.1998.4379. PMID 10066366.
  9. ↑ Bonita DP, Miyake S, Lupher ML, Langdon WY, Band H (August 1997). "Phosphotyrosine binding domain-dependent upregulation of the platelet-derived growth factor receptor alpha signaling cascade by transforming mutants of Cbl: implications for Cbl's function and oncogenicity". Mol. Cell. Biol. 17 (8): 4597–610. doi:10.1128/mcb.17.8.4597. PMC 232313Freely accessible. PMID 9234717.
  10. ↑ Gilbertson DG, Duff ME, West JW, Kelly JD, Sheppard PO, Hofstrand PD, Gao Z, Shoemaker K, Bukowski TR, Moore M, Feldhaus AL, Humes JM, Palmer TE, Hart CE (July 2001). "Platelet-derived growth factor C (PDGF-C), a novel growth factor that binds to PDGF alpha and beta receptor". J. Biol. Chem. 276 (29): 27406–14. doi:10.1074/jbc.M101056200. PMID 11297552.
  11. ↑ Rupp E, Siegbahn A, Rönnstrand L, Wernstedt C, Claesson-Welsh L, Heldin CH (October 1994). "A unique autophosphorylation site in the platelet-derived growth factor alpha receptor from a heterodimeric receptor complex". Eur. J. Biochem. 225 (1): 29–41. doi:10.1111/j.1432-1033.1994.00029.x. PMID 7523122.
  12. ↑ Seifert RA, Hart CE, Phillips PE, Forstrom JW, Ross R, Murray MJ, Bowen-Pope DF (May 1989). "Two different subunits associate to create isoform-specific platelet-derived growth factor receptors". J. Biol. Chem. 264 (15): 8771–8. PMID 2542288.
  13. ↑ Eriksson A, Nånberg E, Rönnstrand L, Engström U, Hellman U, Rupp E, Carpenter G, Heldin CH, Claesson-Welsh L (March 1995). "Demonstration of functionally different interactions between phospholipase C-gamma and the two types of platelet-derived growth factor receptors". J. Biol. Chem. 270 (13): 7773–81. doi:10.1074/jbc.270.13.7773. PMID 7535778.
  14. ↑ Maudsley S, Zamah AM, Rahman N, Blitzer JT, Luttrell LM, Lefkowitz RJ, Hall RA (November 2000). "Platelet-derived growth factor receptor association with Na(+)/H(+) exchanger regulatory factor potentiates receptor activity". Mol. Cell. Biol. 20 (22): 8352–63. doi:10.1128/mcb.20.22.8352-8363.2000. PMC 102142Freely accessible. PMID 11046132.
  15. ↑ https://investor.lilly.com/releasedetail.cfm?ReleaseID=969023

Further reading

  • Hart CE, Bowen-Pope DF (1990). "Platelet-derived growth factor receptor: current views of the two-subunit model". J. Invest. Dermatol. 94 (6 Suppl): 53S–57S. doi:10.1111/1523-1747.ep12875065. PMID 2161888. 
  • Corless CL, Schroeder A, Griffith D, Town A, McGreevey L, Harrell P, Shiraga S, Bainbridge T, Morich J, Heinrich MC (2005). "PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib". J. Clin. Oncol. 23 (23): 5357–64. doi:10.1200/JCO.2005.14.068. PMID 15928335. 
  • Lasota J, Miettinen M (2007). "KIT and PDGFRA mutations in gastrointestinal stromal tumors (GISTs)". Semin Diagn Pathol. 23 (2): 91–102. doi:10.1053/j.semdp.2006.08.006. PMID 17193822. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

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