Product Name: KinSub1RTLYF
Product Number: PE-01AJQ95
Size: 200 µg      Price:99.00
      $US
Peptide Name: KinSub1RTLYF

Product Use: For assaying the phosphotransferase activity of Platelet-derived growth factor receptor kinase beta (PDGFRB, UniProt ID P09619). The KinSub1RTLYF peptide demonstrated low phosphotransferase activity with PDGFRB, and exhibited medium specificity when assayed with over 200 other protein kinases. A listing of other kinases that show appreciable phosphotransferase activity towards this peptide are listed in Table 1.

Peptide Production Method: Solid-phase peptide synthesis

Peptide Origin: KinSub1RTLYF was originally identified using a microarray with peptides that were predicted as optimal substrates for 500 human protein kinases with a proprietary algorithm developed at Kinexus with our academic partners.

Peptide Sequence: HGRSRTLYFYVRGYR

Peptide Modifications N Terminus: Free amino

Peptide Modifications C Terminus: Amide

Peptide Molecular Mass Calculated: 1930.2 Da

Peptide Purity Percent after Synthesis and Purification: >95

Peptide Appearance: White powder

Peptide Form: Solid

Storage Conditions: -20°C

Peptide Recommended Enzyme: PDGFRB

Scientific Background: PDGFRB is one of several protein kinases that can phosphorylate KinSub1RTLYF. Human PDGFRB is a protein-tyrosine kinase of 1106 amino acid length, with a predicted molecular mass of 123,968 Da. It is a member of the TK group of protein kinases in the PDGFR family. It is highly expressed and widely distributed in most tested human tissues. Orthologues are highly conserved in mammals and birds. PDGFRB is activated by binding platelet-derived growth factor. Autophosphorylation of Y579, Y581, Y716, Y740 and Y751 increases PDGFRB kinase activity. Protein interactions are induced with phosphorylation of Y716 (with Grb2 & Grb7), Y579 (with PIK3R1, PLCg1, RasGAP, Shc1 & Src), Y581 (with PIK3R1, PLCg1, RasGAP & Src), Y740 and Y751 (with PIK3C2A, PIK3CA, PIK3R1 & Shc1), Y763 (with SHP2), Y771 (with RasGAP and Shc1), Y775 (with Grb7), Y1009 (with Cbl, PLCg1, SH3KBP1 & SHP2), and Y1021 (with PLCg1). Phosphorylation of Y1009 inhibits binding to PIK3R1 and RasGAP. PDGFRb-deficient mice are hemorrhagic, severely anemic and exhibit a defect in kidney glomeruli function (1). PDGFRb expression and activity is elevated in several cancers and inhibition of PDGFRb activity blocks progression of renal carcinoma in an animal model (2). PDGFRB has also been linked with myeloproliferative disorders, metastatic medulloblastomas, breast carcinomas and gastric adenocarcinomas.
References

[1] Soriano P. Abnormal kidney development and hematological disorders in PDGF beta-receptor mutant mice. Genes Dev. 1994 Aug 15;8(16):1888-96. PMID:7958864

[2] Xu L, Tong R, Cochran DM, Jain RK. Blocking platelet-derived growth factor-D/platelet-derived growth factor receptor beta signaling inhibits human renal cell carcinoma progression in an orthotopic mouse model. Cancer Res. 2005 Jul 1;65(13):5711-9. PMID:15994946