P35968

Background

Protein Name
Vascular endothelial growth factor receptor 2
Gene Name
KDR
Organism
Homo sapiens

Annotations

Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domain, such as isoform 2 and isoform 3, may function as decoy receptors for VEGFA, VEGFC and/or VEGFD. Isoform 2 plays an important role as negative regulator of VEGFA- and VEGFC-mediated lymphangiogenesis by limiting the amount of free VEGFA and/or VEGFC and preventing their binding to FLT4. Modulates FLT1 and FLT4 signaling by forming heterodimers. Binding of vascular growth factors to isoform 1 leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, reorganization of the actin cytoskeleton and activation of PTK2/FAK1. Required for VEGFA-mediated induction of NOS2 and NOS3, leading to the production of the signaling molecule nitric oxide (NO) by endothelial cells. Phosphorylates PLCG1. Promotes phosphorylation of FYN, NCK1, NOS3, PIK3R1, PTK2/FAK1 and SRC.

Mapping Statistics

Site Maximum Consensus Site Population Minimum Consensus Site Population Median Consensus Site Population
MPP 34 4 16.5
DFG 16 2 8.0
PIF 8 5 6.5
DRS 21 2 4.0
EDI 16 5 12.0
MT3 23 2 11.0
AAS 13 2 3.0
CMP 9 2 8.0
PDIG 24 3 14.5
ATP 22 1 12.0

Mapping Results

PDB ID Maximum Consensus Site Population
MPP site DFG site PIF site DRS site DEF site EDI site MT3 site AAS site LBP site CMP site PDIG site ATP site PMP site
Total Druggable Structures per Site 33 1 0 6 0 4 6 0 0 0 13 13 0
2QU6 19 0 0 5 0 13 0 2 0 8 18 15 0
3DTW 24 0 0 3 0 13 4 0 0 9 21 16 0
AFP35968 0 13 0 0 0 0 0 0 0 0 0 0 0
3B8Q 18 2 0 3 0 15 0 0 0 9 18 16 0
4AGD 16 0 0 0 0 0 15 0 0 0 6 0 0
3CP9 22 0 0 0 0 16 6 0 0 7 18 20 0
3VHE 28 0 0 0 0 0 0 0 0 0 14 18 0
2P2H 26 0 0 17 0 11 4 0 0 0 14 15 0
3VNT 26 0 0 2 0 0 0 0 0 0 10 12 0
3C7Q 15 0 0 21 0 0 17 3 0 0 3 6 0
3CJF 7 0 0 19 0 15 20 0 0 0 11 3 0
2OH4 17 0 0 0 0 0 0 3 0 0 20 17 0
1YWN 18 0 0 0 0 12 2 0 0 0 17 15 0
1Y6A 17 0 0 2 0 15 0 2 0 0 16 16 0
3U6J 16 0 5 2 0 8 15 0 0 0 9 13 0
5EW3 19 2 0 13 0 0 0 0 0 0 14 16 0
1Y6B 17 0 0 0 0 12 2 0 0 0 14 15 0
1VR2 16 0 0 9 0 16 0 9 0 0 0 4 0
2XIR 18 0 0 0 0 5 0 0 0 0 11 15 0
3BE2 22 0 0 5 0 13 0 0 0 4 15 16 0
4ASD 20 8 0 4 0 0 0 0 0 0 13 0 0
3EWH 15 0 8 0 0 15 0 0 0 2 10 18 0
2P2I 34 0 0 8 0 16 11 0 0 8 18 15 0
4AG8 17 0 0 6 0 0 11 0 0 0 10 0 0
3EFL 29 16 0 0 0 14 0 0 0 8 20 17 0
3VO3 17 0 0 0 0 11 0 13 0 0 10 15 0
3B8R 24 0 0 7 0 10 21 0 0 5 18 22 0
2RL5 18 0 0 20 0 9 8 5 0 0 24 15 0
3CPC 25 0 0 13 0 16 23 0 0 9 16 11 0
3WZE 24 0 0 0 0 0 4 0 0 0 15 9 0
3CJG 27 0 0 15 0 0 23 0 0 0 14 4 0
3VHK 21 0 0 2 0 9 16 0 0 0 9 4 0
4ASE 18 0 0 0 0 0 0 0 0 0 12 15 0
4AGC 28 0 0 0 0 0 0 0 0 0 11 13 0
2QU5 18 0 0 17 0 14 0 0 0 0 15 15 0
3CPB 20 9 0 4 0 12 0 0 0 8 17 18 0
3VID 14 0 0 16 0 0 0 0 0 0 7 12 0
3WZD 25 0 0 9 0 0 0 0 0 0 13 19 0