KDR
ENSG00000128052
Target class
Kinase
Chromosome
4
Approved drugs
15
Clinical candidates (approved and in development)
75
- Approved drugs
- 15
- ClinGen gene-disease validity
- Definitive
- Clinical candidates (approved and in development)
- 75
- Chemical probe available
- Yes
- Target name
- KDR
- Gene name
- Kinase insert domain receptor
- Gene symbol
- KDR
- Protein name
- Vascular endothelial growth factor receptor 2 (VEGFR-2) (EC 2.7.10.1) (Fetal liver kinase 1) (FLK-1) (Kinase insert domain receptor) (KDR) (Protein-tyrosine kinase receptor flk-1) (CD antigen CD309)
- FLK1
- VEGFR
- VEGFR2
- CD309
- Gene biotype
- Protein coding
- Gene family
- Receptor tyrosine kinases|CD molecules|V-set domain containing|I-set domain containing
- Target class
- Kinase
- Target type
- Human gene
- Tissues expressed in
- 52
- Protein localisation evidence grade
- Approved
- Highest tissue expression
- 80.12
- Tissue specificity (Gini)
- 0.553
- Tissue specificity (tau)
- 0.808
- KEGG gene identifiers
- hsa:3791
- Protein interaction confidence
- 0.865438
- Protein interaction partners
- 153
- R-HSA-194306
- R-HSA-195399
- R-HSA-216083
- R-HSA-4420097
- R-HSA-5218921
- R-HSA-9673768
- R-HSA-9856530
- End position
- 55125595
- Start position
- 55078476
- Chromosome
- 4
- Strand
- Reverse
- Cell junction . Endoplasmic reticulum . Cell membrane . Note=Localized with RAP1A at cell-cell junctions (By similarity). Colocalizes with ERN1 and XBP1 in the endoplasmic reticulum in endothelial cells in a vascular endothelial growth factor (VEGF)-dependent manner (PubMed:23529610). .
- SUBCELLULAR LOCATION: [Isoform 1]: Cell membrane
- Single-pass type I membrane protein. Cytoplasm. Nucleus. Cytoplasmic vesicle. Early endosome. Note=Detected on caveolae-enriched lipid rafts at the cell surface. Is recycled from the plasma membrane to endosomes and back again. Phosphorylation triggered by VEGFA binding promotes internalization and subsequent degradation. VEGFA binding triggers internalization and translocation to the nucleus.
- SUBCELLULAR LOCATION: [Isoform 2]: Secreted .
- SUBCELLULAR LOCATION: [Isoform 3]: Secreted.
- Connecting piece
- Cytosol
- Mid piece
- Nuclear membrane
- Principal piece
- Vesicles
- PubMed 23529610
- PubMed 25825981
- Tissue specificity (tau)
- 0.80837
- Expression inequality (Gini)
- 0.552748
Expression in transcripts per million
- Thyroid
- 80.12
- Uterus
- 78.64
- Adipose - Visceral (Omentum)
- 73.72
- Lung
- 50.77
- Breast - Mammary Tissue
- 47.42
Expression in transcripts per million
- Thyroid80.12
- Uterus78.64
- Adipose - Visceral (Omentum)73.72
- Lung50.77
- Breast - Mammary Tissue47.42
- Adipose - Subcutaneous44.87
- Fallopian Tube40.76
- Nerve - Tibial36.29
- Cervix - Endocervix34.27
- Cervix - Ectocervix25.65
- Prostate23.22
- Esophagus - Muscularis21.34
- Pituitary20.56
- Artery - Coronary19.33
- Esophagus - Gastroesophageal Junction18.06
- Bladder18.06
- Artery - Tibial17.64
- Kidney - Cortex16.48
- Adrenal Gland16.06
- Vagina15.29
- Kidney - Medulla12.92
- Heart - Atrial Appendage11.76
- Small Intestine - Terminal Ileum11.26
- Stomach11.18
- Heart - Left Ventricle10.83
And 29 more, listed on the interactive page.
- GO:0001525
- GO:0001569
- GO:0001934
- GO:0001938
- GO:0007169
- GO:0008284
- GO:0008360
- GO:0010595
- GO:0010629
- GO:0016239
- GO:0018108
- GO:0030335
- GO:0035924
- GO:0036324
- GO:0038084
- GO:0043410
- GO:0043536
- GO:0045766
- GO:0046777
- GO:0048010
- GO:0050927
- GO:0051894
- GO:0051897
- GO:0051901
- GO:0061042
And 7 more, listed on the interactive page.
- GO:0005768
- GO:0005783
- GO:0005794
- GO:0005829
- GO:0005886
- GO:0031965
- GO:0045121
- GO:0004713
- GO:0004714
- GO:0005021
- GO:0005178
- GO:0005515
- GO:0019838
- GO:0038085
- GO:0042802
- GO:0045296
- GO:0051879
decreased appetite
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CNS
PubMed 38773351myocardial hypoperfusion
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351Increased, Developmental Defects
Effects
- Inhibition/Decrease/Downregulation
Studies
- cell-based
Evidence sourcerash
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- skin
PubMed 38773351haemorrhage
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351aneurysm
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351heart disease
Studies
- preclinical: Highly important for the heart and vasculature based on findings in genetically modified or kinase-inhibitor-treated mice. Role of kinase in heart/vasculature: Crucial in angiogenesis and the heart’s response to pressure overload; antihypertensive effects
Biological samples
- cardiovascular system
PubMed 21283106nausea
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
PubMed 38773351vomiting
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- GI
PubMed 38773351fatigue
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
PubMed 38773351proteinuria
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- renal
PubMed 38773351Hypertension
Effects
- Inhibition/Decrease/Downregulation
Studies
- clinical
Biological samples
- CV
PubMed 38773351
regulation of catalytic activity
- biochemical: NVS_ENZ_hVEGFR2, is one of one assay component(s) measured or calculated from the NVS_ENZ_hVEGFR2 assay. It is designed to make measurements of enzyme activity, a form of enzyme reporter, as detected with fluorescence intensity signals by Fluorescence and electrophoretic mobility shift technology.
- biochemical: NVS_ENZ_hVEGFR2, is one of one assay component(s) measured or calculated from the NVS_ENZ_hVEGFR2 assay. It is designed to make measurements of enzyme activity, a form of enzyme reporter, as detected with fluorescence intensity signals by Fluorescence and electrophoretic mobility shift technology.
Biological samples
- cell-free
Evidence source
Related records
Trials (4,768)
- - IKF/AIO-QUINTIS - Evaluating Fruquintinib in Combination With Tislelizumab in Microsatellite Stable / Proficient Mismatch Repair (MSS/pMMR) Metastatic Colorectal Cancer Without Active Liver Metastases
- : A Phase Ib/II Study To Evaluate Fruquintinib Monotherapy Or Plus Sintilimab In Advanced Solid Tumors
- "Thymalfasin Immunotherapy Study with Triple Regimen in Advanced MSS/pMMR Colorectal Cancer"
- (Peak) A Phase 3 Randomized Trial of CGT9486+Sunitinib vs. Sunitinib in Subjects With Gastrointestinal Stromal Tumors
- (VOYAGER) Study of Avapritinib vs Regorafenib in Patients With Locally Advanced Unresectable or Metastatic GIST
- [18F]FLT-PET as a Predictive Imaging Biomaker of Treatment Responses to Regorafenib
- [18F]Fluciclatide-PET, Pazopanib and Paclitaxel in Ovarian Cancer
- [18F]Fluoroestradiol-PET/CT Companion Imaging Study to the FORESEE Trial
- [18F]Fluoroestradiol-PET/CT Imaging of Invasive Lobular Carcinoma
- [68 Ga]-DOTANOC PET/CT in GEP-NETs
- [68Ga]Ga-FAPI-46 in Staging of Head and Neck Carcinomas
- [68Ga]Ga-PentixaFor PET/CT in Acute Myocardial Inflammation
- 11C-methionine in Diagnostics and Management of Glioblastoma Multiforme Patients (GlioMET)
- 12 Week Patient Study in Neovascular Age-related Macular Degeneration (AMD)
- 17-AAG and Sorafenib in Treating Patients With Unresectable or Metastatic Solid Tumors
- 18F-DCFBC PET/CT in Prostate Cancer
- 18F-DCFPyL Positron Emission Tomography (PET)/Computed Tomography (CT) in Men With Prostate Cancer
- 1st or 2nd Line MBC (Metastatic Breast Cancer) With Previous Avastin (Bevacizumab) Therapy
- 1st-line Activity of Dovitinib and Correlation With Genetic Changes in RCC
- 4SC-201 (Resminostat) and Sorafenib in Advanced Hepatocellular Carcinoma
Drugs (83)
- 4SC-203 Vascular endothelial growth factor receptor inhibitor
- AEE-788 Vascular endothelial growth factor receptor 2 inhibitor
- AG-13958 Vascular endothelial growth factor receptor inhibitor
- Alacizumab pegol Vascular endothelial growth factor receptor 2 antagonist
- Altiratinib Vascular endothelial growth factor receptor 2 inhibitor
- Axitinib Vascular endothelial growth factor receptor inhibitor
- BFH-772 Vascular endothelial growth factor receptor 2 inhibitor
- BMS-690514 Vascular endothelial growth factor receptor inhibitor
- BMS-794833 Vascular endothelial growth factor receptor 2 inhibitor
- BMS-817378 Vascular endothelial growth factor receptor 2 inhibitor
- Brivanib Vascular endothelial growth factor receptor inhibitor
- Brivanib alaninate Vascular endothelial growth factor receptor inhibitor
- Cabozantinib Vascular endothelial growth factor receptor 2 inhibitor
- Cabozantinib S-malate Vascular endothelial growth factor receptor 2 inhibitor
- Catequentinib Vascular endothelial growth factor receptor 2 inhibitor
- Cediranib Vascular endothelial growth factor receptor inhibitor
- CEP-11981 Vascular endothelial growth factor receptor inhibitor
- CEP-5214 Vascular endothelial growth factor receptor inhibitor
- CEP-7055 Vascular endothelial growth factor receptor inhibitor
- CM-082 Vascular endothelial growth factor receptor 2 inhibitor