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BIOMARKER:

KDR overexpression

i
Other names: KDR, CD309, FLK1, VEGFR, VEGFR2, Kinase insert domain receptor (a type III receptor tyrosine kinase)
Entrez ID:
Related biomarkers:
1m
Apatinib has anti-tumor effects and induces autophagy in lung cancer cells with high expression of VEGFR-2. (PubMed, Iran J Basic Med Sci)
Immunohistochemistry showed that combining apatinib with chloroquine could reduce the expression of CD31 and Ki67 and increase the expression of caspase-3. Apatinib inhibits proliferation and induces apoptosis in H1975 and H1446 lung cancer cells with high VEGFR2 expression and autophagy in H1975 and H446 cells.
Journal • PARP Biomarker
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KDR (Kinase insert domain receptor) • CASP3 (Caspase 3) • CD31 (Platelet and endothelial cell adhesion molecule 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1)
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KDR overexpression • KDR expression • CD31 expression • VEGFA expression
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AiTan (rivoceranib) • chloroquine phosphate
1m
The expression level of VEGFR2 regulates mechanotransduction, tumor growth and metastasis of high grade serous ovarian cancer cells. (PubMed, Eur J Cell Biol)
This is translated into a reduced FAK activity at FAs, ECM-dependent alterations of mechanical forces through FAs and YAP nuclear translocation. Together, the data show that low expression, silencing or inhibition of VEGFR2 in HGSOC cells alter mechanotransduction and lead to the acquisition of a pro-proliferative/invasive phenotype which explains the need for a more cautious use of anti-VEGFR2 drugs in ovarian cancer.
Journal
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KDR (Kinase insert domain receptor)
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KDR overexpression • KDR expression
9ms
The inhibitory effect of apatinib on different small cell lung cancer cells and in lung cancer-bearing mice and patients. (PubMed, Clin Respir J)
Apatinib has a significant inhibitory effect on small cell lung cancer with high expression of VEGFR2 and may be a treatment for small cell lung cancer patients.
Preclinical • Journal
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KDR (Kinase insert domain receptor)
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KDR overexpression • KDR expression
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AiTan (rivoceranib)
10ms
Development of novel indazolyl-acyl hydrazones as antioxidant and anticancer agent that target VEGFR-2 in human breast cancer cells. (PubMed, Chem Biodivers)
In silico docking study revealed the favorable binding energies of -7.30 kcal/mol and -8.04 kcal/mol for compounds towards Vascular Endothelial Growth Factor Recaptor-2 (VEGFR-2), respectively. In conclusion, we have synthesized antioxidant and anticancer agents that target VEGFR-2 in breast cancer cells.
Journal
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KDR (Kinase insert domain receptor)
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KDR overexpression • KDR expression
1year
Clinicopathological impact of VEGFR2 and VEGF-C in patients with EGFR-major mutant NSCLC receiving osimertinib. (PubMed, Thorac Cancer)
VEGFR2 and VEGF-C are highly expressed in EGFR-mutant NSCLC cells. Increased expression of VEGFR2 was identified as a significant prognostic factor in patients with EGFR del19 mutation who received osimertinib, whereas co-high expression of VEGFR2 and VEGF-C was a significant predictor for those with EGFR L858R mutation.
Journal
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EGFR (Epidermal growth factor receptor) • KDR (Kinase insert domain receptor) • VEGFC (Vascular Endothelial Growth Factor C)
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EGFR mutation • EGFR L858R • EGFR expression • EGFR overexpression • KDR overexpression • KDR expression • VEGFA expression
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Tagrisso (osimertinib)
1year
Discovery of indolinone-bearing benzenesulfonamides as new dual carbonic anhydrase and VEGFR-2 inhibitors possessing anticancer and pro-apoptotic properties. (PubMed, Eur J Med Chem)
The most effective and selective hCA IX and XII inhibitors 8g, 8j and 15b were chosen to be tested for their in vitro inhibitory impact against VEGFR-2 as well as their antiproliferative impact against VEGFR-2 overexpressing MDA-MB-231 and MCF-7 breast cancer cells. Furthermore, molecular docking studies were conducted within the hCA IX, XII, and VEGFR-2 active sites to explain the observed inhibitory results.
Journal
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KDR (Kinase insert domain receptor)
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KDR overexpression • KDR expression
over1year
VEGFR2 and CD34 expression associated with longer survival in patients with pleural mesothelioma in the IFCT-GFPC-0701 MAPS phase 3 trial. (PubMed, Lung Cancer)
VEGFR2 overexpression independently correlated with longer OS or PFS in PM patients, such biomarker deserving prospective evaluation as stratification variable in future clinical trials.
P3 data • Journal
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KDR (Kinase insert domain receptor) • CD34 (CD34 molecule)
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KDR overexpression • KDR expression
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Avastin (bevacizumab) • cisplatin • pemetrexed
over1year
Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • KDR (Kinase insert domain receptor) • IFNG (Interferon, gamma) • TNFA (Tumor Necrosis Factor-Alpha) • CD4 (CD4 Molecule) • GZMB (Granzyme B)
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PD-L1 expression • PD-L1 overexpression • KDR overexpression • KDR expression
over1year
Immunohistochemical analysis of expression of VEGFR2, KIT, PDGFR-β, and CDK4 in canine urothelial carcinoma. (PubMed, J Vet Diagn Invest)
The intense staining of VEGFR2 in UC cells suggested that VEGFR2 may be of prognostic and/or therapeutic value in dogs with UC. Overexpression of VEGFR2 in UC cells validates this receptor as a treatment target in UC.
Journal
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FLT3 (Fms-related tyrosine kinase 3) • KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • KDR (Kinase insert domain receptor) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • CDK4 (Cyclin-dependent kinase 4)
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KDR overexpression • KDR expression
almost2years
Managing MMP-2, MMP-9, VEGFR-2, TGFβ-1, and TIMP-1 in NNK-induced lung carcinoma by nonchemical interventions in female rats. (PubMed, Toxicol Rep)
TGFβ-1 ratio significantly increased following preformed interventions in non-pathologic groups: E (P ≤ 0.001) and NS+E (P ≤ 0.01). IHC and gene assays indicate a favorable and acceptable effect of the designed training protocol besides the treatment with N.sativa nano-drug, by which cancer development could be restricted through recovering the natural balance of angiogenic and angiostatic markers.
Preclinical • Journal
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KDR (Kinase insert domain receptor) • MMP2 (Matrix metallopeptidase 2) • TIMP1 (Tissue inhibitor of metalloproteinases 1) • TGFB1 (Transforming Growth Factor Beta 1) • MMP9 (Matrix metallopeptidase 9)
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KDR overexpression • KDR expression
almost2years
Functional Characterization and Development of Novel Human Kinase Insert Domain Receptor Chimeric Antigen Receptor T-cells for Immunotherapy of Non-Small Cell Lung Cancer. (PubMed, Eur J Pharm Sci)
We evaluated this using both in vitro and in vivo experiments. The KDR-CAR-T cells targeted and killed KDR-A549 with high efficiency by expressing IFN-γ and releasing granzyme B. The in vivo study showed that KDR-CAR-T cells dramatically inhibited the growth of lung cancer KDR-A549 xenografts in BALB/c-nu mice at day 10. The characterization of T cells modified by KDR-CAR by computational biology and wet-lab experiments suggested its applicability as a new treatment strategy for lung cancer and, potentially, for other vascularized solid tumors.
Journal • CAR T-Cell Therapy
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KDR (Kinase insert domain receptor) • IFNG (Interferon, gamma) • GZMB (Granzyme B)
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KDR overexpression • IFNG expression
2years
CML-074 Pathogenesis of Tyrosine Kinase Inhibitor-Associated Vascular Toxicity in Chronic Myeloid Leukemia. (PubMed, Clin Lymphoma Myeloma Leuk)
An increase in VAEs has been documented with ponatinib, nilotinib, and dasatinib but not with imatinib and bosutinib. However, the in-vivo effect of these TKIs on endothelial pathogenesis requires further investigation. Understanding TKI-induced VAE pathogenesis could contribute to the future development of safer next-generation TKIs and could potentially influence TKI-personalized tailoring for CML patients.
Journal
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KDR (Kinase insert domain receptor)
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KDR overexpression • KDR expression
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dasatinib • imatinib • Iclusig (ponatinib) • Tasigna (nilotinib) • Bosulif (bosutinib)
2years
Oral DNA vaccination targeting VEGFR2 combined with the anti-PD-L1 antibody avelumab in patients with progressive glioblastoma - final results. NCT03750071 (EANO 2022)
VXM01 in combination with avelumab was safe and produced detectable peripheral VEGFR-2-specific immune responses. Three non-resected patients had an objective response, three more patients experienced best response stable disease. For future studies a patient enrichment strategy based on immune biomarkers might be envisaged.
Clinical • PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • KDR (Kinase insert domain receptor)
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KDR overexpression • KDR expression
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Bavencio (avelumab) • VXM01
2years
DISSECTING THE DIRECT IMMUNOMODULATORY POTENTIAL OF VEGF AND PD-1 BLOCKADE IN BLOOD AND TISSUE (ILCA 2022)
We show that several key immune subsets express VEGFR2, with compensatory changes following VEGF blockade and enrichment within the tissue, highlighting the need to study the direct immunomodulatory role of anti-angiogenic agents in HCC. The expression of PDL1 on CD8 T cells also merits further investigation since this can autoregulate responses through reverse signalling as well as suppressing neighbouring T cells. Access to liver tissue using minimally invasive approaches and specimens from neoadjuvant studies is essential to further our understanding of highly compartmentalised immune responses, including the potential for rescue of exhausted intrahepatic VEGFR2+ and PDL1+ CD8 T cells in HCC.
PD(L)-1 Biomarker • IO biomarker
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CD8 (cluster of differentiation 8) • KDR (Kinase insert domain receptor) • LAG3 (Lymphocyte Activating 3) • HAVCR2 (Hepatitis A Virus Cellular Receptor 2) • TIGIT (T Cell Immunoreceptor With Ig And ITIM Domains 2)
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PD-L1 expression • KDR overexpression • CD8 expression • LAG3 expression • HAVCR2 expression • KDR expression
over2years
ACSL4 promotes colorectal cancer and is a potential therapeutic target of emodin. (PubMed, Phytomedicine)
Our findings indicate that emodin inhibits proliferation and invasion of CRC cells and reduces VEGF secretion and VEGFR1 and VEGFR2 expression by inhibiting ACSL4. This emodin-induced pathway offers insights into the molecular mechanism of its antitumor effect and provides a potential therapeutic strategy for CRC.
Journal
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FLT1 (Fms-related tyrosine kinase 1) • ACSL4 (Acyl-CoA Synthetase Long Chain Family Member 4)
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KDR overexpression • KDR expression • ACSL4 overexpression • VEGFA expression • FLT1 expression
over2years
Production and Conjugation of Truncated Recombinant Diphtheria Toxin to VEGFR-2 Specific Nanobody and Evaluation of its Cytotoxic Effect on PC-3 Cell Line. (PubMed, Mol Biotechnol)
Cytotoxicity of immunotoxin was evaluated on the VEGFR-2 positive PC-3 cell line by MTT assay. Overexpression of VEGFR-2 in the PC-3 cell line allowed immunotoxin to recognize them by anti-VEGFR-2 nanobodies. The concentrations above 5 μg/ml represented a significant decrease in cell survival rate in PC-3 cells compared to HEK293 cells (VEGFR-2 negative cells) as controls.VGRNb-DT demonstrated a successful bioconjugation; furthermore, variable concentrations were correlated with cell death in prostate cancer PC-3 cells.
Preclinical • Journal
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KDR (Kinase insert domain receptor)
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KDR overexpression • KDR expression
over2years
Significance of HER2 and VEGFR2 in Early-stage Endometrial Cancer. (PubMed, In Vivo)
The association of VEGFR2 and HER2 expression in early EC was elucidated. This study shows that the measurement of VEGFR2 expression may be useful in the preoperative assessment of EC and suggests the possibility of anti-HER2 therapy for EC.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • KDR (Kinase insert domain receptor)
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HER-2 expression • KDR overexpression • KDR expression
over2years
Apatinib inhibits paclitaxel resistance of gastric carcinoma cells through VEGFR2 pathway. (PubMed, Am J Transl Res)
Overexpression of VEGFR2 can offset the rescue effect of Apa on PTX-induced drug resistance of MGC803 cells. Taken together, Apa may inhibit PTX resistance of MGC803 cells via the VEGFR2 signaling pathway.
Journal • IO biomarker
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BCL2 (B-cell CLL/lymphoma 2) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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KDR overexpression • KDR expression
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paclitaxel • AiTan (rivoceranib)
almost3years
Clinical Significance of Major Angiogenesis-Related Effectors in Patients with Metastatic Breast Cancer Treated with Trastuzumab-based Regimens. (PubMed, Cancer Res Treat)
A trend towards longer progression free survival (PFS) was detected univariately for patients with HER2-negative tumors and high expression of VEGFR2, (HR=0.60, p=0.059). VEGFR1 and VEGFR2 seem to have significant prognostic value in BC patients with metastatic disease treated with trastuzumab-based regimens.
Clinical • Journal
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HER-2 (Human epidermal growth factor receptor 2) • KDR (Kinase insert domain receptor) • FLT1 (Fms-related tyrosine kinase 1) • FLT4 (Fms-related tyrosine kinase 4) • VEGFC (Vascular Endothelial Growth Factor C)
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HER-2 positive • HER-2 negative • KDR overexpression • KDR expression • VEGFA expression • FLT1 expression • VEGFA expression + FLT1 expression + KDR expression
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Herceptin (trastuzumab) • trastuzumab biosimilar
3years
Pharmacophore based drug design and synthesis of oxindole bearing hybrid as anticancer agents. (PubMed, Bioorg Chem)
5b not only suppressed tumor growth but also improved vandetanib associated with weight loss toxicity. Moreover, 5b was found safer than sunitinib and erlotinib with LD of 500 mg/kg body weight. These results propose 5b as potential anti-tumor drug with safer profile of conventional inhibitors of VEGFR-2 and EGFR for solid tumors.
Journal
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EGFR (Epidermal growth factor receptor) • MMP9 (Matrix metallopeptidase 9)
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EGFR expression • EGFR overexpression • KDR overexpression • KDR expression
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erlotinib • sunitinib • Caprelsa (vandetanib)
3years
Comprehensive expressional analysis of chemosensitivity-related markers in large cell neuroendocrine carcinoma of the lung. (PubMed, Thorac Cancer)
These findings suggest that elevated Topo-II and TS expression may contribute to poor outcomes through protumoral biology in patients with LCNEC, and elevated VEGFR2 expression might negatively impact tumor immune reactions in LCNEC.
Journal • PD(L)-1 Biomarker • IO biomarker
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PD-L1 (Programmed death ligand 1) • KDR (Kinase insert domain receptor) • TUBB3 (Tubulin beta 3 class III) • TYMS (Thymidylate Synthetase)
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PD-L1 expression • PD-L1 negative • KDR overexpression • KDR expression • TOP2A expression
over3years
Apatinib suppresses the migration, invasion and angiogenesis of hepatocellular carcinoma cells by blocking VEGF and PI3K/AKT signaling pathways. (PubMed, Mol Med Rep)
These effects were associated with the downregulation of VEGF and VEGFR2 and suppression of the PI3K/AKT signaling pathway. Thus, apatinib inhibited cell migration, invasion and angiogenesis by blocking the VEGF and PI3K/AKT pathways, supporting an effective therapeutic strategy in the treatment of HCC.
Journal
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KDR (Kinase insert domain receptor) • CDH1 (Cadherin 1) • VIM (Vimentin)
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KDR overexpression • KDR expression • CDH1 expression • VIM expression
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AiTan (rivoceranib)
over3years
The role of c-Met and VEGFR2 in glioblastoma resistance to bevacizumab. (PubMed, Sci Rep)
Immunohistochemical expression of c-Met, HGF, VEGFR2, and MVD was assessed in tumor specimens of GBM patients treated with bevacizumab, after progression under temozolomide. Concomitant c-Met/VEGFR2 overexpression was associated with worse overall survival (13 months) compared with concomitant c-Met/VEGFR2 negative expression (19 months; p = 0.025). Our data support the hypothesis that c-Met and VEGFR2 overexpression have a role in the development of glioblastoma early resistance and might predict poorer responses to anti-angiogenic therapies.
Journal
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MET (MET proto-oncogene, receptor tyrosine kinase) • KDR (Kinase insert domain receptor)
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MET overexpression • MET expression • KDR overexpression • KDR expression
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Avastin (bevacizumab) • temozolomide
almost4years
Expression of growth factors and their receptors in the primary renal cell carcinoma: new data and review. (PubMed, Cent European J Urol)
In a univariate analysis overexpression of VEGFR2 (p <0.0001) and FGFR2 (p = 0.014) had negative influence on cancer-specific survival. Expression of growth factors and tyrosine kinase receptors in the primary tumor cells is strongly interconnected and associated with unfavorable features of RCC.
Review • Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1) • KDR (Kinase insert domain receptor) • PDGFRB (Platelet Derived Growth Factor Receptor Beta) • FLT1 (Fms-related tyrosine kinase 1)
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KDR overexpression • KDR expression • FGFR2b expression • VEGFA expression
almost4years
Anlotinib as a promising inhibitor on tumor growth of oral squamous cell carcinoma through cell apoptosis and mitotic catastrophe. (PubMed, Cancer Cell Int)
Anlotinib could exert an antitumor effect on oral cancer cell lines via apoptotic pathway and mitotic catastrophe pattern, presenting a promising potential therapy for patients with OSCC.
Journal
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KIT (KIT proto-oncogene, receptor tyrosine kinase) • FGFR (Fibroblast Growth Factor Receptor) • KDR (Kinase insert domain receptor)
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EGFR overexpression • KDR overexpression • KDR expression
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Focus V (anlotinib)
over4years
The VEGFR-2 protein and the VEGFR-2 rs1870377 A>T genetic polymorphism are prognostic factors for gastric cancer. (PubMed, Cancer Biol Ther)
Our study suggested that the high expression of VEGFR-2, as well as the VEGFR-2 rs1870377 A > T genetic polymorphism, may be prognostic markers for GC.
Journal
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KDR (Kinase insert domain receptor)
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EGFR overexpression • KDR overexpression • KDR expression