Over the past decades, significant progress has been made in profiling the KDR (VEGFR-2) specific intracellular signaling cascades resulting in proliferation, migration, survival and increased permeability, all of which contribute to the angiogenic response. Moreover, therapeutic inhibition of KDR action is now involved in the clinic practice for the novel treatment of various diseases. As an expert in animal model, Creative Biolabs is ready to offer the humanized KDR immune checkpoint knock-in mice and professional technical support for your drug discovery studies.

KDR Immune Checkpoint Pathway

KDR (kinase insert domain receptor) is a type III receptor tyrosine kinase and is alternatively called FLK1 (Fetal Liver Kinase 1), CD309 (cluster of differentiation 309), or VEGFR2 (Vascular endothelial growth factor receptor 2). It functions as a cell-surface receptor for VEGF (vascular endothelial growth factor) and plays a crucial role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Similar to the VEGFR1, KDR is expressed in the vascular endothelium. However, the angiogenic activities of VEGFs are transduced mainly by KDR. It acts as the main mediator of VEGF-induced endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. The binding of KDR to VEGF induces its dimerization and activation, leading to the transduction of signals that influence cellular functions. The signaling and trafficking of KDR are regulated by multiple factors, such as Rab GTPase, integrin alphaVbeta3, P2Y purine nucleotide receptor, T-cell protein tyrosine phosphatase.

Since angiogenesis plays a part in numerous pathological conditions, with KDR signaling involved in both tumor angiogenesis and diabetic retinopathy, the phosphorylation sites of KDR may be useful targets for the development of anti-angiogenic therapies to treat cancer and atherosclerosis.

Function of KDR in Cancer

Angiogenesis is essential for tumor growth and development because cancer cells have a relatively high metabolic need of oxygen and nutrients to keep growing. In addition, the vascular and capillary network allows tumor metastasis and spread to other sites in the body. The expression of VEGF in cancer cells is induced during tumor formation by environmental stimuli such as hypoxia, or by genetic mutations such as K-ras, p53 or HER2/ErbB2. The expression of KDR is reported to be upregulated in the tumor vasculature as compared to normal vasculature. In past years, a theory has been proposed that inhibition of angiogenesis may result in the arrest of tumor growth.

Development of Humanized KDR Immune Checkpoint Knock-In Mice

Anti-angiogenic compounds can be divided into two broad classes: agents designed to target the VEGF ligand and agents that target the cell surface receptor such as KDR. Targeting KDR are supposed to not only restrict tumor vascularisation but also create a more stable and normalized vasculature within the solid tumor, enabling efficient delivery of anti-tumor drugs. Since the autophosphorylation of KDR serves as an essential step in the signal pathway that contributes to angiogenesis, the development of blockades that inhibits this reaction has generated great interest for novel drug development. Scientists in Creative Biolabs has developed a variety of well-characterized Magic™ “humanized” animal models via excellent transgenic method, including humanized KDR knock-in mouse. Our humanized KDR immune checkpoint KI mice are fully validated with treatment data and immunoprofiling, ensuring adequate quality assurance. Please feel free to contact us for more details.

Creative Biolabs also offers other various Humanized Mouse Models you may be interested in:

• Humanized PBL SCID Mice
• Humanized SRC SCID Mice
• Humanized BLT Mice
• Humanized Immune Checkpoint knock-in Mouse Models

For Research Use Only.


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