VEGFR Antagonist

Ramucirumab (anti-VEGFR) is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab (anti-VEGFR) is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab (anti-VEGFR) is also an angiogenesis inhibitor.

GNQWFI, an anti-Flt1 peptide, is a VEGFR1-specific antagonist. GNQWFI blocks the interaction of VEGFR1 with various VEGFR1 ligands, such as VEGFA, VEGFB, and placental growth factor (PIGF) and inhibits VEGF-induced endothelial cell migration and tube formation. GNQWFI is promising for research of cancer, asthma, and other ocular diseases.

C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer.

VGB4 is a VEGF-A and VEGF-B antagonist peptide that duplicates two binding domains of VEGF-B (loop 1 and loop3) and are linked together by the receptor-binding domain of VEGF-A (loop3). VGB4 has significant anti-angiogenic and anti-tumor activities and can regulate tumor growth and metastasis through multiple mechanisms. VGB4 could be used in anti-tumor research.

ASKG-712 (AM712) is a recombinant anti-VEGF humanized monoclonal antibody and Ang-2 antagonist peptide fusion protein. ASKG-712 can be used in Wet age-related macular degeneration and Diabetic macular oedema research.

K-106 (KPI-285) is a VEGFR antagonist that also inhibits neurotrophic tyrosine kinase receptors (NTRK). K-106 can be used for retinal research.