αvβ3
Integrin αvβ3 is a heterodimeric receptor that mediates cell adhesion to extracellular matrix (ECM) proteins, primarily vitronectin, and regulates angiogenesis and tumor cell survival[1]. Mechanistically, αvβ3 interacts with intracellular signaling pathways including FAK/ERK to promote osteogenesis and endothelial migration, making it a pivotal regulator of tissue remodeling and pathological angiogenesis[2]. In disease models, αvβ3 expression is elevated in neuroendocrine prostate cancer, medulloblastoma, glioblastoma, and ovarian carcinoma, correlating with tumor aggressiveness, metastatic potential, and radioresistance[3][4][5][6]. Compared with related αv integrins such as αvβ5 and αvβ6, αvβ3 exhibits higher expression in tumor-associated vasculature and metastatic tumor cells, and it mediates platelet-assisted extravasation during hematogenous metastasis[7][1]. In experimental applications, selective αvβ3 inhibitors and agonists, including cyclic RGD peptides and fluorescent or radiolabeled RGD-based ligands, have been used to modulate angiogenesis, visualize tumors via PET/SPECT imaging, and inhibit ectopic ossification or tumor progression in preclinical models[2][5][6][8]. The combination of αvβ3-targeted imaging and pharmacologic blockade provides a dual platform for both mechanistic studies and potential therapeutic intervention in oncology and vascular disease research[5][8].
References:
- [1]. Welser-Alves JV, et al. Microglia use multiple mechanisms to mediate interactions with vitronectin; non-essential roles for the highly-expressed αvβ3 and αvβ5 integrins. J Neuroinflammation. 2011 Nov 10;8:157. [Content Brief]
- [2]. Böger C, et al. Integrins αvβ3 and αvβ5 as prognostic, diagnostic, and therapeutic targets in gastric cancer. Gastric Cancer. 2015 Oct;18(4):784-95. [Content Brief]
- [3]. Quaglia F, et al. Differential expression of αVβ3 and αVβ6 integrins in prostate cancer progression. PLoS One. 2021 Jan 22;16(1):e0244985. [Content Brief]
- [4]. Schittenhelm J, et al. Longitudinal expression analysis of αv integrins in human gliomas reveals upregulation of integrin αvβ3 as a negative prognostic factor. J Neuropathol Exp Neurol. 2013 Mar;72(3):194-210. [Content Brief]
- [5]. Geng X, et al. Integrin αVβ3 antagonist-c(RGDyk) peptide attenuates the progression of ossification of the posterior longitudinal ligament by inhibiting osteogenesis and angiogenesis. Mol Med. 2024 May 2;30(1):57. [Content Brief]
- [6]. Echavidre W, et al. Integrin-αvβ3 is a Therapeutically Targetable Fundamental Factor in Medulloblastoma Tumorigenicity and Radioresistance. Cancer Res Commun. 2023 Dec 7;3(12):2483-2496. [Content Brief]
- [7]. Weber MR, et al. Activated tumor cell integrin αvβ3 cooperates with platelets to promote extravasation and metastasis from the blood stream. Thromb Res. 2016;140 Suppl 1:S27-S36. [Content Brief]
- [8]. Shaw SK, et al. High expression of integrin αvβ3 enables uptake of targeted fluorescent probes into ovarian cancer cells and tumors. Bioorg Med Chem. 2018 May 1;26(8):2085-2091. [Content Brief]
- [9]. Dal Corso A, et al. αvβ3 Integrin-Targeted Peptide/Peptidomimetic-Drug Conjugates: In-Depth Analysis of the Linker Technology. Curr Top Med Chem. 2016;16(3):314-29. [Content Brief]
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αvβ3 Related Products (35)
Related Products (35)
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Recombinant Proteins (5)
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Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA
0 ImagesCat. No.: HY-P2300APurity: 98.69%Synonyms: Cyclo(RGDfC) TFACyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) TFA, a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA can be used in the research of tumors.
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Cyclo(Arg-Gly-Asp-(D-Phe)-Glu)
0 ImagesSynonyms: c(RGDfE)Cyclo(Arg-Gly-Asp-(D-Phe)-Glu) c(RGDfE) is a cyclic RGD peptide targeting integrin αvβ3. Cyclo(Arg-Gly-Asp-(D-Phe)-Glu) is commonly used for modifying drug loaded nanoparticles. Cyclo(Arg-Gly-Asp-(D-Phe)-Glu) is often used in cancer research, such as pancreatic cancer.
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C16Y
0 ImagesCat. No.: HY-P10704CAS No.: 640756-12-3C16Y is a short peptide and an inhibitor of integrins αvβ3 and α5β1. C16Y acts on the cell membrane and exerts its anticancer activity by inhibiting angiogenesis .
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KAFDITYVRLKF
0 ImagesCat. No.: HY-P11780CAS No.: 208116-26-1KAFDITYVRLKF is a selective, competitive integrin αvβ3 binder. KAFDITYVRLKF induces the production of MMP-9. KAFDITYVRLKF blocks monocyte migration, promotes melanoma cell migration, protects neurons, and improves motor and cognitive functions. KAFDITYVRLKF can be used in research related to melanoma and Parkinson's disease.
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PAI-1
0 ImagesCat. No.: HY-P11413CAS No.: 139446-70-1PAI-1 is a serine protease inhibitor (SERPIN). PAI-1 binds to and irreversibly inhibits uPA, tPA and furin; it also interacts with vitronectin, α1-acid glycoprotein, CRT, TLR4, proteasome α-3 subunit, uPAR, LRP1, Integrin αvβ3 and thrombin. PAI-1 regulates fibrinolysis, extracellular matrix turnover, cell migration, angiogenesis, inflammatory response and tissue remodeling; it mediates epithelial-mesenchymal transition (EMT)/endothelial-mesenchymal transition (EndMT), apoptosis and thrombus stabilization. PAI-1 can be used in research related to sepsis, acute lung injury, cardiovascular diseases, tissue fibrosis, diabetic nephropathy, obstructive nephropathy and non-insulin-dependent diabetes mellitus.
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Nesvategrast
0 ImagesCat. No.: HY-117133CAS No.: 1621332-91-9Synonyms: SF0166Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model.
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α5β1 integrin-IN-1
0 ImagesCat. No.: HY-180057CAS No.: 2649899-08-9α5β1 integrin-IN-1 is a potent and selective α5β1 integrin inhibitor with an IC50 value of approximately 0.4 nM (pIC50 = 9.4 M). α5β1 integrin-IN-1 disrupts the interaction between α5β1 integrin and fibronectin, thereby blocking smooth muscle tension transmission and α5β1 integrin-mediated cell adhesion. α5β1 integrin-IN-1 can be used in the research of asthma and allergic asthma.
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SU015
0 ImagesCat. No.: HY-P3335CAS No.: 250612-06-7Synonyms: DOTA-RGDfK dimerSU015 (DOTA-RGDfK dimer) is a Integrin αvβ5 and αvβ3 antagonist. SU015 exhibits comparable affinity for αvβ5 and αvβ3, with relatively higher potency and specificity compared to other integrins. SU015 inhibits αvβ3-mediated cell adhesion to fibrinogen, αvβ3-mediated adhesion of activated platelets to osteopontin, and αvβ5-mediated cell adhesion to vitronectin. SU015 shows potent inhibitory effects on FGF2-induced angiogenesis in the CAM model. SU015 carries a linker arm available for radioisotope conjugation, and acts as a target-specific radioreagent when labeled with 90Y (i.e., RP697) or 177Lu (i.e., RP688). SU015 can be used in studies related to tumor metastasis and tumors.
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αvβ5 integrin-IN-3
0 ImagesCat. No.: HY-189093CAS No.: 2226557-15-7αvβ5 integrin-IN-3 is an orally active, selective αVβ5 integrin inhibitor with an IC50 value of 0.61 nM. αvβ5 integrin-IN-3 inhibits αVβ1, αVβ3 and αVβ6 integrins with IC50 values of 21 nM, 5.5 nM and 18 nM, respectively. αvβ5 integrin-IN-3 reduces total Collagen content in a mouse unilateral ureteral obstruction model. αvβ5 integrin-IN-3 can be used for the research of renal fibrosis.
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3P-RGD2
0 ImagesCat. No.: HY-P11773CAS No.: 1094848-94-8
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c-RGD-SH
0 ImagesCat. No.: HY-P11339CAS No.: 841255-57-0
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T7 Peptide
0 ImagesCat. No.: HY-P10323Synonyms: Tumstatin (74-98), humanT7 Peptide is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma.
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Cilengitide hydrochloride
0 ImagesCat. No.: HY-16142CAS No.: 188969-00-8Synonyms: EMD 121974 hydrochlorideCilengitide hydrochloride (EMD 121974 hydrochloride) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC50 values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide hydrochloride inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide hydrochloride inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide hydrochloride can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors.
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