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 (30)
Related Products (30)
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Recombinant Proteins (5)
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Cilengitide
0 ImagesSynonyms: EMD 121974Cilengitide (EMD 121974) is a BBB-permeable integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.
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Cyclo(Arg-Gly-Asp-D-Phe-Cys)
0 ImagesSynonyms: Cyclo(RGDfC)Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has high affinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors.
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ATN-161
0 ImagesATN-161 is an antagonist of α5β1 integrin and αvβ3 integrin, as well as an inhibitor of fibrosis, an inhibitor of oxidative stress, a tight junction stabilizer, a mitochondrial integrity protector, an angiogenesis inhibitor and an antiviral agent. ATN-161 inhibits NLRP3, MAPK, and ROS. ATN-161 protects mice from SARS-CoV-2 infection. ATN-161 reduces infarct volume, alleviates edema, decreases immune cell infiltration, reduces the area of choroidal neovascularization lesions, lowers tumor microvessel density and viral load. ATN-161 can be used in research related to ischemic stroke, choroidal neovascularization, breast cancer, coronavirus disease 2019 (COVID-19), and liver metastasis of colorectal cancer.
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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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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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3P-RGD2
0 ImagesCat. No.: HY-P11773CAS No.: 1094848-94-8
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SB-273005
0 ImagesSB-273005 is an orally active non-peptide αvβ3 integrin antagonist with Ki values of 1.2 nM and 0.3 nM for αvβ3 and αvβ5, respectively. SB-273005 blocks the binding of integrins to the RGD sequence in the extracellular matrix. SB-273005 inhibits Rictor phosphorylation and reduces IL-10 secretion. SB-273005 inhibits inflammation, prevents bone loss, regulates vascular smooth muscle function, and reverses pregnancy-induced immune deviation. SB-273005 can be used in the study of rheumatoid arthritis, osteoporosis, and aneurysms. .
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GSK 3008348
0 ImagesGSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer.
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GSK 3008348 hydrochloride
0 ImagesGSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer.
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DSPE-PEG2000-iRGD
0 ImagesCat. No.: HY-172494DSPE-PEG2000-iRGD is a PEG compound which composed of DSPE and an αv-integrins targeting peptide (iRGD). iRGD peptide binds to αv-integrins, and then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties. DSPE-PEG2000-iRGD can be used for agent delivery.
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FZ1 peptide
0 ImagesCat. No.: HY-P11474Purity: 99.92%FZ1 peptide is a cyclic heptapeptide and also an integrin αvβ3 agonist. FZ1 peptide activates the FAK/PI3K-AKT/ERK pathway and upregulates VEGFC to promote angiogenesis. FZ1 peptide exhibits antibacterial activity in extracts of HA-c-FZ1 hydrogel; it inhibits LPS-induced proinflammatory cytokine secretion in RAW264.7 macrophages; it reduces H2O2-induced ROS levels; it increases the healing rate of scratch wounds. FZ1 peptide can be used in studies related to diabetic skin wounds.
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Echistatin
0 ImagesCat. No.: HY-P1189CAS No.: 154303-05-6Echistatin is a naturally derived RGD-containing snake venom peptide. Echistatin exhibits an IC50 of 0.6 nM against mouse αvβ3 integrin, and acts as an antagonist against αvβ3, αIIbβ3, α5β1 integrins, pp125FAK and paxillin. Echistatin reduces the phosphorylation of pp125FAK and paxillin, inhibits the autophosphorylation and kinase activity of pp125FAK, and weakens its binding to pp60src and paxillin. Echistatin disrupts the actin cytoskeleton and focal adhesions, induces melanoma cell detachment from fibronectin, and regulates cell adhesion and motility. Echistatin inhibits osteoclast maturation and migration, bone resorption, platelet aggregation, bone loss, as well as adhesion and metastasis of Lewis lung cancer cells; it also increases the number of osteoclasts and bone coverage area in mice with secondary hyperparathyroidism. Echistatin can be used in research related to melanoma, lung cancer and secondary hyperparathyroidism.
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Echistatin TFA
0 ImagesCat. No.: HY-P1189APurity: 99.32%Echistatin TFA is a naturally derived RGD-containing snake venom peptide. Echistatin TFA exhibits an IC50 of 0.6 nM against mouse αvβ3 integrin, and acts as an antagonist against αvβ3, αIIbβ3, α5β1 integrins, pp125FAK and paxillin. Echistatin TFA reduces the phosphorylation of pp125FAK and paxillin, inhibits the autophosphorylation and kinase activity of pp125FAK, and weakens its binding to pp60src and paxillin. Echistatin TFA disrupts the actin cytoskeleton and focal adhesions, induces melanoma cell detachment from fibronectin, and regulates cell adhesion and motility. Echistatin TFA inhibits osteoclast maturation and migration, bone resorption, platelet aggregation, bone loss, as well as adhesion and metastasis of Lewis lung cancer cells; it also increases the number of osteoclasts and bone coverage area in mice with secondary hyperparathyroidism. Echistatin TFA can be used in research related to melanoma, lung cancer and secondary hyperparathyroidism.
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