ArticleThe Biochemical journal2003
The alpha2beta1 integrin inhibitor rhodocetin binds to the A-domain of the integrin alpha2 subunit proximal to the collagen-binding site.
Article in The Biochemical journal, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 70 citations in OpenAlex.
- Promucetin, a new C-type lectin-like protein modulates coagulation by activating platelets via GPIb.The journal of venomous animals and toxins including tropical diseases · 2025Article
- RETRACTED: Structure-Activity Relationship of Synthetic Linear KTS-Peptides Containing Meta-Aminobenzoic Acid as Antagonists of α1β1 Integrin with Anti-Angiogenic and Melanoma Anti-Tumor Activities.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Snake Venom Components as Therapeutic Drugs in Ischemic Heart Disease.Biomolecules · 2023Review
- Sodium Transporters in Human Health and Disease.Frontiers in physiology · 2020Review
- KFrontiers in pharmacology · 2020Article
- Review
- Titration ELISA as a Method to Determine the Dissociation Constant of Receptor Ligand Interaction.Journal of visualized experiments : JoVE · 2018Article
- Dramatic and concerted conformational changes enable rhodocetin to block α2β1 integrin selectively.PLoS biology · 2017Article
- Aggretin Venom Polypeptide as a Novel Anti-angiogenesis Agent by Targeting Integrin alpha2beta1.Scientific reports · 2017Article
- Vipegitide: a folded peptidomimetic partial antagonist of α2β1 integrin with antiplatelet aggregation activity.Drug design, development and therapy · 2015Article
- Identification of inhibitors of α2β1 integrin, members of C-lectin type proteins, in Echis sochureki venom.Toxicology and applied pharmacology · 2013Article
- Extracellular acidic pH inhibits oligodendrocyte precursor viability, migration, and differentiation.PloS one · 2013Article
- Article
- Impairment of the cell-to-matrix adhesion and cytotoxicity induced by the Mediterranean jellyfish Pelagia noctiluca venom and its fractions in cultured glioblastoma cells.Lipids in health and disease · 2012Article
- The glycocalyx maintains a cell surface pH nanoenvironment crucial for integrin-mediated migration of human melanoma cells.Pflugers Archiv : European journal of physiology · 2009Article
- A key role for the integrin alpha2beta1 in experimental and developmental angiogenesis.The American journal of pathology · 2009Article
- Protons make tumor cells move like clockwork.Pflugers Archiv : European journal of physiology · 2009Review
- Small-molecule inhibitors of integrin alpha2beta1 that prevent pathological thrombus formation via an allosteric mechanism.Proceedings of the National Academy of Sciences of the United States of America · 2009Article
- Inhibition of lung tumor colonization and cell migration with the disintegrin crotatroxin 2 isolated from the venom of Crotalus atrox.Toxicon : official journal of the International Society on Toxinology · 2008Article
- Integrins as antimetastatic targets of RGD-independent snake venom components in liver metastasis [corrected].Neoplasia (New York, N.Y.) · 2008Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Rhodocetin is a snake venom protein that binds to alpha2beta1 integrin, inhibiting its interaction with its endogenous ligand collagen. We have determined the mechanism by which rhodocetin inhibits the function of alpha2beta1. The interaction of alpha2beta1 with collagen and rhodocetin differed: Ca(2+) ions and slightly acidic pH values increased the binding of alpha2beta1 integrin to rhodocetin in contrast with their attenuating effect on collagen binding, suggesting that rhodocetin preferentially binds to a less active conformation of alpha2beta1 integrin. The alpha2A-domain [von Willebrand factor domain A homology domain (A-domain) of the integrin alpha2 subunit] is the major site for collagen binding to alpha2beta1. Recombinant alpha2A-domain bound rhodocetin, demonstrating that the A-domain is also the rhodocetin-binding domain. Although the interaction of alpha2beta1 with rhodocetin is affected by altering divalent cations, the interaction of the A-domain was divalent-cation-independent. The rhodocetin-binding site on the alpha2A-domain was mapped first by identifying an anti-alpha2 antibody that blocked rhodocetin binding and then mapping the epitope of the antibody using human-mouse alpha2A-domain chimaeras; and secondly, by binding studies with alpha2A-domain, which bear point mutations in the vicinity of the mapped epitope. In this way, the rhodocetin-binding site was identified as the alpha3-alpha4 loop plus adjacent alpha-helices. This region is known to form part of the collagen-binding site, thus attaining a mainly competitive mode of inhibition by rhodocetin.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.