ArticleBMC structural biology2014
Structural basis of RGD-hirudin binding to thrombin: Tyr3 and five C-terminal residues are crucial for inhibiting thrombin activity.
Article in BMC structural biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 27 citations in OpenAlex.
- The great diversity: monomeric and oligomeric hirudins, hirudin-like factors and decorsins in the Asian medicinal leeches Hirudo nipponia and Hirudo tianjinensis.Parasitology research · 2026Article
- Hirudins and fenestrins of the African medicinal leech Asiaticobdella fenestrata.Parasitology research · 2025Article
- Characterization and antioxidant activities of glycosaminoglycans from dried leech.Glycoconjugate journal · 2023Article
- Design and fabrication of r-hirudin loaded dissolving microneedle patch for minimally invasive and long-term treatment of thromboembolic disease.Asian journal of pharmaceutical sciences · 2022Article
- Short tail stories: the hirudin-like factors HLF6 and HLF7 of the Asian medicinal leech, Hirudinaria manillensis.Parasitology research · 2021Article
- Study on the activity of recombinant mutant tissue-type plasminogen activator fused with the C-terminal fragment of hirudin.Journal of thrombosis and thrombolysis · 2021Article
- The hirudin-like factors HLF3 and HLF4-hidden hirudins of European medicinal leeches.Parasitology research · 2020Article
- Hirudins of the Asian medicinal leech, Hirudinaria manillensis: same same, but different.Parasitology research · 2019Article
- Identification and characterization of hirudin-HN, a new thrombin inhibitor, from the salivary glands ofPeerJ · 2019Article
- Hirudins and hirudin-like factors in Hirudinidae: implications for function and phylogenetic relationships.Parasitology research · 2017Article
- Chinese Medicinal Leech: Ethnopharmacology, Phytochemistry, and Pharmacological Activities.Evidence-based complementary and alternative medicine : eCAM · 2016Review
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundHirudin is an anti-coagulation protein produced by the salivary glands of the medicinal leech Hirudomedicinalis. It is a powerful and specific thrombin inhibitor. The novel recombinant hirudin, RGD-hirudin, which contains an RGD motif, competitively inhibits the binding of fibrinogen to GPIIb/IIIa on platelets, thus inhibiting platelet aggregation while maintaining its anticoagulant activity.
resultsRecombinant RGD-hirudin and six mutant variants (Y3A, S50A, Q53A, D55A, E57A and I59A), designed based on molecular simulations, were expressed in Pichia pastoris. The proteins were refolded and purified to homogeneity as monomers by gel filtration and anion exchange chromatography. The anti-thrombin activity of the six mutants and RGD-hirudin was tested. Further, we evaluated the binding of the mutant variants and RGD-hirudin to thrombin using BIAcore surface plasmon resonance analysis (SPR). Kinetics and affinity constants showed that the KD values of all six mutant proteins were higher than that of RGD-hirudin.
conclusionsThese findings contribute to a novel understanding of the interaction between RGD-hirudin and thrombin.
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