Amerikanische Gesellschaft für Hirudotherapie

Disintegrins from hematophagous sources

Review published in Toxins Basel (2012)

Zuletzt aktualisiert: June 18, 2026Geprüft von: ASH Editorial Board
Research article — evidence reviewArticle reference
Evidence: Narrative reviewSpeichel-PharmakologieGenomik & ProteomikArzneimittelentwicklungAssumpcao TC et al. · Toxins (Basel), 2012

Abstract

Bloodsucking arthropods are a rich source of salivary molecules (sialogenins) which inhibit platelet aggregation, neutrophil function and angiogenesis. Here we review the literature on salivary disintegrins and their targets. Disintegrins were first discovered in snake venoms, and were instrumental in our understanding of integrin function and also for the development of anti-thrombotic drugs. In hematophagous animals, most disintegrins described so far have been discovered in the salivary gland of ticks and leeches. A limited number have also been found in hookworms and horseflies, and none identified in mosquitoes or sand flies. The vast majority of salivary disintegrins reported display a RGD motif and were described as platelet aggregation inhibitors, and few others as negative modulator of neutrophil or endothelial cell functions. This notably low number of reported disintegrins is certainly an underestimation of the actual complexity of this family of proteins in hematophagous secretions. Therefore an algorithm was created in order to identify the tripeptide motifs RGD, KGD, VGD, MLD, KTS, RTS, WGD, or RED (flanked by cysteines) in sialogenins deposited in GenBank database. The search included sequences from various blood-sucking animals such as ticks (e.g., Ixodes sp., Argas sp., Rhipicephalus sp., Amblyommasp.), tabanids (e.g., Tabanus sp.), bugs (e.g., Triatoma sp., Rhodnius prolixus), mosquitoes (e.g., Anopheles sp., Aedes sp., Culex sp.), sand flies (e.g., Lutzomyia sp., Phlebotomus sp.), leeches (e.g., Macrobdella sp., Placobdella sp.) and worms (e.g., Ancylostoma sp.). This approach allowed the identification of a remarkably high number of novel putative sialogenins with tripeptide motifs typical of disintegrins (>450 sequences) whose biological activity remains to be verified. This database is accessible online as a hyperlinked worksheet and displays biochemical, taxonomic, and gene ontology aspects for each putative disintegrin. It is also freely available for download (right click with the mouse) at links http://exon.niaid.nih.gov/transcriptome/RGD/RGD-Peps-WEB.xlsx (web version) and http://exon.niaid.nih.gov/transcriptome/RGD/RGD-sialogenins.zip (stand alone version).

Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.

Publication typeJournal ArticleResearch Support, N.I.H., IntramuralReview
Indexed MeSH termsAmino Acid MotifsAnimalsDisintegrinsOligopeptidesSalivary Glands

Zusammenfassung

Systematic review of disintegrins from hematophagous animals including leeches. Bioinformatic identification of 450+ putative sialogenins with RGD/KGD/MLD tripeptide motifs typical of platelet-aggregation inhibitors.

Warum dies für die Hirudotherapie relevant ist

This review surveys salivary disintegrins from hematophagous animals, noting that most described so far originate from tick and leech salivary glands and typically display RGD motifs functioning as platelet aggregation inhibitors. The authors developed an algorithm to mine GenBank for putative disintegrins across blood-sucking species—including leeches such as Macrobdella sp. and Placobdella sp.—identifying over 450 novel sequences with characteristic tripeptide motifs. For ASH's domain, this highlights the molecular diversity of the leech secretome and its potential for discovering novel anti-platelet or anti-thrombotic agents. Caveat: The biological activity of the vast majority of identified putative disintegrins remains unverified, and leech-derived sequences represent only a fraction of the total dataset.

Zitation

Disintegrins from hematophagous sources.

Assumpcao TC et al. · Toxins (Basel), 2012

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