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  • A novel family of RGD-containing disintegrins (Tablysin-15) from the salivary gland of the horsefly Tabanus yao targets αIIbβ3 or αVβ3 and inhibits platelet aggregation and angiogenesis.

A novel family of RGD-containing disintegrins (Tablysin-15) from the salivary gland of the horsefly Tabanus yao targets αIIbβ3 or αVβ3 and inhibits platelet aggregation and angiogenesis.

Thrombosis and haemostasis (2011-04-09)
D Ma, X Xu, S An, H Liu, X Yang, J F Andersen, Y Wang, F Tokumasu, J M C Ribeiro, I M B Francischetti, R Lai
ABSTRACT

A novel family of RGD-containing molecules (Tablysin-15) has been molecularly characterised from the salivary gland of the haematophagous horsefly Tabanus yao. Tablysin-15 does not share primary sequence homology to any disintegrin discovered so far, and displays an RGD motif in the N-terminus of the molecule. It is also distinct from disintegrins from Viperidae since its mature form is not released from a metalloproteinase precursor. Tablysin-15 exhibits high affinity binding for platelet αIIbβ3 and endothelial cell αVβ3 integrins, but not for α5β1 or α2β1. Accordingly, it blocks endothelial cell adhesion to vitronectin (IC50 ~1 nM) and marginally to fibronectin (IC50 ~1 μM), but not to collagen. It also inhibits fibroblast growth factor (FGF)-induced endothelial cell proliferation, and attenuates tube formation in vitro. In platelets, Tablysin-15 inhibits aggregation induced by collagen, ADP and convulxin, and prevents static platelet adhesion to immobilised fibrinogen. In addition, solid-phase assays and flow cytometry demonstrates that αIIbβ3 binds to Tablysin-15. Moreover, immobilised Tablysin-15 supports platelet adhesion by a mechanism which was blocked by anti-integrin αIIbβ3 monoclonal antibody (e.g. abciximab) or by EDTA. Furthermore, Tablysin-15 dose-dependently attenuates thrombus formation to collagen under flow. Consistent with these findings, Tablysin-15 displays antithrombotic properties in vivo suggesting that it is a useful tool to block αIIbβ3, or as a prototype to develop antithrombotics. The RGD motif in the unique sequence of Tablysin-15 represents a novel template for studying the structure-function relationship of the disintegrin family of inhibitors.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Anti-Integrin β3 Antibody, clone PM6/13, clone PM6/13, Chemicon®, from mouse
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SKUVendor SKUPack SizeAvailabilityPrice
A464310-100MG100 mg
Ships in 7 days - from Aldrich Partner.
$37.95
A464310-250MG250 mg
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$56.35
A464310-1G1 g
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$136.85
A464310-5G5 g
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$392.15

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Sigma-Aldrich
Anti-Mouse IgG (whole molecule)−Alkaline Phosphatase antibody produced in goat, affinity isolated antibody, buffered aqueous glycerol solution
Sign Into View Organizational & Contract Pricing
SKUVendor SKUPack SizeAvailabilityPrice
A464310-100MG100 mg
Ships in 7 days - from Aldrich Partner.
$37.95
A464310-250MG250 mg
Ships in 7 days - from Aldrich Partner.
$56.35
A464310-1G1 g
Ships in 7 days - from Aldrich Partner.
$136.85
A464310-5G5 g
Ships in 7 days - from Aldrich Partner.
$392.15

To order products, please contact your local dealer.