Structural determinants of the selectivity of KTS‐disintegrins for the α1β1 integrin
- 30 October 2004
- journal article
- research article
- Published by Wiley in FEBS Letters
- Vol. 577 (3) , 478-482
- https://doi.org/10.1016/j.febslet.2004.10.050
Abstract
KTS-disintegrins are a subfamily of short monomeric disintegrins that are potent and selective inhibitors of alpha1beta1 integrin. The amino acid sequence of the new KTS-disintegrin, viperistatin, differs from previously characterized obtustatin in three residues at position 24 (within the integrin binding loop), 38 (hydrophobic core) and 40 (C-terminal region). Noteworthy, viperistatin is about 25-fold more potent than obtustatin inhibiting the binding of this integrin to collagen IV. Synthetic peptides representing the full-length of integrin-binding loops of these disintegrins showed that the Leu24/Arg substitution appears to be partly responsible for the increased inhibitory activity of viperistatin over obtustatin.Keywords
This publication has 31 references indexed in Scilit:
- Proteases, Extracellular Matrix, and CancerThe American Journal of Pathology, 2004
- Snake venomics: Characterization of protein families in Sistrurus barbouri venom by cysteine mapping, N‐terminal sequencing, and tandem mass spectrometry analysisProteomics, 2004
- Structural Requirements of MLD-Containing Disintegrins for Functional Interaction with α4β1 and α9β1 IntegrinsBiochemistry, 2004
- Concerted Motions of the Integrin-binding Loop and the C-terminal Tail of the Non-RGD Disintegrin ObtustatinJournal of Biological Chemistry, 2003
- Snake venom disintegrins: novel dimeric disintegrins and structural diversification by disulphide bond engineeringBiochemical Journal, 2003
- Amino acid sequence and homology modeling of obtustatin, a novel non‐RGD‐containing short disintegrin isolated from the venom ofVipera lebetina obtusaProtein Science, 2003
- The Presence of the WGD Motif in CC8 Heterodimeric Disintegrin Increases Its Inhibitory Effect on αIIbβ3, αvβ3, and α5β1 IntegrinsBiochemistry, 2002
- Structural Requirements of Echistatin for the Recognition of αvβ3 and α5β1IntegrinsJournal of Biological Chemistry, 1999
- Structural and Functional Characterization of EMF10, a Heterodimeric Disintegrin from Eristocophis macmahoni Venom That Selectively Inhibits α5β1 Integrin,Biochemistry, 1999
- EC3, a Novel Heterodimeric Disintegrin from Echis carinatus Venom, Inhibits α4 and α5 Integrins in an RGD-independent MannerJournal of Biological Chemistry, 1999