Total Synthesis of Homogeneous Variants of Hirudin P6: A Post-Translationally Modified Anti-Thrombotic Leech-Derived Protein

Title
Total Synthesis of Homogeneous Variants of Hirudin P6: A Post-Translationally Modified Anti-Thrombotic Leech-Derived Protein
Publication Date
2014
Author(s)
Hsieh, Yves S Y
Wijeyewickrema, Lakshmi C
Wilkinson, Brendan
( author )
OrcID: https://orcid.org/0000-0003-1866-6540
Email: bwilkin7@une.edu.au
UNE Id une-id:bwilkin7
Pike, Robert N
Payne, Richard J
Type of document
Journal Article
Language
en
Entity Type
Publication
Publisher
Wiley-VCH Verlag GmbH & Co KGaA
Place of publication
Germany
DOI
10.1002/anie.201310777
UNE publication id
une:20869
Abstract
Hirudin P6 is a leech-derived anti-thrombotic protein which possesses two post-translational modifications, O-glycosylation and tyrosine sulfation. In this study we report the ligation-based synthesis of a library of hirudin P6 proteins possessing homogeneous glycosylation and sulfation modifications. The nature of the modifications incorporated was shown to have a drastic effect on inhibition against both the fibrinogenolytic and amidolytic activities of thrombin and thus highlights a potential means for attenuating the biological activity of the protein.
Link
Citation
Angewandte Chemie (International Edition), 53(15), p. 3947-3951
ISSN
1521-3773
1433-7851
Start page
3947
End page
3951

Files:

NameSizeformatDescriptionLink