Substrate-guided design of selective FXIIa inhibitors based on the plant-derived Momordica cochinchinensis trypsin inhibitor-II (MCoTI-II) scaffold

Swedberg, Joakim E., Mahatmanto, Tunjung, Ghani, Hafiza Abdul, de Veer, Simon J., Schroeder, Christina I., Harris, Jonathan M. and Craik, David J. (2016) Substrate-guided design of selective FXIIa inhibitors based on the plant-derived Momordica cochinchinensis trypsin inhibitor-II (MCoTI-II) scaffold. Journal of Medicinal Chemistry, 59 15: 7287-7292. doi:10.1021/acs.jmedchem.6b00557


Author Swedberg, Joakim E.
Mahatmanto, Tunjung
Ghani, Hafiza Abdul
de Veer, Simon J.
Schroeder, Christina I.
Harris, Jonathan M.
Craik, David J.
Title Substrate-guided design of selective FXIIa inhibitors based on the plant-derived Momordica cochinchinensis trypsin inhibitor-II (MCoTI-II) scaffold
Formatted title
Substrate-guided design of selective FXIIa inhibitors based on the plant-derived Momordica cochinchinensis trypsin inhibitor-II (MCoTI-II) scaffold
Journal name Journal of Medicinal Chemistry   Check publisher's open access policy
ISSN 0022-2623
1520-4804
Publication date 2016-08-01
Year available 2016
Sub-type Article (original research)
DOI 10.1021/acs.jmedchem.6b00557
Open Access Status Not yet assessed
Volume 59
Issue 15
Start page 7287
End page 7292
Total pages 6
Place of publication Washington, DC United States
Publisher American Chemical Society
Language eng
Formatted abstract
Thrombosis is a leading cause of morbidity and mortality associated with cardiovascular diseases. Inhibition of factor XIIa (FXIIa) provides thrombus protection without bleeding complications. Here, we defined the extended substrate specificity of FXIIa and its close homologue factor Xa and used these data, together with inhibitor-based and structure-guided methods, to engineer selective FXIIa inhibitors based on Momordica cochinchinensis trypsin inhibitor-II.
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: HERDC Pre-Audit
Institute for Molecular Bioscience - Publications
 
Versions
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 6 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 5 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Wed, 07 Sep 2016, 02:43:38 EST by Simon De Veer on behalf of Institute for Molecular Bioscience