Imperial College London
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DrElenaDe Vita

Faculty of Natural Sciences, Department of Chemistry

 
 
 
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e.de-vita17 CV

 
 
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Location

 

Molecular Sciences Research HubWhite City Campus

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Summary

 

Publications

Citation

BibTex format

@article{Santamaria:2021:10.1080/14756366.2021.1983808,
author = {Santamaria, S and Buemi, F and Nuti, E and Cuffaro, D and De, Vita E and Tuccinardi, T and Rossello, A and Howell, S and Mehmood, S and Snijders, AP and de, Groot R},
doi = {10.1080/14756366.2021.1983808},
journal = {Journal of Enzyme Inhibition and Medicinal Chemistry},
title = {Development of a fluorogenic ADAMTS-7 substrate},
url = {http://dx.doi.org/10.1080/14756366.2021.1983808},
volume = {36},
year = {2021}
}
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RIS format (EndNote, RefMan)

TY  - JOUR
AB  - The extracellular protease ADAMTS-7 has been identified as a potential therapeutic target in atherosclerosis and associated diseases such as coronary artery disease (CAD). However, ADAMTS-7 inhibitors have not been reported so far. Screening of inhibitors has been hindered by the lack of a suitable peptide substrate and, consequently, a convenient activity assay. Here we describe the first fluorescence resonance energy transfer (FRET) substrate for ADAMTS-7, ATS7FP7. ATS7FP7 was used to measure inhibition constants for the endogenous ADAMTS-7 inhibitor, TIMP-4, as well as two hydroxamate-based zinc chelating inhibitors. These inhibition constants match well with IC50 values obtained with our SDS-PAGE assay that uses the N-terminal fragment of latent TGF-β–binding protein 4 (LTBP4S-A) as a substrate. Our novel fluorogenic substrate ATS7FP7 is suitable for high throughput screening of ADAMTS-7 inhibitors, thus accelerating translational studies aiming at inhibition of ADAMTS-7 as a novel treatment for cardiovascular diseases such as atherosclerosis and CAD.
AU  - Santamaria,S
AU  - Buemi,F
AU  - Nuti,E
AU  - Cuffaro,D
AU  - De,Vita E
AU  - Tuccinardi,T
AU  - Rossello,A
AU  - Howell,S
AU  - Mehmood,S
AU  - Snijders,AP
AU  - de,Groot R
DO  - 10.1080/14756366.2021.1983808
PY  - 2021///
SN  - 1475-6366
TI  - Development of a fluorogenic ADAMTS-7 substrate
T2  - Journal of Enzyme Inhibition and Medicinal Chemistry
UR  - http://dx.doi.org/10.1080/14756366.2021.1983808
UR  - http://hdl.handle.net/10044/1/92315
VL  - 36
ER  -
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