Issue 5, 2013
From the journal:

MedChemComm

Antithrombin stabilisation by sulfated carbohydrates correlates with anticoagulant activity†

Marcelo A. Lima,‡ac   Ashley J. Hughes,‡bc   Noemi Veraldi,d   Timothy R. Rudd,bc   Rohanah Hussain,b   Adriana S. Brito,a   Suely F. Chavante,e   Ivarne I. Tersariol,a   Giuliano Siligardi,bc   Helena B. Nader‡*a  and  Edwin A. Yates‡*c  

* Corresponding authors

a Department of Biochemistry, Universidade Federal de São Paulo (UNIFESP), Rua Três de Maio 100, São Paulo, Brazil
E-mail: hbnader.bioq@epm.br

b Beam line 23 (Circular Dichroism), Diamond Light Source Ltd., Harwell Innovation Campus, Didcot, Oxfordshire, UK

c Department of Structural and Chemical Biology, University of Liverpool, Crown Street, Liverpool, UK
E-mail: eayates@liv.ac.uk

d Istituto di Ricerche Chimiche e Biochimiche “G. Ronzoni”, Via Giuseppe Colombo, 81, Milano 20133, Italy

e Department of Biochemistry, Universidade Federal do Rio Grande do Norte, Natal, RN, Brazil

Abstract

Thermal stabilisation of native antithrombin-III (AT), determined using differential scanning fluorimetry, correlated with the anticoagulant activity of heparin and heparin-related saccharides. Similar conformational changes were induced in native AT by a variety of active and inactive heparin-related sulfated carbohydrates, measured in solution using synchrotron radiation circular dichroism, and their anticoagulant activities. Measurement of native AT stabilisation provides a convenient assay for prospective anticoagulants and represents an additional parameter by which to compare biosimilar heparins.

Graphical abstract: Antithrombin stabilisation by sulfated carbohydrates correlates with anticoagulant activity

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Article information

DOI
https://doi.org/10.1039/C3MD00048F
Article type
Concise Article
Submitted
12 Feb 2013
Accepted
03 Apr 2013
First published
04 Apr 2013

Med. Chem. Commun., 2013,4, 870-873

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Antithrombin stabilisation by sulfated carbohydrates correlates with anticoagulant activity

M. A. Lima, A. J. Hughes, N. Veraldi, T. R. Rudd, R. Hussain, A. S. Brito, S. F. Chavante, I. I. Tersariol, G. Siligardi, H. B. Nader and E. A. Yates, Med. Chem. Commun., 2013, 4, 870 DOI: 10.1039/C3MD00048F

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