Title
Substrate activity screening (SAS) and related approaches in medicinal chemistry Substrate activity screening (SAS) and related approaches in medicinal chemistry
Author
Faculty/Department
Faculty of Sciences. Biology
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Weinheim :Wiley-v c h verlag gmbh ,
Subject
Pharmacology. Therapy
Source (journal)
ChemMedChem. - Place of publication unknown
Volume/pages
11(2016) :5 , p. 467-476
ISSN
1860-7179
ISI
000372192000002
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
Abstract
Substrate activity screening (SAS) was presented a decade ago by Ellman and co-workers as a straightforward methodology for the identification of fragment-sized building blocks for enzyme inhibitors. Ever since, SAS and variations derived from it have been successfully applied to the discovery of inhibitors of various families of enzymatically active drug targets. This review covers key achievements and challenges of SAS and related methodologies, including the modified substrate activity screening (MSAS) approach. Special attention is given to the kinetic and thermodynamic aspects of these methodologies, as a thorough understanding thereof is crucial for successfully transforming the identified fragment-sized hits into potent inhibitors.
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