Publication
Title
Substrate activity screening (SAS) and related approaches in medicinal chemistry
Author
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.
Language
English
Source (journal)
ChemMedChem. - Place of publication unknown
Publication
Weinheim : Wiley-v c h verlag gmbh, 2016
ISSN
1860-7179 [print]
1860-7187 [online]
Volume/pages
11:5(2016), p. 467-476
ISI
000372192000002
Full text (Publishers DOI)
Full text (publishers version - intranet only)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 10.05.2016
Last edited 17.05.2017
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