PROTEIN AFFINITY MAP OF CHEMICAL SPACE

Citation
Lm. Kauvar et al., PROTEIN AFFINITY MAP OF CHEMICAL SPACE, Journal of chromatography B. Biomedical sciences and applications, 715(1), 1998, pp. 93-102
Citations number
29
Categorie Soggetti
Chemistry Analytical","Biochemical Research Methods
Journal title
Journal of chromatography B. Biomedical sciences and applications
ISSN journal
13872273 → ACNP
Volume
715
Issue
1
Year of publication
1998
Pages
93 - 102
Database
ISI
SICI code
0378-4347(1998)715:1<93:PAMOCS>2.0.ZU;2-I
Abstract
Affinity fingerprinting is a quantitative method for mapping chemical space based on binding preferences of compounds for a reference panel of proteins. An effective reference panel of <20 proteins can be empir ically selected which shows differential interaction with nearly all c ompounds. By using this map to iteratively sample the chemical space, identification of active ligands from a library of 30 000 candidate co mpounds has been accomplished for a wide spectrum of specific protein targets. In each case, <200 compounds were directly assayed against th e target. Further, analysis of the fingerprint database suggests a str ategy for effective selection of affinity chromatography ligands and s caffolds for combinatorial chemistry. With such a system, the large nu mbers of potential therapeutic targets emerging from genome research c an be categorized according to ligand binding properties, complementin g sequence based classification. (C) 1998 Elsevier Science B.V. All ri ghts reserved.