Progress in discovery of small-molecule modulators of protein–protein interactions via fragment screening

[Display omitted] Protein–protein interactions (PPIs) present a formidable challenge to medicinal chemistry. The extended and open nature of many binding sites at protein interfaces has made it difficult to find useful chemical matter by traditional screening methods using standard screening librari...

Full description

Saved in:
Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 25; no. 12; pp. 2461 - 2468
Main Author Magee, Thomas V.
Format Journal Article
LanguageEnglish
Published England Elsevier Ltd 15.06.2015
Subjects
Apoptosis Regulatory Proteins - chemistry
Apoptosis Regulatory Proteins - metabolism
Bacterial Proteins - chemistry
Bacterial Proteins - metabolism
Binding Sites
Fragments
Molecular Dynamics Simulation
PPI
Protein Interaction Domains and Motifs
Proteins - chemistry
Proteins - metabolism
Small Molecule Libraries - chemistry
Small Molecule Libraries - metabolism
Fragments
PPI
Online AccessGet full text

Cover

More Information
Summary:[Display omitted] Protein–protein interactions (PPIs) present a formidable challenge to medicinal chemistry. The extended and open nature of many binding sites at protein interfaces has made it difficult to find useful chemical matter by traditional screening methods using standard screening libraries. This Digest focuses on the progress that has been made in discovering small-molecule modulators for a diverse selection of PPI targets using fragment screening and highlights the utility of this strategy in this context.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.04.089