@article{3ac18dddefdd4f8684a938f39227cae2,
title = "Diversity-Oriented Synthesis as a Strategy for Fragment Evolution against GSK3β",
abstract = "Traditional fragment-based drug discovery (FBDD) relies heavily on structural analysis of the hits bound to their targets. Herein, we present a complementary approach based on diversity-oriented synthesis (DOS). A DOS-based fragment collection was able to produce initial hit compounds against the target GSK3β, allow the systematic synthesis of related fragment analogues to explore fragment-level structure-activity relationship, and finally lead to the synthesis of a more potent compound.",
keywords = "Diversity oriented synthesis, GSK3β, fragment growing, fragment-based drug discovery",
author = "Yikai Wang and Wach, {Jean Yves} and Patrick Sheehan and Cheng Zhong and Chenyang Zhan and Richard Harris and Almo, {Steven C.} and Joshua Bishop and Haggarty, {Stephen J.} and Alexander Ramek and Berry, {Kayla N.} and Conor O'Herin and Koehler, {Angela N.} and Hung, {Alvin W.} and Young, {Damian W.}",
note = "Funding Information: Funding support was provided by Broad Institute SPARC Grant. Additional support for the Haggarty Laboratory was provided by the NIH/NIMH (R01MH091115), the Tau Consortium, and the Barrus Foundation. Additional support for the Almo Laboratory was provided by by NIH/NIGMS U54 GM094662 and NIH/NCI P30 CA013330. Publisher Copyright: {\textcopyright} 2016 American Chemical Society.",
year = "2016",
month = sep,
day = "8",
doi = "10.1021/acsmedchemlett.6b00230",
language = "English (US)",
volume = "7",
pages = "852--856",
journal = "ACS Medicinal Chemistry Letters",
issn = "1948-5875",
publisher = "American Chemical Society",
number = "9",
}