Inside Cover: Tailoring Small Molecules for an Allosteric Site on Procaspase‐6 (ChemMedChem 1/2014). Issue 1 (January 2014)

• Record Type: Journal Article
• Authors: Murray, Jeremy; Giannetti, Anthony M.; Steffek, Micah; Gibbons, Paul; Hearn, Brian R.; Cohen, Frederick; Tam, Christine; Pozniak, Christine; Bravo, Brandon; Lewcock, Joe; Jaishankar, Priyadarshini; Ly, Cuong Q.; Zhao, Xianrui; Tang, Yinyan; Chugha, Preeti; Arkin, Michelle R.; Flygare, John; Renslo, Adam R.
• Is Part Of: ChemMedChem. Volume 9:Issue 1(2014:Jan.)
• Page Start: 2
• Page End: 2
• Publication Date: 2014-01
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201390058
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>The inside cover picture shows</bold> small molecules tailored for an allosteric site in procaspase‐6. The combination of biophysical fragment screening, structure‐ and computation‐aided design, and chemical synthesis enabled the discovery of multiple nanomolar‐affinity ligands for this new site. The compounds significantly stabilize the protein, suggesting new avenues for controlling caspase activity and/or activation by allosteric mechanisms. For more details, see the Communication by Jeremy Murray, Adam R. Renslo et al. on <ext-link ext-link-type="doi" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">p. 73 ff.</ext-link><boxed-text content-type="graphic" position="anchor" orientation="portrait"><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgg4t3pvrp5" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></boxed-text></p> </abstract>