Cover Picture: Selective Inhibitors of the Protein Tyrosine Phosphatase SHP2 Block Cellular Motility and Growth of Cancer Cells in vitro and in vivo (ChemMedChem 5/2015). Issue 5 (May 2015)

• Record Type: Journal Article
• Authors: Grosskopf, Stefanie; Eckert, Chris; Arkona, Christoph; Radetzki, Silke; Böhm, Kerstin; Heinemann, Udo; Wolber, Gerhard; von Kries, Jens‐Peter; Birchmeier, Walter; Rademann, Jörg
• Is Part Of: ChemMedChem. Volume 10:Issue 5(2015:May)
• Page Start: 757
• Page End: 757
• Publication Date: 2015-05
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201590011
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="graphical" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold>The front cover picture shows</bold> the first nanomolar and specific inhibitor of the protein tyrosine phosphatase SHP2 depicted in the protein binding site. The molecule contains benzene sulfonate as a phosphotyrosine mimicking fragment, binding affinity and selectivity of the best inhibitor result from secondary site interactions conveyed by the triaryl‐substituted pyrazolone scaffold. The best inhibitor, GS‐493, was capable to block mobility and invasiveness of pancreas adenocarcinoma and of small‐cell lung cancer cells and inhibited tumor growth in a xenograft mouse model, thereby contributing to validate SHP2 as a potential target to prevent metastasis of cancer cells. For further details, see the Full Paper by Jörg Rademann et al. on <ext-link ext-link-type="doi" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink">p. 815 ff.</ext-link><graphic position="anchor" mimetype="image" xlink:href="ark:/27927/pgjjv02jgg" orientation="portrait" xlink:type="simple" xmlns:xlink="http://www.w3.org/1999/xlink" /></p> </abstract>