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New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.

Abstract : Investigation within the pTyr-binding pocket of the STAT3 SH2 domain led us to develop a novel synthesis of two pTyr mimetics, l-tetrazolylmethylphenylalanine (l-Tmp) and l-O-malonyltyrosine (l-OMT), that were next incorporated in a high affinity ligand of STAT3 SH2 domain. Biological evaluation of peptidomimetics on STAT3 dimerization identified l-OMT as the first non-phosphorus pTyr mimetic so far reported against STAT3 SH2 domain, harboring an activity similar to that of the Pmp-containing reference peptidomimetic.
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https://www.hal.inserm.fr/inserm-00168682
Contributor : Elisabeth Hombrados <>
Submitted on : Thursday, August 30, 2007 - 3:23:39 PM
Last modification on : Friday, March 27, 2020 - 2:45:15 AM
Long-term archiving on: : Friday, April 9, 2010 - 1:19:44 AM

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Jennifer Dourlat, Bruno Valentin, Wang-Qing Liu, Christiane Garbay. New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2007, 17 (14), pp.3943-6. ⟨10.1016/j.bmcl.2007.04.107⟩. ⟨inserm-00168682⟩

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