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A chemical epitope-targeting strategy for protein capture agents: The serine 474 epitope of the kinase Akt2

  • Arundhati Nag
  • , Samir Das
  • , Mary Beth Yu
  • , Kaycie M. Deyle
  • , Steven W. Millward
  • , James R. Heath

Research output: Contribution to journalArticlepeer-review

Abstract

Target and click: Peptide ligands targeted to the C-terminal motif of the kinase Akt2 were obtained by combining phosphate recognition of a dinuclear zinc(II) complex with in situ click chemistry to target this epitope. The peptide ligands (shown as XXXXX) selectively bind the C-terminal polypeptide of Akt2, and are selective for Akt2 relative to the Akt1 and Akt3 isoforms. The ligands differentially modulate Akt2 activity.

Original languageEnglish (US)
Pages (from-to)13975-13979
Number of pages5
JournalAngewandte Chemie - International Edition
Volume52
Issue number52
DOIs
StatePublished - Dec 23 2013

Keywords

  • click chemistry
  • drug design
  • inhibitors
  • kinases
  • peptides

ASJC Scopus subject areas

  • Catalysis
  • General Chemistry

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