Modifications of the GSK3β substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics

Katherine J. Kayser, Matthew P. Glenn, Said M. Sebti, Jin Q. Cheng, Andrew Hamilton

Research output: Contribution to journalArticle

Abstract

Amplification, overexpression, and elevated activation of Akt have been detected in many human malignancies making it an important target for cancer therapy. The Akt substrate-binding site offers a large number of potential interactions to an appropriately designed small molecule and can form the basis for the development of selective inhibitors. Here, we report the progression of GSK3β substrate-mimetic inhibitors towards the development of a potent, small molecule substrate-mimetic inhibitor of Akt.

Original languageEnglish (US)
Pages (from-to)2068-2073
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume17
Issue number7
DOIs
StatePublished - Apr 1 2007

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Substrates
Neoplasms
Molecules
Binding Sites
Amplification
Therapeutics
Chemical activation

Keywords

  • Akt
  • Cancer
  • Peptidomimetics
  • Protein kinase B
  • Substrate-mimetic

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Modifications of the GSK3β substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics. / Kayser, Katherine J.; Glenn, Matthew P.; Sebti, Said M.; Cheng, Jin Q.; Hamilton, Andrew.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 17, No. 7, 01.04.2007, p. 2068-2073.

Research output: Contribution to journalArticle

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