Recent development of anticancer therapeutics targeting AKT

John K. Morrow, Lei Du-Cuny, Lu Chen, Emmanuelle J. Meuillet, Eugene A. Mash, Garth Powis, Shuxing Zhang

Research output: Contribution to journalArticle

25 Scopus citations

Abstract

The serine/threonine kinase Akt has proven to be a significant signaling target, involved in various biological functions. Because of its cardinal role in numerous cellular responses, Akt has been implicated in many human diseases, particularly cancer. It has been established that Akt is a viable and feasible target for anticancer therapeutics. Analysis of all Akt kinases reveals conserved homology for an N-terminal regulatory domain, which contains a pleckstrin-homology (PH) domain for cellular translocation, a kinase domain with serine/threonine specificity, and a C-terminal extension domain. These well defined regions have been targeted, and various approaches, including in silico methods, have been implemented to develop Akt inhibitors. In spite of unique techniques and a prolific body of knowledge surrounding Akt, no targeted Akt therapeutics have reached the market yet. Here we will highlight successes and challenges to date on the development of anticancer agents modulating the Akt pathway in recent patents as well as discuss the methods employed for this task. Special attention will be given to patents with focus on those discoveries using computer-aided drug design approaches.

Original languageEnglish (US)
Pages (from-to)146-159
Number of pages14
JournalRecent Patents on Anti-Cancer Drug Discovery
Volume6
Issue number1
DOIs
StatePublished - Jan 11 2011

Keywords

  • Akt
  • Anticancer therapeutics
  • Computer-aided drug design
  • Drug discovery and development
  • Pleckstrin-homology (PH) domain
  • Serine/threonine kinase

ASJC Scopus subject areas

  • Oncology
  • Drug Discovery
  • Cancer Research
  • Pharmacology (medical)

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