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.
Keywords: Akt, anticancer therapeutics, computer-aided drug design, drug discovery and development, pleckstrin-homology (PH) domain, serine/threonine kinase, pleckstrin-homology, Leu156, Thr211, Glu278, Asn279, PDPK1, myelopoiesis, perifosine, ADMET, SYBYL, surface plasmon resonance spectroscopy, X-ray crystallography, Bevacizumab, Tarceva, Gleevec
Recent Patents on Anti-Cancer Drug Discovery
Title: Recent Development of Anticancer Therapeutics Targeting Akt
Volume: 6 Issue: 1
Author(s): John K. Morrow, Lei Du-Cuny, Lu Chen, Emmanuelle J. Meuillet, Eugene A. Mash, Garth Powis and Shuxing Zhang
Affiliation:
Keywords: Akt, anticancer therapeutics, computer-aided drug design, drug discovery and development, pleckstrin-homology (PH) domain, serine/threonine kinase, pleckstrin-homology, Leu156, Thr211, Glu278, Asn279, PDPK1, myelopoiesis, perifosine, ADMET, SYBYL, surface plasmon resonance spectroscopy, X-ray crystallography, Bevacizumab, Tarceva, Gleevec
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.
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Cite this article as:
K. Morrow John, Du-Cuny Lei, Chen Lu, J. Meuillet Emmanuelle, A. Mash Eugene, Powis Garth and Zhang Shuxing, Recent Development of Anticancer Therapeutics Targeting Akt, Recent Patents on Anti-Cancer Drug Discovery 2011; 6 (1) . https://dx.doi.org/10.2174/157489211793980079
DOI https://dx.doi.org/10.2174/157489211793980079 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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