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The development of phosphatidylinositol ether lipid analogues as inhibitors of the serine/threonine kinase, Akt.

Publication ,  Journal Article
Gills, JJ; Dennis, PA
Published in: Expert Opin Investig Drugs
July 2004

The serine/threonine kinase Akt is a component of the phosphatidylinositol 3'-kinase/Akt signal transduction pathway that is activated by receptor tyrosine kinases, activated Ras and integrins. As Akt regulates many processes crucial to carcinogenesis, and Akt activation has been observed in human cancers, intense efforts are underway to develop Akt inhibitors as cancer therapeutics. Towards this aim, phosphatidylinositol ether lipid analogues (PIAs), which are structurally similar to the products of phosphatidylinositol 3'-kinase, have been synthesised. PIAs inhibit Akt translocation, phosphorylation and kinase activity. Furthermore, they selectively induce apoptosis in cancer cell lines that depend on Akt for survival. This review will trace the development of PIAs, cover the biological activities of PIAs and discuss future steps and challenges in their development.

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Published In

Expert Opin Investig Drugs

DOI

EISSN

1744-7658

Publication Date

July 2004

Volume

13

Issue

7

Start / End Page

787 / 797

Location

England

Related Subject Headings

  • Proto-Oncogene Proteins c-akt
  • Proto-Oncogene Proteins
  • Protein Serine-Threonine Kinases
  • Phospholipid Ethers
  • Phosphatidylinositols
  • Pharmacology & Pharmacy
  • Humans
  • Enzyme Inhibitors
  • Animals
  • 3214 Pharmacology and pharmaceutical sciences
 

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Gills, J. J., & Dennis, P. A. (2004). The development of phosphatidylinositol ether lipid analogues as inhibitors of the serine/threonine kinase, Akt. Expert Opin Investig Drugs, 13(7), 787–797. https://doi.org/10.1517/13543784.13.7.787
Gills, Joell J., and Phillip A. Dennis. “The development of phosphatidylinositol ether lipid analogues as inhibitors of the serine/threonine kinase, Akt.Expert Opin Investig Drugs 13, no. 7 (July 2004): 787–97. https://doi.org/10.1517/13543784.13.7.787.
Gills, Joell J., and Phillip A. Dennis. “The development of phosphatidylinositol ether lipid analogues as inhibitors of the serine/threonine kinase, Akt.Expert Opin Investig Drugs, vol. 13, no. 7, July 2004, pp. 787–97. Pubmed, doi:10.1517/13543784.13.7.787.
Gills JJ, Dennis PA. The development of phosphatidylinositol ether lipid analogues as inhibitors of the serine/threonine kinase, Akt. Expert Opin Investig Drugs. 2004 Jul;13(7):787–797.

Published In

Expert Opin Investig Drugs

DOI

EISSN

1744-7658

Publication Date

July 2004

Volume

13

Issue

7

Start / End Page

787 / 797

Location

England

Related Subject Headings

  • Proto-Oncogene Proteins c-akt
  • Proto-Oncogene Proteins
  • Protein Serine-Threonine Kinases
  • Phospholipid Ethers
  • Phosphatidylinositols
  • Pharmacology & Pharmacy
  • Humans
  • Enzyme Inhibitors
  • Animals
  • 3214 Pharmacology and pharmaceutical sciences