PTEN modulators: A patent review

Chandra S. Boosani, Devendra K. Agrawal

Research output: Contribution to journalReview article

41 Citations (Scopus)

Abstract

Introduction: PTEN (phosphatase and tensin homolog deleted on chromosome 10) plays a pivotal role in controlling intracellular signaling for cell survival and proliferation by inhibiting the PI3K/Akt pathway, and its dysfunction is associated with several neoplastic diseases. PTEN is frequently found mutated in many pathological conditions highlighting its importance in normal physiological function. Unlike several cellular proteins which are activated by phosphorylation, PTEN is inactivated upon phosphorylation by specific kinases which phosphorylate serine and threonine residues in its C-terminal region. Therefore, development of therapeutic agents that specifically target kinases and kinase-domain-containing proteins affecting PTEN would lead to the treatment of PTEN-related diseases. Areas covered: With increasing evidence on the role of PTEN in many human diseases, the present review focuses on the clinical relevance of PTEN with a comprehensive list of currently identified modulators of PTEN, and proposes potentially novel molecular targets which could aid in the development of drug candidates for the treatment of PTEN-related diseases such as cardiovascular diseases, diabetes, obesity, cancer, autism, Parkinson's and Alzheimer's diseases. Expert opinion: This review describes several target sites that could help in the development of novel drug candidates to regulate or restore the normal physiological functions of PTEN and are essential in the treatment of human diseases where PTEN plays a pivotal role.

Original languageEnglish
Pages (from-to)569-580
Number of pages12
JournalExpert Opinion on Therapeutic Patents
Volume23
Issue number5
DOIs
StatePublished - May 2013

Fingerprint

PTEN Phosphohydrolase
Phosphotransferases
Phosphorylation
Chromosomes, Human, Pair 10
Expert Testimony
Threonine
Autistic Disorder
Phosphatidylinositol 3-Kinases
Pharmaceutical Preparations
Serine
Parkinson Disease
Cell Survival
Alzheimer Disease
Cardiovascular Diseases
Obesity
Cell Proliferation
Neoplasms
Proteins
Therapeutics
Protein Domains

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Pharmacology

Cite this

PTEN modulators : A patent review. / Boosani, Chandra S.; Agrawal, Devendra K.

In: Expert Opinion on Therapeutic Patents, Vol. 23, No. 5, 05.2013, p. 569-580.

Research output: Contribution to journalReview article

Boosani, Chandra S. ; Agrawal, Devendra K. / PTEN modulators : A patent review. In: Expert Opinion on Therapeutic Patents. 2013 ; Vol. 23, No. 5. pp. 569-580.
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