Target intelligence / Profile preview

Phosphatase and Tensin Homolog (PTEN)

Target
PTEN
Molecular classification
Phosphatase, Tumor Suppressor
01

Overview

PTEN is a tumor suppressor gene encoding a dual-specificity phosphatase that negatively regulates the PI3K/AKT pathway by dephosphorylating PIP3 to PIP2. It plays a crucial role in controlling cell proliferation, survival, metabolism, migration, adhesion, angiogenesis, genetic stability, and DNA repair. Loss or mutation of PTEN is common in many cancers, leading to unchecked PI3K/AKT activity and tumorigenesis.

Other names
MMAC1TEP1
02

Mechanism of action

PTEN dephosphorylates PIP3 to PIP2, inhibiting AKT activation. Drugs may aim to restore PTEN function or indirectly modulate the pathway.

03

Biological functions

Regulation of PI3K/AKT pathwayCell cycle regulationApoptosis regulationCell migrationCell adhesionAngiogenesis regulationDNA damage responseDNA repair
04

Disease associations

CancerBannayan-Riley-Ruvalcaba syndrome
05

Safety considerations

Restoring PTEN activity could have broad effects on cellular signaling.Potential for off-target effects.
06

Interacting drugs

PTEN inhibitors (in development)
07

Biomarkers

PTEN expression levelPTEN mutation statusPIP3 levelsAKT phosphorylation status

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