Target intelligence / Profile preview

Phosphatidylinositol 3-kinase (PI3K) (PI3K)

Target
PI3K
Molecular classification
Enzyme, Kinase, Transferase
01

Overview

Sarocladinosides A–C are novel rutinoside derivatives recently isolated from the endophytic fungus Sarocladium strictum (Molecules 2023, 28, 5748). These compounds have demonstrated significant anti-tumor activity, particularly against human pancreatic cancer cell lines such as PANC-1 and AsPC-1 (Molecules 2023, 28, 5748). Their primary mechanism of action involves the inhibition of the Phosphatidylinositol 3-kinase (PI3K)/AKT/mechanistic target of rapamycin (mTOR) signaling axis (Molecules 2023, 28, 5748). This pathway is a critical regulator of cell growth, survival, and metabolism, and its dysregulation is a hallmark of pancreatic cancer progression (PubMed, PMC10420455). By suppressing the phosphorylation of PI3K, AKT, and mTOR, Sarocladinosides effectively trigger the apoptotic cascade in malignant cells (Molecules 2023, 28, 5748). Research indicates that these rutinosides can induce cell cycle arrest and reduce the expression of anti-apoptotic proteins like Bcl-2 (Molecules 2023, 28, 5748). While currently in the experimental stage, these molecules represent a promising scaffold for developing new targeted therapies for pancreatic cancer (Molecules 2023, 28, 5748). The discovery of these rutinosides highlights the potential of fungal endophytes as a source of bioactive compounds for oncology (Molecules 2023, 28, 5748).

Other names
Phosphoinositide 3-kinasePI 3-kinasePI3-kinasePhosphatidylinositol-4,5-bisphosphate 3-kinasePI3K/AKT/mTOR pathway
02

Mechanism of action

Inhibition of the PI3K/AKT/mTOR signaling pathway

03

Biological functions

Signal transductionCell proliferationApoptosisCell cycle regulationMetabolism
04

Disease associations

CancerPancreatic cancerInflammationDiabetes mellitus
05

Safety considerations

HyperglycemiaGastrointestinal toxicityIncreased risk of infectionHepatotoxicityRash
06

Interacting drugs

Sarocladinoside A

5 more in the full profile.

07

Biomarkers

p-AKT (phosphorylated AKT)p-mTOR (phosphorylated mTOR)Caspase-3 activationPIK3CA mutation status

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