Drug intelligence / Profile preview

2-AAPA

Development stage
Preclinical
Lead developer
South Dakota State University
Modality
Small Molecules
01

Overview

2-AAPA is a novel small molecule anticancer agent that induces microtubule depolymerization and subsequent apoptosis. Its unique mechanism of action involves the glutathionylation of proteins, specifically tubulin, which disrupts microtubule assembly and function. This disruption leads to cell cycle arrest at the G2/M phase and triggers programmed cell death. Preclinical research has demonstrated that 2-AAPA inhibits a wide range of human cancer cell lines, including lung, prostate, breast, skin, melanoma, and renal cancers. Notably, it has also shown efficacy against doxorubicin-resistant ovarian cancer cell lines. The compound was developed and characterized by researchers at South Dakota State University.

Other names
2-acetylamino-3-[4-(2-acetylamino-2-carboxyethylsulfanylthiocarbonylamino)phenylthiocarbamoylsulfanyl]propionic acid
02

Targets

TXNRD2 (Thioredoxin reductase 2)GPX4 (Glutathione peroxidase 4)GSR (Glutathione reductase)GST (Glutathione S-transferase alpha 3)

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