Drug intelligence / Profile preview

wentilactone a

Development stage
Preclinical
Modality
Classical Binding Small Molecules → Small Molecules
01

Overview

**Wentilactone A** is a fungal-derived diterpene isolated from *Aspergillus wentii* with a distinct 6/6/6/5 fused ABCD-ring system and lactone functionalities. It has been characterized as a novel, potent, and selective antitumor agent, especially investigated for its effects against non-small cell lung carcinoma (NSCLC) and small cell lung carcinoma (SCLC) in preclinical studies. Its mechanism involves direct binding to the active, GTP-bound form of HRas, leading to excessive activation of the Ras/Raf/ERK signaling pathway, accumulation of G2/M phase cell cycle arrest, mitochondrial-related apoptosis, and upregulation of p53 and p21. This mechanism is distinct from EGFR inhibitors and suggests potential utility in tumors with HRas-driven mitogenic signaling. In vivo studies demonstrated antitumor efficacy with low observed toxicity[5][6][7].

Other names
76235-83-1UNII-581J1Y5MJ6UNII581J1Y5MJ6UNII 581J1Y5MJ6581J1Y5MJ63H,8H-Furo(2',3',4':4,5)oxireno(7,8)naphtho(2,1-c)pyran-3,8-dione,1a,2,2a,4a,4b,6,9b,9c-octahydro-2-hydroxy-2a,9b-dimethyl-(1aR,2R,2aR,4aR,4bR,9bS,9cS)-
02

Targets

HRAS (H-Ras protein)

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