Drug intelligence / Profile preview

N-(beta-elemene-13-yl)tryptophan methyl ester

Development stage
Preclinical
Lead developer
Dalian Medical University
Modality
Small Molecules
01

Overview

ETME (N-(β-elemene-13-yl)tryptophan methyl ester) is a novel small molecule derivative of β-elemene, a sesquiterpene extracted from the Chinese medicinal herb *Curcuma wenyujin*. It is being investigated as a sensitizing agent to enhance the therapeutic efficacy of arsenic trioxide (ATO) in solid tumors, particularly hepatocellular carcinoma (HCC). ETME exerts its effects by inducing p53-dependent apoptosis through the mitochondrial pathway, characterized by the upregulation of pro-apoptotic proteins Bax and BID, the downregulation of the anti-apoptotic protein Bcl-2, and the activation of the caspase cascade. Additionally, ETME induces cell cycle arrest at the G2/M phase. Preclinical studies in HCC cell lines and xenograft models have demonstrated that the combination of ETME and ATO synergistically inhibits tumor growth and reduces tumor volume and weight.

Other names
N-(beta-elemene-13-yl)tryptophan methyl ester
02

Targets

CASP3 (Caspase-3)TP53 (Cellular Tumor Antigen p53 R175H)BAX (Apoptosis regulator BAX)BID (BH3 interacting-domain death agonist)CASP (Caspase family)

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