Drug intelligence / Profile preview

yangonin

Development stage
Preclinical
Lead developer
University of California, Irvine
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Yangonin is a major kavalactone constituent derived from the kava plant (*Piper methysticum*). It has been investigated for its potential anticancer and chemopreventive properties, particularly in the context of bladder cancer. The compound's mechanism of action involves the induction of autophagy and the inhibition of the mTOR (mammalian target of rapamycin) signaling pathway. Specifically, yangonin promotes the formation of the TSC1/TSC2 complex, which leads to decreased phosphorylation of mTOR and 4E-BP1, thereby halting translation initiation. Preclinical research has demonstrated that yangonin can act synergistically with other kava-derived compounds, such as the chalcone flavokawain A, to inhibit tumor cell growth and anchorage-independent colony formation.

Other names
4-methoxy-6-[(E)-2-(4-methoxyphenyl)ethenyl]pyran-2-one
02

Targets

CNR1 (Cannabinoid receptor 1)GABRR (GABA-A receptor subunit rho)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)mTOR (Mammalian target of rapamycin kinase)MAOB (Monoamine oxidase B)MAOA (Monoamine oxidase A)

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