Drug intelligence / Profile preview

nemorosone

Development stage
Preclinical
Lead developer
German Cancer Research Center
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) isolated from the flower resin of *Clusia rosea*. It is being investigated as a potential anti-cancer lead compound, particularly for chemoresistant pancreatic cancer. Its mechanism of action involves the induction of endoplasmic reticulum (ER) stress and the activation of the unfolded protein response (UPR) pathway, specifically through the up-regulation of GADD153 (DDIT3). This leads to rapid depletion of ER calcium stores, depolarization of the mitochondrial membrane, and subsequent activation of the intrinsic apoptotic pathway. Unlike its structural relative hyperforin, nemorosone does not significantly induce CYP3A4 expression, suggesting a lower risk for drug-drug interactions in combination therapy settings.

02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)CASP3 (Caspase-3)MAPK3 (Mitogen-activated protein kinase 1)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)SLC7A11 (Cystine-Glutamate Antiporter)CDKN1A (Cyclin-dependent kinase inhibitor 1A)DDIT3 (DNA damage-inducible transcript 3 protein)

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