Drug intelligence / Profile preview

heteronemin

Development stage
Preclinical
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

**Heteronemin** is a marine sesterterpenoid-type natural product isolated primarily from sponges (such as Hippospongia sp. and Hyrtios sp.). It possesses potent antitumor activities, including anticancer, antitubercular, and anti-inflammatory effects[6][1][4][5][10]. Heteronemin induces cell apoptosis and autophagy in multiple cancer cell types (e.g., prostate cancer, cholangiocarcinoma, acute myeloid leukemia, hepatocellular carcinoma), mainly by targeting several molecular pathways: it serves as a *topoisomerase II catalytic inhibitor*, inhibits the N-terminal ATP-binding pocket of *heat shock protein 90 (Hsp90)*, and activates *protein tyrosine phosphatases (PTP)*[1][10][3]. It also leads to mitochondrial dysfunction, oxidative and ER stresses, reactive oxygen species (ROS) generation, cell cycle arrest, and pronounced apoptosis via caspase activation, often in a dose-dependent manner[1][3][5][10]. Heteronemin suppresses expression and proliferative signaling via *PD-L1*, inhibits *MAPK pathway* kinases (ERK, JNK, p38), and has effects mediated via *integrin αvβ3* interaction[4][5][3][7][9]. Preclinical studies support its potential for clinical development as an anticancer agent.

Other names
heteronemin62008-04-25'α,16β-Diacetoxy-5',17aα-dihydro-4,4,8-trimethyl-D-homo-5α-androstano[17,17a-c]furan-12β-olChryseno[1,2-c]furan-1,4,13-triol, 1,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a,13b-octadecahydro-5b,8,8,11a,13a-pentamethyl-, 1,4-diacetate, (1S,4S,5aS,5bR,7aS,11aS,11bR,13R,13aS,13bR)[(1S,4S,5aS,5bR,7aS,11aS,11bR,13R,13aS,13bR)-1-acetyloxy-13-hydroxy-5b,8,8,11a,13a-pentamethyl-1,4,5,5a,6,7,7a,9,10,11,11b,12,13,13b-tetradecahydrophenanthro[2,1-e][2]benzofuran-4-yl] acetate
02

Targets

TOP1 (DNA Topoisomerase I)HSP90AA1 (Heat shock protein HSP90-alpha)TOP2A (DNA topoisomerase II)FTase (Protein Farnesyltransferase)

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