Target intelligence / Profile preview

Human colorectal adenocarcinoma Caco-2 cell viability (Caco-2 viability)

Target
Caco-2 viability
Molecular classification
Cell line, Phenotypic endpoint
01

Overview

The Caco-2 cell line is a continuous line of human epithelial colorectal adenocarcinoma cells (ATCC HTB-37) that serves as a gold-standard in vitro model for the intestinal barrier (Lea, 2015). When cultured, these cells differentiate into a polarized monolayer with microvilli, mimicking the functional characteristics of the small intestinal epithelium, including the expression of various transporters and enzymes (Sambuy et al., 2005). "Human colorectal adenocarcinoma Caco-2 cell viability" is a phenotypic assay endpoint used to measure the survival or growth inhibition of these cells in response to chemical exposure. While frequently listed as a target in bioactivity databases like ChEMBL, it is not a single molecular target but rather a complex biological system used to screen for cytotoxicity or anti-cancer activity (Natoli et al., 2011). In drug development, this endpoint is critical for assessing the safety profile of oral medications and the efficacy of potential chemotherapeutic agents against colorectal cancer. Because viability is a holistic measure, it can be influenced by numerous signaling pathways, including those involved in apoptosis, necrosis, and cell cycle arrest. The use of Caco-2 cells allows researchers to predict human intestinal absorption and identify compounds that may cause gastrointestinal distress. However, the model has limitations, such as the lack of certain metabolic enzymes like CYP3A4, which must be considered when interpreting viability data.

Other names
Caco-2 cell lineCaco-2 cytotoxicityCaco-2 proliferation assayCaco2 viability
02

Mechanism of action

Not applicable; this is a phenotypic measurement of cell health rather than a specific drug-target interaction mechanism.

03

Biological functions

Cell proliferationCell survivalApoptosisIntestinal absorption
04

Disease associations

Colorectal adenocarcinoma
05

Safety considerations

In vitro results may not fully translate to in vivo toxicityCell line heterogeneityLack of major drug-metabolizing enzymes (e.g., CYP3A4) compared to primary tissue
06

Interacting drugs

5-Fluorouracil

2 more in the full profile.

07

Biomarkers

Lactate dehydrogenase (LDH)Adenosine triphosphate (ATP) levelsMTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide)

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