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New dimeric cGMP analogues reduce proliferation in three colon cancer cell lines
- Publication Year :
- 2017
-
Abstract
- Activation of the cGMP-dependent protein kinase G (PKG) can inhibit growth and/or induce apoptosis in colon cancer. In this study we evaluated the effects on cell viability, cell death and proliferation of novel dimeric cGMP analogues, compared to a monomeric compound. Three colon cancer cell lines, which only express isoform 2 of PKG, were treated with these novel cGMP analogues and responded with increased PKG activity. cGMP analogues reduced cell viability in the three cell lines and this was due to a cytostatic rather than cytotoxic effect. These findings suggest that activation of PKG2 can be a therapeutic target in the treatment of colon cancer and, most importantly, that dimeric cGMP analogues can further improve the beneficial effects previously observed with monomeric cGMP analogues.
- Subjects :
- 0301 basic medicine
Programmed cell death
Cell Survival
Antineoplastic Agents
Apoptosis
Structure-Activity Relationship
03 medical and health sciences
0302 clinical medicine
Cell Line, Tumor
Drug Discovery
Humans
Cytotoxic T cell
Viability assay
Cyclic GMP
Cell Proliferation
Pharmacology
Dose-Response Relationship, Drug
Molecular Structure
Chemistry
Cell growth
Organic Chemistry
General Medicine
3. Good health
Cell biology
030104 developmental biology
Caco-2
Cell culture
030220 oncology & carcinogenesis
cGMP
HCT 116
HT-29
PKG2
VASP
Dimerization
Drug Screening Assays, Antitumor
Drug Discovery3003 Pharmaceutical Science
Cancer research
cGMP-dependent protein kinase
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....f6720cc7ef5afc701848d11538e57aa8