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Ref Type Journal Article
PMID (26515494)
Authors Wang X, Zhang C, Yan X, Lan B, Wang J, Wei C, Cao X, Wang R, Yao J, Zhou T, Zhou M, Liu Q, Jiang B, Jiang P, Kesari S, Lin X, Guo F
Title A Novel Bioavailable BH3 Mimetic Efficiently Inhibits Colon Cancer via Cascade Effects of Mitochondria.
Journal Clinical cancer research : an official journal of the American Association for Cancer Research
Vol 22
Issue 6
Date 2016 Mar 15
Abstract Text Gossypol and its analogs, through their ability to bind to and inactivate BH3 domain-containing antiapoptotic proteins, have been shown to inhibit the growth of various human cancer cells in culture and xenograft models. Here, we evaluated the antitumor efficacy of a novel gossypol derivative and BH3 mimetic ch282-5 (2-aminoethanesulfonic acid sodium-gossypolone) in colon cancer models. Several innovative combination strategies were also explored and elaborated.Ch282-5 was synthesized by modifying the active aldehyde groups and R groups of gossypol according to a computer-aided drug design program. The stability of ch282-5 was examined by high-performance liquid chromatography, and cytotoxic effects of ch282-5 on colon cancer cells were assessed by MTS assay. Activation of mitochondrial apoptotic pathway by ch282-5 was evidenced with a series of molecular biology techniques. In vivo antitumor activity of ch282-5 and its combination with chloroquine, rapamycin, oxaliplatin, and ABT-263 was also evaluated in colon cancer xenograft models and experimental liver metastasis models.Ch282-5 showed antiproliferative and pro-cell death activity against colon cancer cells both in vitro and in vivo, and the response to the drug correlated with inhibition of antiapoptotic Bcl-2 proteins, induction of mitochondria-dependent apoptotic pathway, and disruption of mitophagy and mTOR pathway. Ch282-5 also suppressed liver metastasis produced by intrasplenic injection of colon cancer cells. Furthermore, ch282-5 could potentiate the effectiveness of oxaliplatin and rescue ABT-263 efficacy by downregulation of Mcl-1 and elevation of platelet number.These findings provide a rational basis for clinical investigation of this highly promising BH3 mimetic in colon cancer.


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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Ch282-5 Ch282-5 2 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
Ch282-5 BCL2 Family Inhibitor 6 Ch282-5 is a gossypol derivative that binds to and inhibits BCL2, family proteins, resulting in decreased tumor cell growth and increased sensitivity to chemotherapeutic agents (PMID: 26515494, PMID: 29885833).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown colon cancer not applicable Ch282-5 Preclinical - Cell line xenograft Actionable In a preclinical study, ch282-5 induced apoptosis and inhibited growth and migration of several human and mouse colon cancer cell lines in culture, and inhibited tumor growth and metastasis in xenograft models (PMID: 26515494). 26515494
Unknown unknown colon cancer not applicable Ch282-5 + Oxaliplatin Preclinical - Cell line xenograft Actionable In a preclinical study, the combination of ch282-5 and Eloxatin (oxaliplatin) inhibited cell growth in human and mouse colon cancer cell lines in culture, and the combination synergized to inhibit tumor growth in mouse colon cancer cell line xenograft models (PMID: 26515494). 26515494
Unknown unknown Advanced Solid Tumor not applicable Ch282-5 Preclinical Actionable In a preclinical study, ch282-5 inhibited growth of a variety of human solid tumor cell lines in culture (PMID: 26515494). 26515494