ReferenceID 379
Statin and rottlerin small-molecule inhibitors restrict colon cancer progression and metastasis via MACC1
PLoS Biol
MACC1 (Metastasis Associated in Colon Cancer 1) is a key driver and prognostic biomarker for cancer progression and metastasis in a large variety of solid tumor types, particularly colorectal cancer (CRC). However, no MA
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Record Fields
Scalar fields from the final reference record.
- Reference Id
- 379
- Evidence Id
- 16969
- Core Evidence Id
- 16969
- Source Reference Id
- 735
- Herb2 Reference Id
- HBREF001267
- Subject Paper Key
- HBIN042467_28570591
- Pubmed Id
- 28570591
- Doi
- 10.1371/journal.pbio.2000784
- Paper Title
- Statin and rottlerin small-molecule inhibitors restrict colon cancer progression and metastasis via MACC1
- Paper Abstract
- MACC1 (Metastasis Associated in Colon Cancer 1) is a key driver and prognostic biomarker for cancer progression and metastasis in a large variety of solid tumor types, particularly colorectal cancer (CRC). However, no MACC1 inhibitors have been identified yet. Therefore, we aimed to target MACC1 expression using a luciferase reporter-based high-throughput screening with the ChemBioNet library of more than 30,000 compounds. The small molecules lovastatin and rottlerin emerged as the most potent MACC1 transcriptional inhibitors. They remarkably inhibited MACC1 promoter activity and expression, resulting in reduced cell motility. Lovastatin impaired the binding of the transcription factors c-Jun and Sp1 to the MACC1 promoter, thereby inhibiting MACC1 transcription. Most importantly, in CRC-xenografted mice, lovastatin and rottlerin restricted MACC1 expression and liver metastasis. This is-to the best of our knowledge-the first identification of inhibitors restricting cancer progression and metastasis via the novel target MACC1. This drug repositioning might be of therapeutic value for CRC patients.
- Journal
- PLoS Biol
- Publish Year
- 2017
- Experiment Subject
- crc-xenografted mice
- Experiment Type
- Animal Experiment
- Phenotype Related
- Paper Title Cn
- Paper Title En
- Statin and rottlerin small-molecule inhibitors restrict colon cancer progression and metastasis via MACC1
- Bilingual Status
- semi_complete