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Drug intelligence / Profile preview
cholic acid 7-sulfate
- Development stage
- Preclinical
- Lead developer
- Harvard University
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Cholic acid 7-sulfate (CA7S) is an endogenous, gut-restricted sulfated bile acid metabolite produced in the liver by the sulfotransferase SULT2A1. It acts as a potent and selective agonist of the G-protein coupled bile acid receptor 1 (GPBAR1, also known as TGR5) and as an endogenous ligand for the MHC class I-related protein (MR1). By agonizing GPBAR1 on enteroendocrine L cells, cholic acid 7-sulfate stimulates the secretion of glucagon-like peptide-1 (GLP-1), which enhances insulin secretion and improves systemic glucose tolerance, making it an investigational candidate for the treatment of type 2 diabetes and obesity. Additionally, cholic acid 7-sulfate binds to MR1 to promote the survival and homeostatic function of mucosal-associated invariant T (MAIT) cells. In the context of oncology, SULT2A1-derived cholic acid 7-sulfate has been shown to activate GPBAR1 on CD8+ T cells, enhancing their cytotoxicity via CREB-IL-2Rβ-mTORC1 signaling and synergizing with anti-PD-1 immunotherapy to inhibit hepatocellular carcinoma progression.
- Other names
- 7-sulfocholate7-sulfocholic acid7-sulphocholatCA7SCA-7SCA 7Scholic acid-7-sulfate
02
Targets
GPBAR1MR1 (Thioesterase PNKD)
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