Chenodeoxycholic Acid, Free Acid and its 7β-isomer ursodeoxycholic acid (sc-204935), are potent (nanomolar affinity) selective inhibitors of DD2 (AKR1C2). These compounds were non-competitive inhibitors of AKR1D1 yielding Ki values of 3.2 μM for chenodeoxycholic acid. This chemical is a hydrophobic primary bile acid, which increases intracellular Ca2+ in rat hepatocyte couplets. Studies indicate that Chenodeoxycholic Acid induces apoptosis through a PKC dependent pathway. It is known that Chenodeoxycholic Acid is essential in the metabolism of cholesterol via activation of nuclear receptors. This bile acid can also bind to BABP with a stoichiometery of 1:2. Alternate studies indicate that chenodeoxycholic acid can inhibit the expression of IL-6 and cell viability in QBC939 cells.
1. McNeilly, A.D., et al. 2010. J. Hepatol. 52: 705-711. PMID: 20347173
2. Wang, J., et al. 2010. Zhonghua Wai Ke Za Zhi. 48(: 919-923. PMID: 21055228
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