Synthesis and proteasome inhibition of lithocholic acid derivatives.
Journal Article (Journal Article)
A new class of proteasome inhibitors was synthesized using lithocholic acid as a scaffold. Modification at the C-3 position of lithocholic acid with a series of acid acyl groups yielded compounds with a range of potency on proteasome inhibition. Among them, the phenylene diacetic acid hemiester derivative (13) displayed the most potent proteasome inhibition with IC(50) = 1.9 μM. Enzyme kinetic analysis indicates that these lithocholic acid derivatives are noncompetitive inhibitors of the proteasome.
Full Text
Duke Authors
Cited Authors
- Dang, Z; Lin, A; Ho, P; Soroka, D; Lee, K-H; Huang, L; Chen, C-H
Published Date
- April 1, 2011
Published In
Volume / Issue
- 21 / 7
Start / End Page
- 1926 - 1928
PubMed ID
- 21388808
Pubmed Central ID
- PMC3072167
Electronic International Standard Serial Number (EISSN)
- 1464-3405
Digital Object Identifier (DOI)
- 10.1016/j.bmcl.2011.02.041
Language
- eng
Conference Location
- England