Synthesis and proteasome inhibition of lithocholic acid derivatives.
Publication
, Journal Article
Dang, Z; Lin, A; Ho, P; Soroka, D; Lee, K-H; Huang, L; Chen, C-H
Published in: Bioorg Med Chem Lett
April 1, 2011
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.
Duke Scholars
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
April 1, 2011
Volume
21
Issue
7
Start / End Page
1926 / 1928
Location
England
Related Subject Headings
- Proteasome Inhibitors
- Proteasome Endopeptidase Complex
- Protease Inhibitors
- Medicinal & Biomolecular Chemistry
- Lithocholic Acid
- Kinetics
- Humans
- Hela Cells
- HeLa Cells
- 3405 Organic chemistry
Citation
APA
Chicago
ICMJE
MLA
NLM
Dang, Z., Lin, A., Ho, P., Soroka, D., Lee, K.-H., Huang, L., & Chen, C.-H. (2011). Synthesis and proteasome inhibition of lithocholic acid derivatives. Bioorg Med Chem Lett, 21(7), 1926–1928. https://doi.org/10.1016/j.bmcl.2011.02.041
Dang, Zhao, Andrew Lin, Phong Ho, Dominique Soroka, Kuo-Hsiung Lee, Li Huang, and Chin-Ho Chen. “Synthesis and proteasome inhibition of lithocholic acid derivatives.” Bioorg Med Chem Lett 21, no. 7 (April 1, 2011): 1926–28. https://doi.org/10.1016/j.bmcl.2011.02.041.
Dang Z, Lin A, Ho P, Soroka D, Lee K-H, Huang L, et al. Synthesis and proteasome inhibition of lithocholic acid derivatives. Bioorg Med Chem Lett. 2011 Apr 1;21(7):1926–8.
Dang, Zhao, et al. “Synthesis and proteasome inhibition of lithocholic acid derivatives.” Bioorg Med Chem Lett, vol. 21, no. 7, Apr. 2011, pp. 1926–28. Pubmed, doi:10.1016/j.bmcl.2011.02.041.
Dang Z, Lin A, Ho P, Soroka D, Lee K-H, Huang L, Chen C-H. Synthesis and proteasome inhibition of lithocholic acid derivatives. Bioorg Med Chem Lett. 2011 Apr 1;21(7):1926–1928.
Published In
Bioorg Med Chem Lett
DOI
EISSN
1464-3405
Publication Date
April 1, 2011
Volume
21
Issue
7
Start / End Page
1926 / 1928
Location
England
Related Subject Headings
- Proteasome Inhibitors
- Proteasome Endopeptidase Complex
- Protease Inhibitors
- Medicinal & Biomolecular Chemistry
- Lithocholic Acid
- Kinetics
- Humans
- Hela Cells
- HeLa Cells
- 3405 Organic chemistry