Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine
Publication
, Journal Article
Bergnest, G; Kaddurah-Daouk, R
Published in: Bioorganic and Medicinal Chemistry Letters
April 22, 1997
The first hydrolytically stable phosphocreatine (CrP) analogs with a CH2-P isostere in place of the NH-P linkage have been synthesized and found to inhibit creatine kinase (CK) with potencies in the low mM range. The closest structural analog of CrP, 2, was found to have a K(i) (1.4 mM) near the K(m) of CrP (2.5 mM), making it the most potent known reversible inhibitor of CK.
Duke Scholars
Published In
Bioorganic and Medicinal Chemistry Letters
DOI
ISSN
0960-894X
Publication Date
April 22, 1997
Volume
7
Issue
8
Start / End Page
1021 / 1026
Related Subject Headings
- Medicinal & Biomolecular Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry
Citation
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Chicago
ICMJE
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Bergnest, G., & Kaddurah-Daouk, R. (1997). Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine. Bioorganic and Medicinal Chemistry Letters, 7(8), 1021–1026. https://doi.org/10.1016/S0960-894X(97)00161-3
Bergnest, G., and R. Kaddurah-Daouk. “Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine.” Bioorganic and Medicinal Chemistry Letters 7, no. 8 (April 22, 1997): 1021–26. https://doi.org/10.1016/S0960-894X(97)00161-3.
Bergnest G, Kaddurah-Daouk R. Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine. Bioorganic and Medicinal Chemistry Letters. 1997 Apr 22;7(8):1021–6.
Bergnest, G., and R. Kaddurah-Daouk. “Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine.” Bioorganic and Medicinal Chemistry Letters, vol. 7, no. 8, Apr. 1997, pp. 1021–26. Scopus, doi:10.1016/S0960-894X(97)00161-3.
Bergnest G, Kaddurah-Daouk R. Synthesis and creatine kinase inhibitory activity of nonhydrolyzable analogs of phosphocreatine. Bioorganic and Medicinal Chemistry Letters. 1997 Apr 22;7(8):1021–1026.
Published In
Bioorganic and Medicinal Chemistry Letters
DOI
ISSN
0960-894X
Publication Date
April 22, 1997
Volume
7
Issue
8
Start / End Page
1021 / 1026
Related Subject Headings
- Medicinal & Biomolecular Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry