Diacylglycerols with lipophilically equivalent branched acyl chains display high affinity for protein kinase C (PK-C). A direct measure of the effect of constraining the glycerol backbone in DAG lactones

Bioorganic and Medicinal Chemistry Letters

Volumn 10, Issue 7, 2000, Pages 653-655

  Nacro, Kassoum ^a   Bienfait, Bruno ^a   Lewin, Nancy E ^a   Blumberg, Peter M ^a   Marquez, Victor E ^a  

^a NATIONAL INSTITUTES OF HEALTH   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

DIACYLGLYCEROL; DIACYLGLYCEROL DERIVATIVE; LACTONE; LIGAND; PROTEIN KINASE C;

ARTICLE; BINDING AFFINITY; CHEMICAL MODIFICATION; DRUG STRUCTURE; ENZYME BINDING; LIPOPHILICITY; STRUCTURE ANALYSIS;

DIGLYCERIDES; ENZYME ACTIVATORS; GLYCEROL; LACTONES; LIGANDS; PROTEIN KINASE C; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0034599717     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(00)00070-6     Document Type: Article

References (17)

1. Nishizuka, Y. Nature 1988, 334, 661.
2. Nishizuka, Y. Science 1992, 258, 607.
3. Newton, A. C. Curr. Biol. 1995, 5, 973.
4. Quest, A. F. Enzyme Protein 1996, 49, 231.
5. Hurley, J. H.; Gobler, J. A. Curr. Opin. Struct. Biol. 1997, 7, 557.
6. Sakai, N.; Sasaki, K.; Ikegaki, N.; Shirai, Y.; Ono, Y.; Saito, N. J. Cell Biol. 1997, 139, 1465.
7. Van Lint, J.; Sinnett Smith, J.; Rozengurt, E. J. Biol. Chem. 1995, 270, 1455.
8. Caloca, M. J.; Garcia-Bermejo, M. L.; Blumberg, P. M.; Lewin, N. E.; Kremmer, E.; Mischak, H.; Wang, S.; Nacro, K.; Bienfait, B.; Marquez, V. E.; Kazanietz, M. G. Proc. Natl. Acad. Sci. USA 1999, 96, 11854.
9. Ebinu, J. O.; Bottorff, D. A.; Chan, E. Y. W.; Stang, S. L.; Dunn, R. J.; Stone, J. C. Science 1998, 280, 1082.
10. Kazanietz, M. G.; Lewin, N. E.; Bruns, J. D.; Blumberg, P. M. J. Biol. Chem. 1995, 270, 10777.
11. Marquez, V. E.; Nacro, K.; Benzaria, S.; Lee, J.; Sharma, R.; Teng, K.; Milne, G. W. A.; Bienfait, B.; Wang, S.; Lewin, N. E.; Blumberg, P. M. Pharmacol Ther. 1999, 82, 251.
12. Nacro, K.; Bienfait, B.; Lee, J.; Han, K.-C; Kang, J.-H.; Benzaria, S.; Lewin, N. E.; Bhattacharyya, D. K.; Blumberg, P. M.; Marquez, V. E. J. Med. Chem. (in press).
13. Sharma, R.; Lee, J.; Wang, S.; Milne, G. W. A.; Lewin, N. E.; Blumberg, P. M.; Marquez, V. E. J. Med. Chem. 1996, 39, 19.
14. Lee, J.; Wang, S.; Milne, G. W. A.; Sharma, R.; Lewin, N. E.; Blumberg, P. M.; Marquez, V. E. J. Med. Chem. 1996, 39, 29.
15. Lee, J.; Sharma, R.; Wang, S.; Milne, G. W. A.; Lewin, N. E.; Szallasi, Z.; Blumberg, P. M.; George, C.; Marquez, V. E. J. Med. Chem. 1996, 39, 36.
16. Meylan, W. M.; Howard, P. H. J. Pharm. Sci. 1995, 84, 83, KOWWIN 1.63, Syracuse Research Corp., http://esc.syrres.com/
17. Leo, A.; Hansch, C.; Elkins, D. Chem. Rev. 1971, 71, 525.