Molecular modeling study of species-selective peroxisome proliferator-activated receptor (PPAR) αagonist; possible mechanism(s) of human PPARα selectivity of an α-substituted phenylpropanoic acid derivative (KCL)

Chemical and Pharmaceutical Bulletin

Volumn 52, Issue 3, 2004, Pages 365-367

  Uchiki, Hideharu ^a   Miyachi, Hiroyuki ^a  

^a KYORIN PHARMACEUTICAL CO LTD   (Japan)

Author keywords

KCL; Molecular modeling; Mutation; Peroxisome proliferator activated receptor (PPAR) ; Species selectivity

Indexed keywords

GW 409544; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONIST; PHENYLPROPIONIC ACID DERIVATIVE; PIRINIXIC ACID; UNCLASSIFIED DRUG; CELL RECEPTOR; TRANSCRIPTION FACTOR;

AMINO ACID SEQUENCE; ARTICLE; BINDING AFFINITY; COMPUTER AIDED DESIGN; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG SPECIFICITY; DRUG STRUCTURE; HYDROPHOBICITY; MOLECULAR MODEL; PROTEIN DOMAIN; PROTEIN STRUCTURE; STRUCTURE ACTIVITY RELATION; ANIMAL; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DRUG EFFECT; DRUG POTENTIATION; HUMAN; METABOLISM; PHYSIOLOGY; RAT; SPECIES DIFFERENCE; TRANSACTIVATION;

ANIMALS; HUMANS; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PHENYLPROPIONATES; RATS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; SPECIES SPECIFICITY; STRUCTURE-ACTIVITY RELATIONSHIP; TRANS-ACTIVATION (GENETICS); TRANSCRIPTION FACTORS;

EID: 4544292919     PISSN: 00092363     EISSN: 13475223     Source Type: Journal    
DOI: 10.1248/cpb.52.365     Document Type: Article

References (17)

1. Porte D., Jr., Schwartz M. W., Science, 272, 699-700 (1996).
2. Staels B., Auwerx J., Curr. Pharmaceut. Des., 3, 1-14 (1997).
3. Staels B., Dallongeville J., Auwerx J., Schoonjans E., Leitersdorf E., Fruchart J.-C., Circulations, 98, 2088-2093 (1998).
4. Fruchart J.-C., Duriez P., Staels B., Curr. Opin. Lipidol., 10, 245-257 (1999).
5. Forman B. M., Chen J., Evans R. M., Proc. Natl. Acad. Sci. U.S.A., 94, 4312-4317 (1997).
6. Nomura M., Takahashi Y., Tanase T., Miyachi H., Ide T., Tsunoda M., Murakami K., PCT Int. Appl. WO 00/75103.
7. Miyachi H., Nomura M., Tanase T., Takahashi Y., Ide T., Tsunoda M., Murakami K., Awano K., Bioorg. Med. Chem. Lett., 12, 77-80 (2002).
8. Miyachi H., Nomura M., Tanase T., Suzuki M., Murakami K., Awano K., Bioorg. Med. Chem. Lett., 12, 333-335 (2002).
9. Nomura M., Tanase T., Ide T., Tsunoda M., Suzuki M., Uchiki H., Murakami K., Miyachi H., J. Med. Chem., 46, 3581-3599 (2003).
10. Murakami K., Nagasawa M., Suzuki M., First International Symposium on PPARs: From Basic Science To Clinical Applications, 2001.
11. Miyachi H., Uchiki H., Bioorg. Med. Chem. Lett., 13, 3145-3149 (2003).
12. Xu H. E., Stanley T. B., Montana V. G., Lambert M. H., Shearer B. G., Cobb J. E., McKee D, D., Galardi C. M., Plunket K. D., Nolte R. D., Parks D. J., Moore J. T., Kliewer S. A., Willson T. M., Stimmel J. B., Nature (London), 415, 813-817 (2002).
13. Keller H., Devchand P. R., Perround M., Wali W., Biol. Chem., 378, 651-655 (1997).
14. Brown P. J., Wineger D. A., Plunket K. D., Moor L. B., Lewis M. C., Wilson J. G., Sundseth S. S., Coble C. S., Wu Z., Chapman J. M., Lehmann J. M., Kliewer S. A., Willson T. M., J. Med. Chem., 42, 3785-3788 (1999).
15. Takeda I., Yu R. T., Xu H. E., Lambert M. H., Montana V. G., Kliewer S. A., Evans R. M., Umesono K., Mol. Endocrinol., 14, 733-740 (2000).
16. Willson T. M., Brown T. J., Sternbach D. D., Henke B. R., J. Med. Chem., 43, 527-550 (2000).
17. Iwata Y., Miyamoto S., Takamura M., Yanagisawa H., Kasuya A., J. MolGraphics Modell., 19, 536-542 (2001).