Analogs of sub-nanomolar hMC1R agonist LK-184 [Ph(CH2) 3CO-His-D-Phe-Arg-Trp-NH2]. An additional binding site within the human melanocortin receptor 1?

Bioorganic and Medicinal Chemistry Letters

Volumn 14, Issue 15, 2004, Pages 3997-4000

  Koikov, L N ^a,c   Ebetino, F H ^b   Solinsky, M G ^b   Cross Doersen, D ^b   Knittel, J J ^a  

^a UNIVERSITY OF CINCINNATI   (United States)

^b PROCTER AND GAMBLE PHARMACEUTICALS   (United States)

^c UNIVERSITY OF CONNECTICUT   (United States)

Author keywords

Melanocortin agonists

Indexed keywords

LK 184; LK 394; MELANOCORTIN 1 RECEPTOR; NANOPARTICLE; TETRAPEPTIDE; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ARTICLE; BINDING SITE; CONTROLLED STUDY; DRUG POTENCY; DRUG POTENTIATION; HUMAN; RECEPTOR BINDING;

BINDING SITES; HUMANS; KINETICS; OLIGOPEPTIDES; RECEPTOR, MELANOCORTIN, TYPE 1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 3042636196     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.05.039     Document Type: Article

References (17)

1. Cone R.D. The Melanocortin Receptors. 2000;Humana, Totowa
2. Wikberg J.E.S. Eur. J. Pharm. 375:1999;295
3. Koikov, L. N.; Knittel, J. J.; Solinsky, M. G.; Cross-Doersen, D.; Ebetino F. H. Abstracts of Papers, 224 National Meeting of the American Chemical Society, Boston, MA; American Chemical Society: Washington, DC, 2002; Abstract 337
4. Koikov L.N., Knittel J.J., Solinsky M.G., Cross-Doersen D., Ebetino F.H. Bioorg. Med. Chem. Lett. 13:2003;2647
5. King H. J. Chem. Soc. 115:1919;476
6. Haskell-Luevano C., Sawyer T.K., Trumpp-Kallmayer S., Bikker J.A., Humblet C., Gantz I., Hruby V.J. Drug Des. Discov. 14:1996;197
7. Prusis P., Frandberg P.-A., Muceniece R., Kalvinsh I., Wikberg J.E.S. Biochem. Biophys. Res. Commun. 210:1995;205
8. Prusis P., Schioth H.B., Muceniece R., Herzyk P., Asfar M., Hubbard R.E., Wikberg J.E.S. J. Mol. Graphics Mod. 15:1997;307
9. Schioth H.B., Yook P., Muceniece R., Wikberg J.E.S., Szardenings M. Mol. Pharmacol. 54:1998;154
10. Schioth H.B., Fredriksson A., Carlson C., Yook P., Muceniece R., Wikberg J.E.S. Mol. Cell. Endocrinol. 139:1998;109
11. Hruby V.J., Wilkes B.C., Hadley M.E., Al-Obeidi F., Sawyer T.K., Staples D.J., DeVaux A., Dym O., Castrucci A.M., Hintz M.F., Riehm J.P., Rao K.R. J. Med. Chem. 30:1987;2126
12. Haskell-Luevano C., Sawyer T.K., Hendrata S., North C., Panahinia L., Stum M., Staples D.J., Castrucci A.M., Hadley M.E., Hruby V.J. Peptides. 17:1996;995
13. Sahm U.G., Oliver G.W.J., Branco S.K., Moss S.H., Pouton C.W. Peptides. 15:1994;1297
14. Sahm U.G., Quarawi M.A., Oliver G.W.J., Ahmed A.R.H., Moss S.H., Pouton C.W. FEBS Lett. 350:1994;29
15. Bednarek M.A., Silva M.V., Arison B., MacNeil T., Kalyani R.N., Huang R.-R.C., Weinberg D.H. Peptides. 20:1999;401
16. Bednarek M.A., MacNeil T., Kalyani R.N., Tang R., Van der Ploeg L.H.T., Weinberg D.H. Biochem. Biophys. Res. Commun. 261:1999;209
17. Holder J.R., Xiang Z., Bauzo R., Haskell-Luevano C. J. Med. Chem. 45:2002;5736