PD 165929 - The first high affinity non-peptide neuromedin-B (NMB) receptor selective antagonist

Bioorganic and Medicinal Chemistry Letters

Volumn 6, Issue 21, 1996, Pages 2617-2622

  Eden, J M ^a   Hall, M D ^a   Higginbottom, M ^a   Horwell, D C ^a   Howson, W ^a   Hughes, J ^a   Jordan, R E ^a   Lewthwaite, R A ^a   Martin, K ^a   McKnight, A T ^a   O'Toole, J C ^a   Pinnock, R D ^a   Pritchard, M C ^a   Suman Chauhan, N ^a   Williams, S C ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BOMBESIN; BOMBESIN DERIVATIVE; CHLORIDE CHANNEL; GASTRIN RELEASING PEPTIDE; GASTRIN RELEASING PEPTIDE RECEPTOR; NEUROMEDIN B; NEUROMEDIN B RECEPTOR; NEUROPEPTIDE RECEPTOR; OLIGOPEPTIDE; PD 165929; UNCLASSIFIED DRUG;

AMINO ACID COMPOSITION; ANIMAL CELL; ANIMAL TISSUE; ARTICLE; CHO CELL; CONTROLLED STUDY; DRUG DESIGN; DRUG RECEPTOR BINDING; DRUG SYNTHESIS; FROG; GENE EXPRESSION; HUMAN; NONHUMAN; OLFACTORY BULB; OOCYTE; QUANTITATIVE STRUCTURE ACTIVITY RELATION; RAT;

ANIMALIA; ANURA;

EID: 2242427578     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/0960-894X(96)00481-7     Document Type: Article

References (20)

1. 1. Burgaud, B.G.M.; Horwell, D.C.; Pritchard, M.C.; Bernad, N.; Martinez, J. Tetrahedron: Asymmetry 1995, 6, 1081.
2. 2. Horwell, D.C.; Hughes, J.; Hunter, J.C.; Pritchard, M.C.; Richardson, R.S.; Roberts, E.; Woodruff, G.N. J. Med. Chem. 1991, 34, 404.
3. 3. See Boden, P.; Eden, J. M.; Hodgson, J.; Horwell, D. C.; Pritchard, M. C.; Raphy, J.; Suman-Chauhan, N. Bioorg. Med. Chem. Lett. 1995, 5, 1773 and references cited therein.
4. 4. For a recent review of this work see Horwell, D. C. Trends Biotechnol. 1995, 13, 132.
5. 5. For a more detailed description of the peptoid design strategy see Boyle, S.; Guard, S.; Hodgson, J.; Horwell, D. C.; Howson, W.; Hughes, J.; McKnight, A.; Martin, K.; Pritchard, M. C.; Watling, K. J.; Woodruff, G. N. Bioorg. Med. Chem. 1994, 2, 101.
6. 6. In accordance with Ariens and Farmers' "three ligand hypothesis" Farmer, P. S.; Ariens, E. J.; Trends Pharmacol. Sci. 1982, 5, 362.
7. 7. See Chapter 2 in Dutta, A. S. Small Peptides : Chemistry, Biology and Clinical Studies, (1993) Pharmacochemistry Library Vol. 19 (Timmerman, H., ed), Elsevier.
8. 8. Battey, J.; Wada, E. Trends Neurosci. 1991, 14, 524.
9. 9. For a review of biological actions see Lebacq-Verheyden, A.; Trepel, J.; Sausville, E.; Battey, J. Handbook of Experimental Pharmacology 1990, 95 (Part II), 71.
10. 10. Jensen, R. T.; Coy, D. H.; Trends Pharmacol. Sci. 1991, 12, 13.
11. 11. The structures of relatively low affinity non-peptide bombesin ligands have been disclosed: Valentine, J. J.; Nakanishi, S.; Hageman, D. L.; Snider, R. M.; Spencer, R. W.; Vinick, F. J. Bioorg. Med. Chem. Lett. 1992, 2, 333 and Mihara, S.; Hara, M.; Nakamura, M.; Sakurawi, K.; Tokura, K.; Fujimoto, M.; Fukai, T.; Nomura, T. Biochem. Biophys. Res. Comm. 1995, 213, 594.
12. 11. The structures of relatively low affinity non-peptide bombesin ligands have been disclosed: Valentine, J. J.; Nakanishi, S.; Hageman, D. L.; Snider, R. M.; Spencer, R. W.; Vinick, F. J. Bioorg. Med. Chem. Lett. 1992, 2, 333 and Mihara, S.; Hara, M.; Nakamura, M.; Sakurawi, K.; Tokura, K.; Fujimoto, M.; Fukai, T.; Nomura, T. Biochem. Biophys. Res. Comm. 1995, 213, 594.
13. 12. Broccardo, M.; Falconieri Erspamer, G.; Melchiorri, P.; Negri, L.; De Castiglione, R. Br. J. Pharmacol. 1975, 55, 221.
14. 13. Horwell, D. C.; Howson, W.; Naylor, D.; Osborne, S.; Pinnock, R. D.; Ratcliffe, G. S.; Suman-Chauhan Int. J. Pept. Prot. Res. (in press).
15. 13 is a non-conserved residue within the bombesin family of peptides being Phe in the equivalent position in the NMB sequence. Leu is present in both bombesin and GRP.
16. 15. Suman-Chauhan, N.; Hall, M.; Franks, R.; Webdale, L.; Chilvers, H.; Pinnock, R. D.; Woodruff, G. N. Br. J. Pharmacol. 1995, 116, 22P.
17. 16. Horwell, D. C.; Ratcliffe, G.; Roberts, E. Bioorg. Med. Chem. Lett. 1991, 1, 169.
18. 17. Guard, S.; Watling, K. J.; Howson, W. Eur. J. Pharmacol. 1993, 240, 177.
19. 18. Pinnock, R. D.; Suman-Chauhan, N.; Hall, M.; Webdale, L.; Franks, R.; Chilvers, H.; McKnight, A. T.; Daum, P.; Woodruff, G. N. Br. J. Pharmacol. 1995, 116, 23P.
20. 19. Pinnock, R. D.; Woodruff, G. N.; Holland, S.; Hall, M. D. J. Physiol. (in press).