Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and-1 receptors in linear …

…, W Danho, J Swistok, AWH Cheung, G Kurylko…

Index: Chu, Xin-Jie; Bartkovitz, David; Danho, Waleed; Swistok, Joseph; Cheung, Adrian Wai-Hing; Kurylko, Grazyna; Rowan, Karen; Yeon, Mitch; Franco, Lucia; Qi, Lida; Chen, Li; Yagaloff, Keith Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 22 p. 4910 - 4914

Full Text: HTML

Citation Number: 9

Abstract

Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4- phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assays. This study, together with our earlier report on 5-BrAtc, demonstrated the importance of replacing His6 with phenyl-containing rigid templates in achieving good hMC4R ...

Related Articles:

Aryl extensions of thienopyrimidinones as fibroblast growth factor receptor 1 kinase inhibitors

[Ekkati, Anil R.; Mandiyan, Valsan; Ravindranathan, Krishna P.; Bae, Jae H.; Schlessinger, Joseph; Jorgensen, William L. Tetrahedron Letters, 2011 , vol. 52, # 17 p. 2228 - 2231]

Partly reduced biphenyls as central nervous system agents. 2. cis-and trans-4-Arylcyclohexylamines

[Lednicer,D. et al. Journal of Medicinal Chemistry, 1972 , vol. 15, # 12 p. 1239 - 1243]

More Articles...