0000000000543776
AUTHOR
Hajime Watanobe
showing 2 related works from this author
Subtype selective binding properties of substituted linear melanocyte stimulating hormone analogues
2002
The melanocortin receptors are peptide binding G-protein coupled receptors that play a role in important physiological functions such as energy balance, inflammatory processes and several aspects of reproduction. In this study, we synthesised 11 new linear MSH analogues and tested their binding to the human MC receptors (MC1, MC3, MC4 and MC5) expressed in COS cells. Our results show that introduction of Asp in position 4 similarly affects the binding to the MC1, MC4 and MC5 receptors, but drastically lowers the binding to the MC3 receptor. Arg(5) substitution shows relatively high affinity for the MC4 receptor, while the results also give further support for specific importance of His(6) f…
Pharmacological comparison of rat and human melanocortin 3 and 4 receptors in vitro.
2002
Abstract The melanocortin 3 and 4 receptors are G-protein-coupled receptors found in the hypothalamus with important role in regulation of the energy balance. In this study, we performed pharmacological comparison of the rat and human melancortin (MC) 3 and MC4 receptors. We transiently expressed the genes for these receptors individually in a mammalian cell line and determined the binding affinities to several MSH peptides. The results showed no major difference between the rat and human MC3 receptors while the rat MC4 receptor had higher affinity to several peptides compared with the human MC4 receptor. NDP-, α-, β-, γ-MSH, ACTH(1–24), HS014 and MTII had from 5- to 34-fold higher affinity…