Search results for "ACTH receptor"
showing 4 items of 4 documents
Pharmacological Characterization of Melanocortin Receptors in Fish Suggests an Important Role for ACTH
2005
The melanocortin (MC) receptor subtypes have distinctive characteristic binding profiles. We found that the trout and Fugu MC4 receptors have similar affinity for alpha-MSH and beta-MSH and a much higher affinity for ACTH than does the human MC4 receptor. The Fugu MC1 and the trout and Fugu MC5 receptors also have higher affinity for ACTH-derived peptides than alpha-, beta-, or gamma-MSH. It is tempting to speculate that ACTH-derived peptides may have played an important role as "original" ligands at the MC receptors, while the specificity of the different subtypes for the alpha-, beta-, and gamma-MSH peptides may have appeared at later stages during vertebrate evolution.
The Fundamental Role of Melanocortins in Brain Processes
2003
The discoveries of the latest ten years have shed new light in understanding the roles of melanocortins and their receptors in brain functions and in the development of different pathologies. Since 1992 when genes encoded melanocortin receptor five subtypes were identified, cloned and characterized, the molecular mechanisms underlying different effects such as skin darkening, behaviour, food intake, anti-inflammatory action, analgesia have been clarified. The contribution of melanocortins and their receptors in the physiological control of organism homeostasis has become as the background for the search of agonists and antagonists of separate receptor subtypes, that can be targeted to the m…
New Melanocortin 1 Receptor Binding Motif Based on the C-Terminal Sequence of ?-Melanocyte-Stimulating Hormone
2006
The C-terminal tripeptide of the alpha-melanocyte stimulating hormone (alpha-MSH11-13) possesses strong antiinflammatory activity without known cellular target. In order to better understand the structural requirements for function of such motif, we designed, synthesized and tested out Trp- and Tyr-containing analogues of the alpha-MSH11-13. Seven alpha-MSH11-13 analogues were synthesized and characterized for their binding to the melanocortin receptors recombinantly expressed in insect (Sf9) cells, infected with baculovirus carrying corresponding MC receptor DNA. We also tested these analogues on B16-F1 mouse melanoma cells endogenously expressing the MC1 receptor for binding and for abili…
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…