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- W2321825042 abstract "When establishing the physiological roles of specific receptors in normal and disease states, it is critical to have selective antagonist ligands for each receptor in a receptor system with several subtypes. The melanocortin receptors have five subtypes referred to as the melanocortin 1 receptor, melanocortin 2 receptor, melanocortin 3 receptor, melanocortin 4 receptor and melanocortin 5 receptor, and they are of critical importance for many aspects of human health and disease.This article reviews the current efforts to design selective antagonistic ligands for the five human melanocortin receptors summarizing the currently published orthosteric and allosteric antagonists for each of these receptors.Though there has been progress, there are still few drugs available that address the many significant biological activities and diseases that are associated with these receptors, which is possibly due to the lack of receptor selectivity that these designed ligands are currently showing. The authors believe that further studies into the antagonists' 3D conformational and topographical properties in addition to future mutagenesis studies will provide greater insight into these ligands which could play a role in the treatment of various diseases in the future." @default.
- W2321825042 created "2016-06-24" @default.
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- W2321825042 creator A5063994952 @default.
- W2321825042 creator A5070071799 @default.
- W2321825042 creator A5076760321 @default.
- W2321825042 date "2011-03-24" @default.
- W2321825042 modified "2023-09-24" @default.
- W2321825042 title "Approaches to the rational design of selective melanocortin receptor antagonists" @default.
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- W2321825042 doi "https://doi.org/10.1517/17460441.2011.565743" @default.
- W2321825042 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4608743" @default.
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- W2321825042 hasPublicationYear "2011" @default.
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