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首页> 美国卫生研究院文献>Molecules >Structure–Activity Relationships of the Tetrapeptide Ac-His-Arg-(pI)DPhe-Tic-NH2 at the Mouse Melanocortin Receptors: Modification at the (pI)DPhe Position Leads to mMC3R Versus mMC4R Selective Ligands
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Structure–Activity Relationships of the Tetrapeptide Ac-His-Arg-(pI)DPhe-Tic-NH2 at the Mouse Melanocortin Receptors: Modification at the (pI)DPhe Position Leads to mMC3R Versus mMC4R Selective Ligands

机译：小鼠黑皮质素受体上四肽Ac-His-Arg-（pI）DPhe-Tic-NH2的结构-活性关系：（pI）DPhe位置的修饰导致mMC3R与mMC4R选择性配体。

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The five melanocortin receptors (MC1R–MC5R) are involved in numerous biological pathways, including steroidogenesis, pigmentation, and food intake. In particular, MC3R and MC4R knockout mice suggest that the MC3R and MC4R regulate energy homeostasis in a non-redundant manner. While MC4R-selective agonists have been utilized as appetite modulating agents, the lack of MC3R-selective agonists has impeded progress in modulating this receptor in vivo. In this study, the (pI)DPhe position of the tetrapeptide Ac-His-Arg-(pI)DPhe-Tic-NH2 (an MC3R agonist/MC4R antagonist ligand) was investigated with a library of 12 compounds. The compounds in this library were found to have higher agonist efficacy and potency at the mouse (m) MC3R compared to the MC4R, indicating that the Arg-DPhe motif preferentially activates the mMC3R over the mMC4R. This observation may be used in the design of new MC3R-selective ligands, leading to novel probe and therapeutic lead compounds that will be useful for treating metabolic disorders.
机译：五个黑皮质素受体（MC1R–MC5R）参与多种生物途径，包括类固醇生成，色素沉着和食物摄入。特别是，MC3R和MC4R敲除小鼠表明MC3R和MC4R以非冗余方式调节能量稳态。尽管已经将MC4R-选择性激动剂用作食欲调节剂，但是缺乏MC3R-选择性激动剂已经阻碍了体内调节该受体的进展。在这项研究中，使用12种化合物的文库研究了四肽Ac-His-Arg-（pI）DPhe-Tic-NH2（MC3R激动剂/ MC4R拮抗剂配体）的（pI）DPhe位置。发现与MC4R相比，该文库中的化合物对小鼠（m）MC3R具有更高的激动剂功效和效力，表明Arg-DPhe基序比mMC4R优先激活mMC3R。该观察结果可用于设计新的MC3R选择性配体，从而产生可用于治疗代谢异常的新型探针和治疗性先导化合物。

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