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新型黑皮质素受体配体的设计：多受体，复杂的药理学，挑战。

Design of novel melanocortin receptor ligands: multiple receptors, complex pharmacology, the challenge.

机构信息

Department of Chemistry and Biochemistry, University of Arizona, Tucson, AZ 85721, USA.

出版信息

Eur J Pharmacol. 2011 Jun 11;660(1):88-93. doi: 10.1016/j.ejphar.2010.10.109. Epub 2011 Jan 3.

DOI:10.1016/j.ejphar.2010.10.109
PMID:21208601
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3138524/
Abstract

The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.

摘要

黑皮质素 1、3、4 和 5 受体的主要药效基团是 -His-Phe-Arg-Trp-序列。这些受体需要具有高效、生物稳定和受体选择性的激动剂和拮抗剂配体。在本报告中，我们简要探讨了我们为开发可穿透（或不可穿透）血脑屏障的选择性激动剂和拮抗剂配体而采取的结构和生物物理方法。还讨论了存在的问题和未满足的需求。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a2b/3138524/0b4053dfc2a8/nihms290877f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a2b/3138524/c3083e04d935/nihms290877f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a2b/3138524/0b4053dfc2a8/nihms290877f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a2b/3138524/c3083e04d935/nihms290877f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a2b/3138524/0b4053dfc2a8/nihms290877f2.jpg

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