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首页> 外文期刊>Life sciences >Design of novel peptide ligands which have opioid agonist activity and CCK antagonist activity for the treatment of pain.
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Design of novel peptide ligands which have opioid agonist activity and CCK antagonist activity for the treatment of pain.

机译：具有阿片样物质激动剂活性和CCK拮抗剂活性的新型肽配体的设计，用于治疗疼痛。

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摘要

Disease states such as neuropathic pain offer special challenges in drug design due to the system changes which accompany these diseases. In this manuscript we provide an example of a new approach to drug design in which we have modified a potent and selective peptide ligand for the CCK-2 receptor to a peptide which has potent agonist binding affinity and bioactivity at delta and mu opioid receptors, and simultaneous antagonist activity at CCK receptors. De novo design based on the concept of overlapping pharmacophores was a central hypothesis of this design, and led to compounds such as H-Tyr-DPhe-Gly-DTrp-NMeNle-Asp-Phe-NH(2) (i.e., RSA 601) which have the designed properties.
机译：由于伴随这些疾病的系统变化，诸如神经性疼痛之类的疾病状态在药物设计中提出了特殊的挑战。在本手稿中，我们提供了一种新的药物设计方法实例，其中我们将CCK-2受体的有效而选择性的肽配体修饰为对δ和μ阿片受体具有有效的激动剂结合亲和力和生物活性的肽，并且CCK受体同时具有拮抗剂活性。基于重叠药效团概念的从头设计是该设计的主要假设，并导致了诸如H-Tyr-DPhe-Gly-DTrp-NMeNle-Asp-Phe-NH（2）之类的化合物（即RSA 601）具有设计的属性。

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