Potential of Nociceptin/Orphanin FQ Peptide Analogs for Drug Development,Chemistry & Biodiversity

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Potential of Nociceptin/Orphanin FQ Peptide Analogs for Drug Development
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2020-12-22 , DOI: 10.1002/cbdv.202000871
Karol Wtorek ₁ , Anna Janecka ₁

Affiliation

Nociceptin receptor (NOP) belongs to the family of opioid receptors but was discovered and characterized much later than the so called classical opioid receptors, μ, δ and κ (or MOP, DOP and KOP, resp.). Nociceptin/orphanin FQ (N/OFQ) is the endogenous ligand of this receptor and it controls numerous important functions in the central nervous system and in the periphery, so its analogs may be developed as innovative drugs for the treatment of a variety of conditions and pathological states. Availability of potent and selective ligands with high affinity to NOP receptor is essential to fully understand the role of NOP‐N/OFQ system in the body, which in turn may lead to designing novel therapeutics. Here, we have focused on reviewing the structure of potent peptide‐based agonists, antagonists, biased analogs and bivalent ligands that target NOP receptor.

中文翻译：

伤害感受肽/孤啡宁 FQ 肽类似物在药物开发中的潜力

伤害感受肽受体 (NOP) 属于阿片受体家族，但其发现和表征远远晚于所谓的经典阿片受体 μ、δ 和 κ（或 MOP、DOP 和 KOP）。伤害感受肽/孤啡肽 FQ (N/OFQ) 是该受体的内源性配体，控制着中枢神经系统和外周的许多重要功能，因此其类似物可开发为治疗多种疾病和疾病的创新药物。病理状态。与 NOP 受体具有高亲和力的有效和选择性配体的可用性对于充分了解 NOP-N/OFQ 系统在体内的作用至关重要，这反过来可能会导致设计新的治疗方法。在这里，我们重点回顾了针对 NOP 受体的有效肽激动剂、拮抗剂、偏向类似物和二价配体的结构。

更新日期：2020-12-22

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