Department of Biomolecular Chemistry, Medical University of Lodz, Mazowiecka 6/8, PL-92-215 Lodz, Poland.
Chem Biodivers. 2021 Jan;18(1):e2000871. doi: 10.1002/cbdv.202000871. Epub 2020 Dec 22.
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.
阿片受体样蛋白 1 受体（NOP）属于阿片受体家族，但比所谓的经典阿片受体μ、δ和κ（或 MOP、DOP 和 KOP）发现和鉴定得晚得多。阿片肽/孤啡肽（N/OFQ）是该受体的内源性配体，它在中枢神经系统和外周控制着许多重要的功能，因此它的类似物可以开发成治疗各种疾病和病理状态的创新药物。具有高亲和力和选择性的 NOP 受体的有效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，这反过来又可能导致设计新的治疗方法。在这里，我们重点回顾了针对 NOP 受体的强效肽类激动剂、拮抗剂、偏向性类似物和双价配体的结构。
