靶向κ阿片受体以实现镇痛和抗肿瘤作用。
Targeting the kappa opioid receptor for analgesia and antitumour effects.
作者信息
Lambert David G, Mincer Joshua S
机构信息
Department of Cardiovascular Sciences, Anaesthesia, Critical Care and Pain Management, University of Leicester, Hodgkin Building, Leicester, UK.
Department of Anesthesiology and Critical Care Medicine, Memorial Sloan Kettering Cancer Center, New York, NY, USA; Department of Anesthesiology, Weill Cornell Medicine, New York, NY, USA.
出版信息
Br J Anaesth. 2025 Mar;134(3):646-648. doi: 10.1016/j.bja.2024.10.014. Epub 2025 Jan 3.
Kappa opioid (KOP) receptor agonists have analgesic actions in a range of models, but central side-effects can limit their utility. In addition, non-analgesic actions of opioid receptors are receiving significant research interest. A recent article reports that high KOP receptor expression in glioma tissue correlates with improved survival and that KOP receptor agonism further promotes apoptosis of glioma cells through regulation of the p38 MAPK oncogenic pathway. This suggests that KOP receptor ligands could be developed as chemotherapeutic adjuncts in addition to their use as analgesics.
κ阿片受体（KOP）激动剂在一系列模型中具有镇痛作用，但中枢副作用可能会限制其应用。此外，阿片受体的非镇痛作用正受到广泛的研究关注。最近一篇文章报道，胶质瘤组织中高KOP受体表达与生存期延长相关，且KOP受体激动作用通过调节p38丝裂原活化蛋白激酶致癌途径进一步促进胶质瘤细胞凋亡。这表明，KOP受体配体除用作镇痛药外，还可开发为化疗辅助药物。
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