Bhattacharjee Pinaki, Iyer Malliga R
Section on Medicinal Chemistry, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, 5625 Fishers Lane, Rockville, MD 20852, USA.
Pharmaceuticals (Basel). 2023 Aug 31;16(9):1235. doi: 10.3390/ph16091235.
The cannabinoid receptors CB and CB are class A G protein-coupled receptors (GPCRs) that are activated via endogenous lipids called endocannabinoids. The endocannabinoid system (ECS) plays a critical role in the regulation of several physiological states and a wide range of diseases. In recent years, drug discovery approaches targeting the cannabinoid type 2 receptor (CBR) have gained prominence. Particular attention has been given to selective agonists targeting the CB receptors to circumvent the neuropsychotropic side effects associated with CB receptors. The pharmacological modulation of CBR holds therapeutic promise for various diseases, such as inflammatory disorders and immunological conditions, as well as pain management and cancer treatment. Recently, the utilization of fluorescent probes has emerged as a valuable technique for investigating the interactions between ligands and proteins at an exceptional level of spatial and temporal precision. In this review, we aim to examine the progress made in the development of fluorescent probes targeting CB receptors and highlight their significance in facilitating the successful clinical translation of CBR-based therapies.
大麻素受体CB1和CB2是A类G蛋白偶联受体（GPCRs），可通过称为内源性大麻素的内源性脂质激活。内源性大麻素系统（ECS）在多种生理状态和广泛疾病的调节中起关键作用。近年来，靶向大麻素2型受体（CB2R）的药物发现方法备受关注。人们特别关注靶向CB2受体的选择性激动剂，以规避与CB1受体相关的神经精神副作用。CB2R的药理调节对各种疾病具有治疗前景，如炎症性疾病和免疫性疾病，以及疼痛管理和癌症治疗。最近，荧光探针的应用已成为一种有价值的技术，可在极高的空间和时间精度水平上研究配体与蛋白质之间的相互作用。在本综述中，我们旨在研究靶向CB2受体的荧光探针开发所取得的进展，并强调它们在促进基于CB2R的疗法成功临床转化方面的重要性。
