Oshima Kumi, Ichinohe Tatsuo
Nihon Rinsho. 2014 Jun;72(6):1130-5.
Immunomodulatory drugs (IMiDs) are a new class of anti-inflammatory and antineoplastic agents that have structural and functional similarities with their prototype compound, thalidomide. Although thalidomide and its derivatives, lenalidomide and pomalidomide, are widely used as an essential component in the treatment of selected hematologic neoplasms including multiple myeloma, the precise mechanisms by which these agents exert anti-tumor effects have yet to be clarified. Recently, a component of E3 ubiquitin ligase complex, cereblon (CRBN), has been identified as a direct molecular target for anti-neoplastic activities of IMiDs. CRBN has also been shown to be involved in IMiDs-mediated T-cell co-stimulation and cytokine production. Further studies are necessary to elucidate the CRBN-related molecular pathways that are essential for antitumor and immunomodulatory activities of IMiDs.
免疫调节药物（IMiDs）是一类新型的抗炎和抗肿瘤药物，它们与其原型化合物沙利度胺在结构和功能上具有相似性。尽管沙利度胺及其衍生物来那度胺和泊马度胺被广泛用作治疗包括多发性骨髓瘤在内的特定血液系统肿瘤的重要组成部分，但这些药物发挥抗肿瘤作用的确切机制尚未阐明。最近，E3泛素连接酶复合物的一个组分，脑啡肽（CRBN），已被确定为IMiDs抗肿瘤活性的直接分子靶点。CRBN也被证明参与IMiDs介导的T细胞共刺激和细胞因子产生。需要进一步研究以阐明对IMiDs的抗肿瘤和免疫调节活性至关重要的与CRBN相关的分子途径。
