Suppr超能文献

免疫调节药物破坏 cereblon-CD147-MCT1 轴发挥抗肿瘤活性和致畸性。

Immunomodulatory drugs disrupt the cereblon-CD147-MCT1 axis to exert antitumor activity and teratogenicity.

机构信息

Department of Medicine III, Klinikum rechts der Isar, Technische Universität München, Munich, Germany.

German Cancer Consortium (DKTK), Heidelberg, Germany.

出版信息

Nat Med. 2016 Jul;22(7):735-43. doi: 10.1038/nm.4128. Epub 2016 Jun 13.

Abstract

Immunomodulatory drugs (IMiDs), such as thalidomide and its derivatives lenalidomide and pomalidomide, are key treatment modalities for hematologic malignancies, particularly multiple myeloma (MM) and del(5q) myelodysplastic syndrome (MDS). Cereblon (CRBN), a substrate receptor of the CRL4 ubiquitin ligase complex, is the primary target by which IMiDs mediate anticancer and teratogenic effects. Here we identify a ubiquitin-independent physiological chaperone-like function of CRBN that promotes maturation of the basigin (BSG; also known as CD147) and solute carrier family 16 member 1 (SLC16A1; also known as MCT1) proteins. This process allows for the formation and activation of the CD147-MCT1 transmembrane complex, which promotes various biological functions, including angiogenesis, proliferation, invasion and lactate export. We found that IMiDs outcompete CRBN for binding to CD147 and MCT1, leading to destabilization of the CD147-MCT1 complex. Accordingly, IMiD-sensitive MM cells lose CD147 and MCT1 expression after being exposed to IMiDs, whereas IMiD-resistant cells retain their expression. Furthermore, del(5q) MDS cells have elevated CD147 expression, which is attenuated after IMiD treatment. Finally, we show that BSG (CD147) knockdown phenocopies the teratogenic effects of thalidomide exposure in zebrafish. These findings provide a common mechanistic framework to explain both the teratogenic and pleiotropic antitumor effects of IMiDs.

摘要

免疫调节药物(IMiDs),如沙利度胺及其衍生物来那度胺和泊马度胺,是血液系统恶性肿瘤,特别是多发性骨髓瘤(MM)和 del(5q)骨髓增生异常综合征(MDS)的主要治疗方法。CRBN(CRBN)是 CRL4 泛素连接酶复合物的底物受体,是 IMiDs 介导抗癌和致畸作用的主要靶标。在这里,我们确定了 CRBN 的一种非泛素依赖的生理伴侣样功能,该功能促进了 basigin(BSG;也称为 CD147)和溶质载体家族 16 成员 1(SLC16A1;也称为 MCT1)蛋白的成熟。这个过程允许 CD147-MCT1 跨膜复合物的形成和激活,从而促进各种生物学功能,包括血管生成、增殖、侵袭和乳酸盐输出。我们发现 IMiDs 与 CD147 和 MCT1 的结合竞争 CRBN,导致 CD147-MCT1 复合物的不稳定性。因此,在暴露于 IMiD 后,IMiD 敏感的 MM 细胞会失去 CD147 和 MCT1 的表达,而 IMiD 耐药的细胞则保留其表达。此外,del(5q) MDS 细胞具有升高的 CD147 表达,在用 IMiD 处理后其表达会减弱。最后,我们表明 BSG(CD147)敲低可模拟沙利度胺暴露在斑马鱼中的致畸作用。这些发现为解释 IMiD 的致畸和多效抗肿瘤作用提供了一个共同的机制框架。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验