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Iberdomide (CC-220) is a potent cereblon E3 ligase modulator with antitumor and immunostimulatory activities in lenalidomide- and pomalidomide-resistant multiple myeloma cells with dysregulated CRBN.

作者信息

Bjorklund Chad C, Kang Jian, Amatangelo Michael, Polonskaia Ann, Katz Mark, Chiu Hsiling, Couto Suzana, Wang Maria, Ren Yan, Ortiz Maria, Towfic Fadi, Flynt J Erin, Pierceall William, Thakurta Anjan

机构信息

Celgene Corporation, Summit, NJ, USA.

Celgene Corporation, San Diego, CA, USA.

出版信息

Leukemia. 2020 Apr;34(4):1197-1201. doi: 10.1038/s41375-019-0620-8. Epub 2019 Nov 12.

DOI:10.1038/s41375-019-0620-8
PMID:31719682
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7214241/
Abstract
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd4d/7214241/cef21aded10c/41375_2019_620_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd4d/7214241/9e53c2d3050a/41375_2019_620_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd4d/7214241/cef21aded10c/41375_2019_620_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd4d/7214241/9e53c2d3050a/41375_2019_620_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fd4d/7214241/cef21aded10c/41375_2019_620_Fig2_HTML.jpg

相似文献

1
Iberdomide (CC-220) is a potent cereblon E3 ligase modulator with antitumor and immunostimulatory activities in lenalidomide- and pomalidomide-resistant multiple myeloma cells with dysregulated CRBN.伊布多米德（CC-220）是一种强效的脑啡肽E3连接酶调节剂，在对来那度胺和泊马度胺耐药且CRBN失调的多发性骨髓瘤细胞中具有抗肿瘤和免疫刺激活性。
Leukemia. 2020 Apr;34(4):1197-1201. doi: 10.1038/s41375-019-0620-8. Epub 2019 Nov 12.
2
Cereblon expression is required for the antimyeloma activity of lenalidomide and pomalidomide.Cereblon 表达是来那度胺和泊马度胺抗骨髓瘤活性所必需的。
Blood. 2011 Nov 3;118(18):4771-9. doi: 10.1182/blood-2011-05-356063. Epub 2011 Aug 22.
3
Genome-wide screening reveals a role for subcellular localization of CRBN in the anti-myeloma activity of pomalidomide.全基因组筛选揭示了 CRBN 的亚细胞定位在泊马度胺抗骨髓瘤活性中的作用。
Sci Rep. 2020 Mar 4;10(1):4012. doi: 10.1038/s41598-020-61027-w.
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Generation of a lenalidomide-sensitive syngeneic murine in vivo multiple myeloma model by expression of Crbn.通过表达 Crbn 生成 lenalidomide 敏感的同种异体小鼠体内多发性骨髓瘤模型。
Exp Hematol. 2021 Jan;93:61-69.e4. doi: 10.1016/j.exphem.2020.11.004. Epub 2020 Nov 11.
5
Dual inhibition of DNMTs and EZH2 can overcome both intrinsic and acquired resistance of myeloma cells to IMiDs in a cereblon-independent manner.双重抑制 DNMTs 和 EZH2 可以在不依赖 cereblon 的情况下克服骨髓瘤细胞对 IMiDs 的内在和获得性耐药。
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Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide. cereblon 是来那度胺和泊马度胺免疫调节和抗增殖活性的直接蛋白靶标。
Leukemia. 2012 Nov;26(11):2326-35. doi: 10.1038/leu.2012.119. Epub 2012 May 3.
7
High expression of cereblon (CRBN) is associated with improved clinical response in patients with multiple myeloma treated with lenalidomide and dexamethasone.高表达的 cereblon（CRBN）与来那度胺和地塞米松治疗多发性骨髓瘤患者的临床改善相关。
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A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos.一种具有改善的 Ikaros 和 Aiolos 降解功能的 Cereblon 调节剂（CC-220）。
J Med Chem. 2018 Jan 25;61(2):535-542. doi: 10.1021/acs.jmedchem.6b01921. Epub 2017 Apr 20.
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Multiple cereblon genetic changes are associated with acquired resistance to lenalidomide or pomalidomide in multiple myeloma.多发性骨髓瘤患者对来那度胺或泊马度胺获得性耐药与多个 cereblon 基因突变相关。
Blood. 2021 Jan 14;137(2):232-237. doi: 10.1182/blood.2020007081.
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Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs.基于泊马度胺的同型PROTAC对E3泛素连接酶大脑神经酰胺酶的化学失活作用
J Vis Exp. 2019 May 15(147). doi: 10.3791/59472.

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