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沙利度胺及其类似物的药理特性。

Pharmacological properties of thalidomide and its analogues.

作者信息

De Sanctis Juan B, Mijares Michael, Suárez Alírica, Compagnone Reinaldo, Garmendia Jenny, Moreno Dolores, Salazar-Bookaman Margarita

机构信息

Instituto de Inmunología, Facultad de Medicina, Universidad Central de Venezuela, Caracas, Venezuela.

出版信息

Recent Pat Inflamm Allergy Drug Discov. 2010 Jun;4(2):144-8. doi: 10.2174/187221310791163026.

DOI:10.2174/187221310791163026
PMID:20307255
Abstract

Thalidomide and its immunomodulatory imide drugs (IMiDs) analogues CC-5013 (Revlimid, Lenalidomide) and CC-4047 (Actimid, Pomalidomide) have been used as anti-inflammatory and anticancerous drugs in the recent years. Thalidomide and IMiDs inhibit the cytokines tumour necrosis factor-alpha (TNF-alpha), interleukins (IL) 1-beta, 6, 12, and granulocyte macrophage-colony stimulating factor (GM-CSF). They also costimulate primary human T, NKT and NK lymphocytes inducing their proliferation, cytokine production, and cytotoxic activity. On the other hand, the compounds are anti-angiogenic, anti-proliferative, and pro-apoptotic. Thalidomide analogues have been used as inhibitors of alpha glucosidase and could be potential drugs for diabetes treatment. In this review, we explore the current trend of the different structures, the new patents, and the possible new applications in different pathologies.

摘要

沙利度胺及其免疫调节性酰亚胺药物(IMiDs)类似物CC - 5013(来那度胺,Revlimid)和CC - 4047(泊马度胺,Actimid)近年来已被用作抗炎和抗癌药物。沙利度胺和IMiDs可抑制细胞因子肿瘤坏死因子-α(TNF-α)、白细胞介素(IL)1-β、6、12以及粒细胞巨噬细胞集落刺激因子(GM-CSF)。它们还能共刺激原代人T细胞、NKT细胞和NK淋巴细胞,诱导其增殖、细胞因子产生及细胞毒性活性。另一方面,这些化合物具有抗血管生成、抗增殖和促凋亡作用。沙利度胺类似物已被用作α-葡萄糖苷酶抑制剂,可能成为治疗糖尿病的潜在药物。在本综述中,我们探讨了不同结构的当前趋势、新专利以及在不同病理情况下可能的新应用。

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Pharmacological properties of thalidomide and its analogues.沙利度胺及其类似物的药理特性。
Recent Pat Inflamm Allergy Drug Discov. 2010 Jun;4(2):144-8. doi: 10.2174/187221310791163026.
2
Properties of thalidomide and its analogues: implications for anticancer therapy.沙利度胺及其类似物的特性:对癌症治疗的启示。
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The anti-cancer agents lenalidomide and pomalidomide inhibit the proliferation and function of T regulatory cells.抗癌药物来那度胺和泊马度胺可抑制调节性T细胞的增殖和功能。
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Immunomodulatory drugs stimulate natural killer-cell function, alter cytokine production by dendritic cells, and inhibit angiogenesis enhancing the anti-tumour activity of rituximab in vivo.免疫调节药物可刺激自然杀伤细胞功能,改变树突状细胞的细胞因子产生,并抑制血管生成,从而增强利妥昔单抗在体内的抗肿瘤活性。
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Lenalidomide - current understanding of mechanistic properties.来那度胺-对作用机制特性的现有认识。
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Immunomodulatory drugs as a therapy for multiple myeloma.
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The thalidomide saga.沙利度胺事件
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Thalidomide analogs as emerging anti-cancer drugs.沙利度胺类似物作为新兴的抗癌药物。
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