Emerging Bcl-2 inhibitors for the treatment of cancer.
Emerging Bcl-2 inhibitors for the treatment of cancer.
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DOI：
10.1517/14728214.2010.515210
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发表时间：
2011-03
影响因子：
3.4
通讯作者：
Sarkar FH
中科院分区：
文献类型：
--
作者：
Azmi AS;Wang Z;Philip PA;Mohammad RM;Sarkar FH
BCL-2家族蛋白是抗细胞凋亡机制的一个组成部分，在不同的恶性肿瘤中过表达。因此，它们的增强表达被归因于在大多数癌症中观察到的化疗耐药。因此，靶向Bcl-2家族成员成为癌症治疗的一种重要和有吸引力的方法，目前是一个发展非常迅速的研究领域。这篇文章重点介绍了在设计和合成促进生存的Bcl-2蛋白的小分子抑制物(SMI)方面取得的许多进展。本文综述了近20年来在这方面的研究进展，包括Bcl2家族蛋白SMI的临床研究现状。我们将获得更新的洞察力，了解我们对Bcl-2家族蛋白SMI的了解状况，它们最有益的应用，以及该领域的当前和未来方向。随着某些新类型的抑制剂在I期和II期临床环境中的出现，使用SMI策略靶向Bcl-2家族蛋白的势头正在增强。鉴于这种抑制剂的开发取得了巨大的进步，这种创新的方法肯定是有希望的，并有可能成为未来癌症治疗的支柱。
Bcl-2 family proteins are a component of the anti-apoptotic machinery and are overexpressed in different malignancies. Accordingly, their enhanced expression has been attributed to the observed chemoresistance in most of the cancers. Therefore, targeting Bcl-2 family members becomes an important and attractive approach towards cancer therapy and is currently a very rapidly evolving area of research. This article highlights the numerous advancements that have been made in the design and synthesis of small molecule inhibitors (SMI) of pro-survival Bcl-2 proteins. This review comprehensively describes the progress made over the last 2 decades on this subject including the clinical status of SMIs of Bcl-2 family proteins. Newer insights will be gained on the status of our knowledge on SMIs of Bcl-2 family proteins, their most beneficial application as well as current and future directions in this field. Targeting Bcl-2 family proteins using SMI strategies is gaining momentum with emergence of certain new classes of inhibitors in Phase I and II clinical setting. In view of the tremendous progress toward the development of such inhibitors, this innovative approach certainly holds promise and has the potential to become a future mainstay for cancer therapy.
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