Apoptosis-inducing agents: a patent review (2010-2013)

被引:40
作者
Kamal, Ahmed [1 ]
Faazil, Shaikh [1 ]
Malik, Mohammed Shaheer [1 ]
机构
[1] Indian Inst Chem Technol, CSIR, Hyderabad 500007, Andhra Pradesh, India
关键词
apoptosis; apoptosis inducers; Bcl-2; proteins; cancer drug development; caspases; heterocyclics; sulfonamides; BIOLOGICAL EVALUATION; DESIGN;
D O I
10.1517/13543776.2014.877445
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Introduction: Apoptosis is an important and extensively studied pathway of programmed cell death, which is central to different physiological processes. Varied pathological implications, not limited to cancer and neurodegenerative diseases, occur if a slight dysfunction happens in the intricate apoptotic pathway. Therefore, it has become one of the prime molecular target for drug discovery and development particularly for diseases like cancer. Areas covered: As a promising drug target in the development of cancer chemotherapeutics, apoptosis has received extensive attention and hundreds of thousands of reports have been published. In the present review, the patents filed/published on apoptosis-inducing agents during the period of 2010 - 2013 have been compiled and discussed. Expert opinion: Most of the chemotherapeutics employed in cancer treatment leads to suppression of tumor via cell death irrespective of the mechanism of action or molecular target. No effective drug has emerged from the direct activation/inhibition of apoptotic regulatory proteins and of late some potential drugs, such as oblimersen, navitoclax, etc., targeting Bcl-2 family of proteins are under clinical trials. However, most of these molecules lacks efficacy accompanied with significant toxicity and resistance. Concerted efforts are required such as combination therapies and identification of newer selective inhibitor to overcome these limitations.
引用
收藏
页码:339 / 354
页数:16
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