De Oindrila, Chatterji Biswa P
Post Graduate Department of Biotechnology, St. Xavier's College (Autonomous), 5, Mahapalika Marg, Mumbai, Maharashtra 400 001. India.
Post Graduate Department of Biotechnology, St. Xavier's College (Autonomous), Mumbai. India.
Recent Pat Anticancer Drug Discov. 2017;12(2):102-127. doi: 10.2174/1574892812666170109141003.
Microtubule dynamics plays a vital role in regulating crucial cellular functions and is one of the most attractive anticancer drug targets. Microtubule targeting agents (MTAs) such as the vinca alkaloids or taxanes, although are effective for cancer therapy, have adverse side effects. Another hindrance in their development is multiple drug resistance in tumor cells. These drawbacks have urged the need to develop novel MTAs from alternative sources, with better therapeutic efficacy. Recently, MTAs from marine sources have grabbed much attention due to unique tubulin binding features and remarkable ability to reduce tumor progression.
The emphasis of the article is to provide an overview of some of the most promising marine derived MTAs and highlight their major characteristics in brief.
Patent databases such as USPTO, Espacenet and WIPO were searched systematically for recent patents published from 2006 up to 2016. Numerous data retrieved was analyzed critically, and only those patents focusing on the chemical synthesis and/or modifications of marine derived MTAs along with a significant demonstration of their in vitro and/or in vivo activity are summarized here.
Some of the marine derived MTAs have significant antiproliferative potency against a wide array of cancers and are also able to overcome multidrug resistance.
The marine derived MTAs hold great potential in the field of cancer therapeutics and are gradually advancing in the clinical set up. A deeper understanding of the molecular mechanisms combined with innovative therapeutic regimen would lead to major advances in the field.
微管动力学在调节关键细胞功能中起着至关重要的作用，并且是最具吸引力的抗癌药物靶点之一。微管靶向剂（MTAs），如长春花生物碱或紫杉烷，虽然对癌症治疗有效，但有不良副作用。它们开发中的另一个障碍是肿瘤细胞中的多药耐药性。这些缺点促使人们需要从其他来源开发新型MTAs，以获得更好的治疗效果。最近，来自海洋来源的MTAs由于独特的微管蛋白结合特性和显著的降低肿瘤进展的能力而备受关注。
本文的重点是概述一些最有前景的海洋来源的MTAs，并简要突出它们的主要特征。
系统检索了美国专利商标局（USPTO）、欧洲专利局（Espacenet）和世界知识产权组织（WIPO）等专利数据库中2006年至2016年发表的近期专利。对检索到的大量数据进行了严格分析，这里仅总结那些专注于海洋来源的MTAs的化学合成和/或修饰以及其体外和/或体内活性的显著证明的专利。
一些海洋来源的MTAs对多种癌症具有显著的抗增殖效力，并且还能够克服多药耐药性。
海洋来源的MTAs在癌症治疗领域具有巨大潜力，并且正在临床应用中逐步推进。对分子机制的更深入理解与创新的治疗方案相结合将导致该领域的重大进展。
