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Target protein degradation by protacs: A budding cancer treatment strategy
Pharmacology & Therapeutics ( IF 12.0 ) Pub Date : 2023-09-09 , DOI: 10.1016/j.pharmthera.2023.108525
Diksha Choudhary 1 , Amritpal Kaur 1 , Pargat Singh 1 , Gaurav Chaudhary 1 , Rajwinder Kaur 1 , Mohammad F Bayan 2 , Balakumar Chandrasekaran 2 , Saeed M Marji 2 , Reema Ayman 2
Affiliation  

Cancer is one of the most common causes of death. So, its lethal effect increases with time. Near about hundreds of cancers are known in humans. Cancer treatment is done to cure or prolonged remission, and shrinkage of the tumor. Cytotoxic agents, biological agents/targeted drugs, hormonal drugs, surgery, radiotherapy/proton therapy, chemotherapy, immunotherapy, and gene therapy are currently used in the treatment of cancer but their cost is high and cause various side effects. Seeing this, some new targeted strategies such as PROTACs are the need of the time. Proteolysis targeting chimera (PROTAC) has become one of the most discussed topics regarding cancer treatment. Few of the PROTAC molecules are in the trial phases. PROTACs have many advantages over other strategies such as modularity, compatibility, sub-stoichiometric activity, acting on undruggable targets, molecular design, and acts on intracellular targets, selectivity and specificity can be recruited for any cancer, versatility, and others. PROTACs are having some unclear questions on their pharmacokinetics, heavy-molecular weight, etc. PROTACs are anticipated to bring about a conversion in current healthcare and will emerge as booming treatments. In this review article we summarize PROTACs, their mechanism of action, uses, advantages, disadvantages, challenges, and future aspects for the successful development of potent PROTACs as a drug strategy.



中文翻译:

Protacs 降解靶蛋白:一种新兴的癌症治疗策略

癌症是最常见的死亡原因之一。因此,其杀伤力会随着时间的推移而增加。人类已知近数百种癌症。癌症治疗的目的是治愈或延长缓解时间以及缩小肿瘤。目前用于治疗癌症的方法有细胞毒剂、生物制剂/靶向药物、激素药物、手术、放疗/质子治疗、化疗、免疫治疗和基因治疗,但其成本较高且会产生各种副作用。看到这一点,一些新的针对性策略如PROTACs就应运而生了。蛋白水解靶向嵌合体(PROTAC)已成为癌症治疗中讨论最多的话题之一。很少有 PROTAC 分子处于试验阶段。与其他策略相比,PROTAC 具有许多优势,例如模块化、兼容性、亚化学计量活性、作用于不可成药的靶标、分子设计、作用于细胞内靶标、可针对任何癌症、多功能性等招募选择性和特异性。PROTAC 在药代动力学、重分子量等方面存在一些不清楚的问题。PROTAC 预计将带来当前医疗保健的转变,并将成为蓬勃发展的治疗方法。在这篇综述文章中,我们总结了 PROTAC、其作用机制、用途、优点、缺点、挑战以及成功开发有效 PROTAC 作为药物策略的未来方面。

更新日期:2023-09-09
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