Recent advances in cancer therapeutics.

Q1 Pharmacology, Toxicology and Pharmaceutics
Progress in medicinal chemistry Pub Date : 2015-01-01 Epub Date: 2015-01-23 DOI:10.1016/bs.pmch.2014.11.002
Nicola Chessum, Keith Jones, Elisa Pasqua, Michael Tucker
{"title":"Recent advances in cancer therapeutics.","authors":"Nicola Chessum,&nbsp;Keith Jones,&nbsp;Elisa Pasqua,&nbsp;Michael Tucker","doi":"10.1016/bs.pmch.2014.11.002","DOIUrl":null,"url":null,"abstract":"<p><p>In the past 20 years, cancer therapeutics has undergone a paradigm shift away from the traditional cytotoxic drugs towards the targeting of proteins intimately involved in driving the cancer phenotype. The poster child for this alternative approach to the treatment of cancer is imatinib, a small-molecule kinase inhibitor designed to target chronic myeloid leukaemia driven by the BCR-ABL translocation in a defined patient population. The improvement in survival achieved by treatment of this patient cohort with imatinib is impressive. Thus, the aim is to provide efficacy but with low toxicity. The role of the medicinal chemist in oncology drug discovery is now closely aligned with the role in most other therapeutic areas with high-throughput and/or fragment-based screening, structure-based design, selectivity, pharmacokinetic optimisation and pharmacodynamic biomarker modulation, all playing a familiar part in the process. In this chapter, we selected four areas in which compounds are either approved drugs or in clinical trials. These are chaperone inhibitors, kinase inhibitors, histone deacetylase inhibitors and inhibitors of protein-protein interactions. Even within these areas, we have been selective, particularly for kinase inhibitors, and our aim has been to exemplify newer approaches and novel aspects of medicinal chemistry. </p>","PeriodicalId":20755,"journal":{"name":"Progress in medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2015-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/bs.pmch.2014.11.002","citationCount":"32","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Progress in medicinal chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1016/bs.pmch.2014.11.002","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2015/1/23 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 32

Abstract

In the past 20 years, cancer therapeutics has undergone a paradigm shift away from the traditional cytotoxic drugs towards the targeting of proteins intimately involved in driving the cancer phenotype. The poster child for this alternative approach to the treatment of cancer is imatinib, a small-molecule kinase inhibitor designed to target chronic myeloid leukaemia driven by the BCR-ABL translocation in a defined patient population. The improvement in survival achieved by treatment of this patient cohort with imatinib is impressive. Thus, the aim is to provide efficacy but with low toxicity. The role of the medicinal chemist in oncology drug discovery is now closely aligned with the role in most other therapeutic areas with high-throughput and/or fragment-based screening, structure-based design, selectivity, pharmacokinetic optimisation and pharmacodynamic biomarker modulation, all playing a familiar part in the process. In this chapter, we selected four areas in which compounds are either approved drugs or in clinical trials. These are chaperone inhibitors, kinase inhibitors, histone deacetylase inhibitors and inhibitors of protein-protein interactions. Even within these areas, we have been selective, particularly for kinase inhibitors, and our aim has been to exemplify newer approaches and novel aspects of medicinal chemistry.

癌症治疗的最新进展。
在过去的20年里,癌症治疗经历了从传统的细胞毒性药物到靶向与驱动癌症表型密切相关的蛋白质的范式转变。这种替代癌症治疗方法的典型代表是伊马替尼,这是一种小分子激酶抑制剂,旨在针对特定患者群体中由BCR-ABL易位驱动的慢性髓性白血病。通过伊马替尼治疗该患者队列获得的生存改善令人印象深刻。因此,目的是提供低毒性的功效。药物化学家在肿瘤药物发现中的作用现在与大多数其他治疗领域的作用密切相关,包括高通量和/或基于片段的筛选,基于结构的设计,选择性,药代动力学优化和药效学生物标志物调节,都在该过程中发挥着熟悉的作用。在本章中,我们选择了四个领域,其中化合物要么是批准的药物,要么是处于临床试验阶段。这些是伴侣抑制剂,激酶抑制剂,组蛋白去乙酰化酶抑制剂和蛋白质-蛋白质相互作用抑制剂。即使在这些领域,我们也一直是有选择性的,特别是激酶抑制剂,我们的目标是举例说明药物化学的新方法和新方面。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
Progress in medicinal chemistry
Progress in medicinal chemistry Pharmacology, Toxicology and Pharmaceutics-Pharmacology
CiteScore
15.60
自引率
0.00%
发文量
6
期刊介绍: This series has a long established reputation for excellent coverage of almost every facet of Medicinal Chemistry and is one of the most respected and instructive sources of information on the subject. The latest volume certifies to the continuing success of a unique series reflecting current progress in a broadly developing field of science.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信