小分子激酶药物的演变
Evolution of Small Molecule Kinase Drugs.
作者信息
Lightfoot Helen L, Goldberg Frederick W, Sedelmeier Joerg
机构信息
IMED Biotech Unit,Discovery Sciences, AstraZeneca, Alderley Park SK10 4TG, U.K.
Oncology, IMED Biotech Unit, Medicinal Chemistry, AstraZeneca, Cambridge CB4 0WG, U.K.
出版信息
ACS Med Chem Lett. 2018 Dec 18;10(2):153-160. doi: 10.1021/acsmedchemlett.8b00445. eCollection 2019 Feb 14.
Abstract
The development of small molecule kinase drugs is a rapidly evolving field and represents one of the most important research areas within oncology. This innovation letter provides an overview and analysis of approved kinase drugs according to their WHO registration (INN) dates, primary biological targets, and selectivity and structural similarities, which are also depicted in an associated poster. It also discusses new trends in kinase drug discovery programs such as new kinase targets, novel mechanisms of action, and diverse indications.
摘要
小分子激酶药物的研发是一个快速发展的领域，也是肿瘤学中最重要的研究领域之一。本创新快报根据世界卫生组织注册（国际非专利名称）日期、主要生物学靶点以及选择性和结构相似性，对已批准的激酶药物进行了概述和分析，相关海报中也有展示。此外，还讨论了激酶药物发现项目的新趋势，如新的激酶靶点、新的作用机制和多样的适应症。
相似文献
1
Evolution of Small Molecule Kinase Drugs.
ACS Med Chem Lett. 2018 Dec 18;10(2):153-160. doi: 10.1021/acsmedchemlett.8b00445. eCollection 2019 Feb 14.
2
Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview.
Med Res Rev. 2017 Mar;37(2):314-367. doi: 10.1002/med.21409. Epub 2016 Oct 24.
3
Small-molecule kinase inhibitors: an analysis of FDA-approved drugs.
Drug Discov Today. 2016 Jan;21(1):5-10. doi: 10.1016/j.drudis.2015.07.008. Epub 2015 Jul 23.
4
A historical overview of protein kinases and their targeted small molecule inhibitors.
Pharmacol Res. 2015 Oct;100:1-23. doi: 10.1016/j.phrs.2015.07.010. Epub 2015 Jul 21.
5
Human kinome drug discovery and the emerging importance of atypical allosteric inhibitors.
Expert Opin Drug Discov. 2010 Mar;5(3):277-90. doi: 10.1517/17460441003636820. Epub 2010 Feb 18.
6
System-based drug discovery within the human kinome.
Expert Opin Drug Discov. 2012 Nov;7(11):1053-70. doi: 10.1517/17460441.2012.724056. Epub 2012 Sep 13.
7
Editorial: Current status and perspective on drug targets in tubercle bacilli and drug design of antituberculous agents based on structure-activity relationship.
Curr Pharm Des. 2014;20(27):4305-6. doi: 10.2174/1381612819666131118203915.
8
Properties of FDA-approved small molecule protein kinase inhibitors.
Pharmacol Res. 2019 Jun;144:19-50. doi: 10.1016/j.phrs.2019.03.006. Epub 2019 Mar 13.
9
Kinomics-structural biology and chemogenomics of kinase inhibitors and targets.
Biochim Biophys Acta. 2004 Mar 11;1697(1-2):243-57. doi: 10.1016/j.bbapap.2003.11.028.
10
Small molecule kinase inhibitors as anti-cancer therapeutics.
Mini Rev Med Chem. 2012 May;12(5):399-411. doi: 10.2174/138955712800493915.
引用本文的文献
1
Small molecule inhibitors target multiple neuropathological signaling to exert novel neuroprotection in intracranial aneurysms.
Front Pharmacol. 2024 Nov 7;15:1469211. doi: 10.3389/fphar.2024.1469211. eCollection 2024.
2
Occurrence of "Natural Selection" in Successful Small Molecule Drug Discovery.
J Med Chem. 2024 Jul 11;67(13):11226-11241. doi: 10.1021/acs.jmedchem.4c00811. Epub 2024 Jul 1.
3
An essential protein kinase: a functional analysis of regulation and the identification of inhibitors.
Front Parasitol. 2023;2. doi: 10.3389/fpara.2023.1272378. Epub 2023 Nov 14.
4
GCN2 kinase activation by ATP-competitive kinase inhibitors.
Nat Chem Biol. 2022 Feb;18(2):207-215. doi: 10.1038/s41589-021-00947-8. Epub 2021 Dec 23.
5
Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.
ACS Med Chem Lett. 2021 Mar 19;12(4):653-661. doi: 10.1021/acsmedchemlett.1c00096. eCollection 2021 Apr 8.
6
7-(2-Anilinopyrimidin-4-yl)-1-benzazepin-2-ones Designed by a "Cut and Glue" Strategy Are Dual Aurora A/VEGF-R Kinase Inhibitors.
Molecules. 2021 Mar 14;26(6):1611. doi: 10.3390/molecules26061611.
7
Identification of Potent Reverse Indazole Inhibitors for HPK1.
ACS Med Chem Lett. 2021 Mar 1;12(3):459-466. doi: 10.1021/acsmedchemlett.0c00672. eCollection 2021 Mar 11.
8
Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.
ACS Med Chem Lett. 2020 Dec 8;12(1):162-167. doi: 10.1021/acsmedchemlett.0c00392. eCollection 2021 Jan 14.
9
Activity-Based Kinome Profiling Using Chemical Proteomics and ATP Acyl Phosphates.
Curr Protoc Chem Biol. 2019 Sep;11(3):e72. doi: 10.1002/cpch.72.
本文引用的文献
1
WHO Listed Small Molecule Kinase Inhibitors 2001-2017.
Chimia (Aarau). 2018 Aug 22;72(7):518. doi: 10.2533/chimia.2018.518.
2
Delineating the role of cooperativity in the design of potent PROTACs for BTK.
Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):E7285-E7292. doi: 10.1073/pnas.1803662115. Epub 2018 Jul 16.
3
Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy.
J Hematol Oncol. 2018 Jun 20;11(1):84. doi: 10.1186/s13045-018-0624-2.
4
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation.
Biochemistry. 2018 Jul 3;57(26):3564-3575. doi: 10.1021/acs.biochem.8b00391. Epub 2018 Jun 14.
5
Kinase inhibitors: the road ahead.
Nat Rev Drug Discov. 2018 May;17(5):353-377. doi: 10.1038/nrd.2018.21. Epub 2018 Mar 16.
6
Kinase-targeted cancer therapies: progress, challenges and future directions.
Mol Cancer. 2018 Feb 19;17(1):48. doi: 10.1186/s12943-018-0804-2.
7
TGFβ attenuates tumour response to PD-L1 blockade by contributing to exclusion of T cells.
Nature. 2018 Feb 22;554(7693):544-548. doi: 10.1038/nature25501. Epub 2018 Feb 14.
8
Progress with covalent small-molecule kinase inhibitors.
Drug Discov Today. 2018 Mar;23(3):727-735. doi: 10.1016/j.drudis.2018.01.035. Epub 2018 Jan 11.
9
Drug resistance in anaplastic lymphoma kinase-rearranged lung cancer.
Cancer Sci. 2018 Mar;109(3):572-580. doi: 10.1111/cas.13504. Epub 2018 Feb 15.
10
New Perspectives, Opportunities, and Challenges in Exploring the Human Protein Kinome.
Cancer Res. 2018 Jan 1;78(1):15-29. doi: 10.1158/0008-5472.CAN-17-2291. Epub 2017 Dec 18.
Zotero 插件