Structural and biophysical insights into the mode of covalent binding of rationally designed potent BMX inhibitors-Reference-Cited by-同舟云学术

登录注册会员服务联系我们

Structural and biophysical insights into the mode of covalent binding of rationally designed potent BMX inhibitors

Published:2020 Issue:4 Volume:1 Page:251-262
ISSN:2633-0679
Container-title:RSC Chemical Biology
language:en
Short-container-title:RSC Chem. Biol.

Author:

Seixas João D.¹²³⁴⁵,Sousa Bárbara B.¹²³⁴⁵,Marques Marta C.¹²³⁴⁵,Guerreiro Ana¹²³⁴⁵,Traquete Rui¹²³⁴⁵,Rodrigues Tiago¹²³⁴⁵^ORCID,Albuquerque Inês S.¹²³⁴⁵^ORCID,Sousa Marcos F. Q.⁶⁷⁸⁵⁹,Lemos Ana R.⁶⁷⁸⁵⁹,Sousa Pedro M. F.⁶⁷⁸⁵⁹,Bandeiras Tiago M.⁶⁷⁸⁵⁹,Wu Di¹⁰¹¹¹²¹³,Doyle Shelby K.¹⁴¹⁵¹⁶¹⁷,Robinson Carol V.¹⁰¹¹¹²¹³^ORCID,Koehler Angela N.¹⁴¹⁵¹⁶¹⁷,Corzana Francisco¹⁸¹⁹²⁰²¹²²^ORCID,Matias Pedro M.⁶⁷⁸⁵⁹,Bernardes Gonçalo J. L.¹²³⁴⁵^ORCID

Affiliation:

1. Instituto de Medicina Molecular João Lobo Antunes

2. Faculdade de Medicina

3. Universidade de Lisboa

4. 1649-028 Lisboa

5. Portugal

6. Instituto de Tecnologia Química e Biológica António Xavier

7. Universidade Nova de Lisboa

8. 2780-157 Oeiras

9. IBET - Instituto de Biologia Experimental e Tecnológica

10. Department of Chemistry

11. University of Oxford

12. Oxford

13. UK

14. David H. Koch Institute for Integrative Cancer Research

15. Massachusetts Institute of Technology

16. Cambridge

17. USA

18. Departamento de Química

19. Universidad de La Rioja

20. Centro de Investigación en Síntesis Química

21. 26006 Logroño

22. Spain

Abstract

We identified potent, functionalisable BMX inhibitors and revealed their covalent mode of binding to BMX by X-ray crystallography.

Funder

Ministerio de Economía y Competitividad

H2020 Marie Skłodowska-Curie Actions

Fundação para a Ciência e a Tecnologia

Wellcome Trust

H2020 Spreading Excellence and Widening Participation

Royal Society

National Science Foundation

Publisher

Royal Society of Chemistry (RSC)

Subject

Biochemistry, Genetics and Molecular Biology (miscellaneous),Molecular Biology,Biochemistry,Chemistry (miscellaneous)

Link

http://pubs.rsc.org/en/content/articlepdf/2020/CB/D0CB00033G

Reference51 articles.

1. The resurgence of covalent drugs

2. Progress with covalent small-molecule kinase inhibitors

3. The Cysteinome of Protein Kinases as a Target in Drug Development

4. Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks

5. Covalent inhibitors: an opportunity for rational target selectivity

Cited by 8 articles. 订阅此论文施引文献订阅此论文施引文献，注册后可以免费订阅5篇论文的施引文献，订阅后可以查看论文全部施引文献

1. BMX controls 3βHSD1 and sex steroid biosynthesis in cancer;Journal of Clinical Investigation;2023-01-17

2. Insights and Future Perspectives of Covalent Protein Degraders;Inducing Targeted Protein Degradation;2022-11-25

3. Selective Inhibition of Bruton’s Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors;ACS Pharmacology & Translational Science;2022-11-02

4. BMX kinase mediates gilteritinib resistance in FLT3-mutated AML through microenvironmental factors;BLOOD ADV;2022

5. BMX kinase mediates gilteritinib resistance inFLT3-mutated AML through microenvironmental factors;Blood Advances;2022-08-31

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线，采集、加工和组织学术论文而形成的新型学术文献查询和分析系统，可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容，当前同舟云学术共收录了国内外主流学术期刊6万余种，收集的期刊论文及会议论文总量共计约1.5亿篇，并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询！咨询电话：010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号京ICP备18003416号-3