The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K-Reference-Cited by-同舟云学术

The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K

Published:2019-01-28 Issue:8 Volume:141 Page:3507-3514
ISSN:0002-7863
Container-title:Journal of the American Chemical Society
language:en
Short-container-title:J. Am. Chem. Soc.

Author:

Mons Elma¹²^ORCID,Jansen Ineke D. C.³,Loboda Jure⁴⁵,van Doodewaerd Bjorn R.¹,Hermans Jill¹,Verdoes Martijn⁶^ORCID,van Boeckel Constant A. A.⁷,van Veelen Peter A.⁸,Turk Boris⁴⁹,Turk Dusan⁴¹⁰,Ovaa Huib¹²^ORCID

Affiliation:

1. Department of Cell and Chemical Biology, Oncode Institute, Leiden University Medical Center, 2300 RC Leiden, The Netherlands

2. Division of Cell Biology, Netherlands Cancer Institute, 1066 CX Amsterdam, The Netherlands

3. Department of Periodontology, Academic Center For Dentistry Amsterdam (ACTA), 1081 LA Amsterdam, The Netherlands

4. Department of Biochemistry and Molecular and Structural Biology, Jožef Stefan Institute, Ljubljana 1000, Slovenia

5. Jožef Stefan International Postgraduate School, Ljubljana 1000, Slovenia

6. Department of Tumor Immunology, Institute for Molecular Life Sciences Radboud UMC, 6525 GA Nijmegen, The Netherlands

7. Leiden Institute of Chemistry, Leiden University, 2311 EZ Leiden, The Netherlands

8. Centre for Proteomics and Metabolomics, Leiden University Medical Center, 2333 ZA Leiden, The Netherlands

9. Faculty of Chemistry and Chemical Technology, University of Ljubljana, Ljubljana 1000, Slovenia

10. Centre of Excellence for Integrated Approaches in Chemistry and Biology of Proteins, Ljubljana 1000, Slovenia

Funder

Javna Agencija za Raziskovalno Dejavnost RS

Nederlandse Organisatie voor Wetenschappelijk Onderzoek

Publisher

American Chemical Society (ACS)

Subject

Colloid and Surface Chemistry,Biochemistry,General Chemistry,Catalysis

Link

http://pubs.acs.org/doi/pdf/10.1021/jacs.8b11027

Reference58 articles.

1. The resurgence of covalent drugs

2. Covalent inhibitors in drug discovery: from accidental discoveries to avoided liabilities and designed therapies

3. A comparative study of warheads for design of cysteine protease inhibitors

4. Expanding the Armory: Predicting and Tuning Covalent Warhead Reactivity

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

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