Hydroxylammonium derivatives for selective active-site lysine modification in the anti-virulence bacterial target DHQ1 enzyme-Reference-Cited by-同舟云学术

Hydroxylammonium derivatives for selective active-site lysine modification in the anti-virulence bacterial target DHQ1 enzyme

Published:2019 Issue:17 Volume:6 Page:3127-3135
ISSN:2052-4129
Container-title:Organic Chemistry Frontiers
language:en
Short-container-title:Org. Chem. Front.

Author:

Maneiro María¹²³⁴⁵^ORCID,Lence Emilio¹²³⁴⁵^ORCID,Sanz-Gaitero Marta⁶⁷⁸⁵,Otero José M.¹²³⁴⁵^ORCID,van Raaij Mark J.⁶⁷⁸⁵^ORCID,Thompson Paul⁹¹⁰¹¹¹²¹³^ORCID,Hawkins Alastair R.⁹¹⁰¹¹¹²¹³,González-Bello Concepción¹²³⁴⁵^ORCID

Affiliation:

1. Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS)

2. Departamento de Química Orgánica

3. Universidade de Santiago de Compostela

4. 15782 Santiago de Compostela

5. Spain

6. Departamento de Estructura de Macromoléculas

7. Centro Nacional de Biotecnología (CSIC)

8. 28049 Madrid

9. Institute of Cell and Molecular Biosciences

10. Medical School

11. University of Newcastle upon Tyne

12. Newcastle upon Tyne NE2 4HH

13. UK

Abstract

The first example of a hydroxylammonium derivative that causes a specific covalent modification of the active-site lysine residue of an aldolase enzyme, which is a promising target for anti-bacterial drug discovery, is reported.

Funder

Secretaría de Estado de Investigación, Desarrollo e Innovación

Consellería de Cultura, Educación e Ordenación Universitaria, Xunta de Galicia

European Regional Development Fund

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2019/QO/C9QO00453J

Reference38 articles.

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