Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis

Author:

Neres João123,Pojer Florence12,Molteni Elisabetta14,Chiarelli Laurent R.14,Dhar Neeraj12,Boy-Röttger Stefanie12,Buroni Silvia14,Fullam Elizabeth12,Degiacomi Giulia14,Lucarelli Anna Paola4,Read Randy J.5,Zanoni Giuseppe6,Edmondson Dale E.7,De Rossi Edda14,Pasca Maria Rosalia14,McKinney John D.12,Dyson Paul J.3,Riccardi Giovanna14,Mattevi Andrea4,Cole Stewart T.12,Binda Claudia14

Affiliation:

1. More Medicines for Tuberculosis (MM4TB) Consortium.

2. Global Health Institute, École Polytechnique Fédérale de Lausanne, CH-1015 Lausanne, Switzerland.

3. Institute of Chemical Sciences and Engineering, École Polytechnique Fédérale de Lausanne, CH-1015 Lausanne, Switzerland.

4. Department of Biology and Biotechnology, University of Pavia, Via Ferrata 9, 27100 Pavia, Italy.

5. Department of Haematology, University of Cambridge, Cambridge Institute for Medical Research, Wellcome Trust/MRC Building, Hills Road, Cambridge CB2 0XY, UK.

6. Department of Chemistry, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy.

7. Department of Biochemistry, Emory University, Atlanta, GA 30322, USA.

Abstract

The crystal structure of the mycobacterial DprE1 reveals how the TB drug benzothiazinone BTZ043 blocks this microbial enzyme target.

Publisher

American Association for the Advancement of Science (AAAS)

Subject

General Medicine

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