Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen
The L,D-transpeptidases (Ldts) are promising antibiotic targets for treating tuberculosis. We report screening of cysteine-reactive inhibitors against LdtMt2 from Mycobacterium tuberculosis. Structural studies on LdtMt2 with potent inhibitor ebselen reveal opening of the benzisoselenazolone ring by...
| Main Authors: | , , , , , , , |
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| Format: | Journal article |
| Published: |
Royal Society of Chemistry
2019
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| _version_ | 1797064197370019840 |
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| author | De Munnik, M Lohans, CT Lang, PA Langley, G Malla, TR Tumber, A Schofield, C Brem, J |
| author_facet | De Munnik, M Lohans, CT Lang, PA Langley, G Malla, TR Tumber, A Schofield, C Brem, J |
| author_sort | De Munnik, M |
| collection | OXFORD |
| description | The L,D-transpeptidases (Ldts) are promising antibiotic targets for treating tuberculosis. We report screening of cysteine-reactive inhibitors against LdtMt2 from Mycobacterium tuberculosis. Structural studies on LdtMt2 with potent inhibitor ebselen reveal opening of the benzisoselenazolone ring by a nucleophilic cysteine, forming a complex involving extensive hydrophobic interactions with a substrate-binding loop. |
| first_indexed | 2024-03-06T21:10:48Z |
| format | Journal article |
| id | oxford-uuid:3e16fb22-e697-412c-b913-4757c08a9e43 |
| institution | University of Oxford |
| last_indexed | 2024-03-06T21:10:48Z |
| publishDate | 2019 |
| publisher | Royal Society of Chemistry |
| record_format | dspace |
| spelling | oxford-uuid:3e16fb22-e697-412c-b913-4757c08a9e432022-03-26T14:23:23ZTargeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselenJournal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:3e16fb22-e697-412c-b913-4757c08a9e43Symplectic Elements at OxfordRoyal Society of Chemistry2019De Munnik, MLohans, CTLang, PALangley, GMalla, TRTumber, ASchofield, CBrem, JThe L,D-transpeptidases (Ldts) are promising antibiotic targets for treating tuberculosis. We report screening of cysteine-reactive inhibitors against LdtMt2 from Mycobacterium tuberculosis. Structural studies on LdtMt2 with potent inhibitor ebselen reveal opening of the benzisoselenazolone ring by a nucleophilic cysteine, forming a complex involving extensive hydrophobic interactions with a substrate-binding loop. |
| spellingShingle | De Munnik, M Lohans, CT Lang, PA Langley, G Malla, TR Tumber, A Schofield, C Brem, J Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen |
| title | Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen |
| title_full | Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen |
| title_fullStr | Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen |
| title_full_unstemmed | Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen |
| title_short | Targeting the Mycobacterium tuberculosis transpeptidase LdtMt2 with cysteine-reactive inhibitors including ebselen |
| title_sort | targeting the mycobacterium tuberculosis transpeptidase ldtmt2 with cysteine reactive inhibitors including ebselen |
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