메뉴 건너뛰기




Volumn 12, Issue 5, 2017, Pages 1390-1396

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays

Author keywords

[No Author keywords available]

Indexed keywords

CARBAMIC ACID; ETHIONAMIDE; ETHR PROTEIN; PROTEIN; SULFONAMIDE; UNCLASSIFIED DRUG; BACTERIAL PROTEIN; ENZYME INHIBITOR; ETHR PROTEIN, MYCOBACTERIUM TUBERCULOSIS; LIGAND; REPRESSOR PROTEIN; TUBERCULOSTATIC AGENT;

EID: 85019649436     PISSN: 15548929     EISSN: 15548937     Source Type: Journal    
DOI: 10.1021/acschembio.7b00091     Document Type: Article
Times cited : (26)

References (21)
  • 1
    • 85019576523 scopus 로고    scopus 로고
    • World Health Organization, Global tuberculosis report
    • World Health Organization, Global tuberculosis report, (2015; http://www.who.int/tb/publications/global-report/gtbr2015-executive-summary.pdf.
    • (2015)
  • 2
    • 85019598132 scopus 로고    scopus 로고
    • World Health Organization, 2011/ 2012 tuberculosis global facts
    • World Health Organization, 2011/ 2012 tuberculosis global facts, (2011.
    • (2011)
  • 3
    • 84863764493 scopus 로고    scopus 로고
    • World Health Organization. 4th ed. WHO Press: Geneva, Switzerland
    • World Health Organization. Guidelines for treatment of tuberculosis, 4th ed.; WHO Press: Geneva, Switzerland, 2010.
    • (2010) Guidelines for Treatment of Tuberculosis
  • 4
    • 80053351516 scopus 로고    scopus 로고
    • Tuberculosis vaccines: Progress and challenges
    • Checkley, A. M. and McShane, H. (2011) Tuberculosis vaccines: progress and challenges Trends Pharmacol. Sci. 32, 601-606 10.1016/j.tips.2011.06.003
    • (2011) Trends Pharmacol. Sci. , vol.32 , pp. 601-606
    • Checkley, A.M.1    McShane, H.2
  • 5
    • 85011421635 scopus 로고    scopus 로고
    • Drug development pipeline for the treatment of tuberculosis: Needs, challenges, success and opportunities for the future
    • Anand, N., Upadhyaya, K., and Tripathi, R. P. (2015) Drug development pipeline for the treatment of tuberculosis: Needs, challenges, success and opportunities for the future Chem. Biol. Interface 5, 84-127
    • (2015) Chem. Biol. Interface , vol.5 , pp. 84-127
    • Anand, N.1    Upadhyaya, K.2    Tripathi, R.P.3
  • 6
    • 79251589638 scopus 로고    scopus 로고
    • The challenge of new drug discovery for tuberculosis
    • Koul, A., Arnoult, E., Lounis, N., Guillemont, N., and Andries, K. (2011) The challenge of new drug discovery for tuberculosis Nature 469, 483-490 10.1038/nature09657
    • (2011) Nature , vol.469 , pp. 483-490
    • Koul, A.1    Arnoult, E.2    Lounis, N.3    Guillemont, N.4    Andries, K.5
  • 9
    • 0032472224 scopus 로고    scopus 로고
    • Modification of the NADH of the isoniazid target (InhA) from Mycobacterium tuberculosis
    • Rozwarski, D. A., Grant, G. A., Barton, D. H. R., Jacobs, W. R., Jr., and Sacchettini, J. C. (1998) Modification of the NADH of the isoniazid target (InhA) from Mycobacterium tuberculosis Science 279, 98-102 10.1126/science.279.5347.98
    • (1998) Science , vol.279 , pp. 98-102
    • Rozwarski, D.A.1    Grant, G.A.2    Barton, D.H.R.3    Jacobs, W.R.4    Sacchettini, J.C.5
  • 11
    • 34250198660 scopus 로고    scopus 로고
    • The Mycobacterium tuberculosis FAS-II condensing enzymes: Their role in mycolic acid biosynthesis, acid-fastness, pathogenesis and in future drug development
    • Bhatt, A., Molle, V., Besra, G. S., Jacobs, W. R., Jr., and Kremer, L. (2007) The Mycobacterium tuberculosis FAS-II condensing enzymes: their role in mycolic acid biosynthesis, acid-fastness, pathogenesis and in future drug development Mol. Microbiol. 64, 1442-1454 10.1111/j.1365-2958.2007.05761.x
    • (2007) Mol. Microbiol. , vol.64 , pp. 1442-1454
    • Bhatt, A.1    Molle, V.2    Besra, G.S.3    Jacobs, W.R.4    Kremer, L.5
  • 12
    • 0026705772 scopus 로고
    • The catalase-peroxidase gene and isoniazid resistance of Mycobacterium tuberculosis
    • Zhang, Y., Heym, B., Allen, B., Young, D., and Cole, S. (1992) The catalase-peroxidase gene and isoniazid resistance of Mycobacterium tuberculosis Nature 358, 591-593 10.1038/358591a0
    • (1992) Nature , vol.358 , pp. 591-593
    • Zhang, Y.1    Heym, B.2    Allen, B.3    Young, D.4    Cole, S.5
  • 13
    • 0346964261 scopus 로고    scopus 로고
    • EthR, a repressor of the TetR/CamR family implicated in ethionamide resistance in mycobacteria, octamerizes cooperatively on its operator
    • Engohang-Ndong, J., Baillat, D., Aumercier, M., Bellefontaine, F., Besra, G. S., Locht, C., and Baulard, A. R. (2004) EthR, a repressor of the TetR/CamR family implicated in ethionamide resistance in mycobacteria, octamerizes cooperatively on its operator Mol. Microbiol. 51, 175-188 10.1046/j.1365-2958.2003.03809.x
    • (2004) Mol. Microbiol. , vol.51 , pp. 175-188
    • Engohang-Ndong, J.1    Baillat, D.2    Aumercier, M.3    Bellefontaine, F.4    Besra, G.S.5    Locht, C.6    Baulard, A.R.7
  • 15
    • 0034662963 scopus 로고    scopus 로고
    • Ethionamide activation and sensitivity in multidrug-resistant Mycobacterium tuberculosis
    • DeBarber, A. E., Mdluli, K., Bosman, M., Bekker, L. G., and Barry, C. E., 3rd (2000) Ethionamide activation and sensitivity in multidrug-resistant Mycobacterium tuberculosis Proc. Natl. Acad. Sci. U. S. A. 97, 9677-9682 10.1073/pnas.97.17.9677
    • (2000) Proc. Natl. Acad. Sci. U. S. A. , vol.97 , pp. 9677-9682
    • DeBarber, A.E.1    Mdluli, K.2    Bosman, M.3    Bekker, L.G.4    Barry, C.E.5
  • 19
    • 84894266263 scopus 로고    scopus 로고
    • A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR
    • Surade, S., Ty, N., Hengrung, N., Lechartier, B., Cole, S. T., Abell, C., and Blundell, T. L. (2014) A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR Biochem. J. 458, 387-394 10.1042/BJ20131127
    • (2014) Biochem. J. , vol.458 , pp. 387-394
    • Surade, S.1    Ty, N.2    Hengrung, N.3    Lechartier, B.4    Cole, S.T.5    Abell, C.6    Blundell, T.L.7
  • 20
    • 84959018166 scopus 로고    scopus 로고
    • A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters
    • Nikiforov, P. O., Surade, S., Blaszczyk, M., Delorme, V., Brodin, P., Baulard, A. R., Blundell, T. L., and Abell, C. (2016) A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters Org. Biomol. Chem. 14, 2318-2326 10.1039/C5OB02630J
    • (2016) Org. Biomol. Chem. , vol.14 , pp. 2318-2326
    • Nikiforov, P.O.1    Surade, S.2    Blaszczyk, M.3    Delorme, V.4    Brodin, P.5    Baulard, A.R.6    Blundell, T.L.7    Abell, C.8


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.