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Items: 1 to 20 of 121

1.

Structural basis for benzothiazinone-mediated killing of Mycobacterium tuberculosis.

Neres J, Pojer F, Molteni E, Chiarelli LR, Dhar N, Boy-Röttger S, Buroni S, Fullam E, Degiacomi G, Lucarelli AP, Read RJ, Zanoni G, Edmondson DE, De Rossi E, Pasca MR, McKinney JD, Dyson PJ, Riccardi G, Mattevi A, Cole ST, Binda C.

Sci Transl Med. 2012 Sep 5;4(150):150ra121. doi: 10.1126/scitranslmed.3004395.

2.

Characterization of DprE1-Mediated Benzothiazinone Resistance in Mycobacterium tuberculosis.

Foo CS, Lechartier B, Kolly GS, Boy-Röttger S, Neres J, Rybniker J, Lupien A, Sala C, Piton J, Cole ST.

Antimicrob Agents Chemother. 2016 Oct 21;60(11):6451-6459. doi: 10.1128/AAC.01523-16. Print 2016 Nov.

3.

Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance.

Manina G, Bellinzoni M, Pasca MR, Neres J, Milano A, Ribeiro AL, Buroni S, Skovierová H, Dianišková P, Mikušová K, Marák J, Makarov V, Giganti D, Haouz A, Lucarelli AP, Degiacomi G, Piazza A, Chiarelli LR, De Rossi E, Salina E, Cole ST, Alzari PM, Riccardi G.

Mol Microbiol. 2010 Sep;77(5):1172-85. doi: 10.1111/j.1365-2958.2010.07277.x.

4.

Towards a new combination therapy for tuberculosis with next generation benzothiazinones.

Makarov V, Lechartier B, Zhang M, Neres J, van der Sar AM, Raadsen SA, Hartkoorn RC, Ryabova OB, Vocat A, Decosterd LA, Widmer N, Buclin T, Bitter W, Andries K, Pojer F, Dyson PJ, Cole ST.

EMBO Mol Med. 2014 Mar;6(3):372-83. doi: 10.1002/emmm.201303575. Epub 2014 Feb 5.

5.

Structure, dynamics, and interaction of Mycobacterium tuberculosis (Mtb) DprE1 and DprE2 examined by molecular modeling, simulation, and electrostatic studies.

Bhutani I, Loharch S, Gupta P, Madathil R, Parkesh R.

PLoS One. 2015 Mar 19;10(3):e0119771. doi: 10.1371/journal.pone.0119771. eCollection 2015.

6.

DprE1--from the discovery to the promising tuberculosis drug target.

Mikusová K, Makarov V, Neres J.

Curr Pharm Des. 2014;20(27):4379-403. Review.

PMID:
24245764
7.

Crystal structure of decaprenylphosphoryl-β- D-ribose 2'-epimerase from Mycobacterium smegmatis.

Li H, Jogl G.

Proteins. 2013 Mar;81(3):538-43. doi: 10.1002/prot.24220. Epub 2012 Dec 24.

8.

In vitro combination studies of benzothiazinone lead compound BTZ043 against Mycobacterium tuberculosis.

Lechartier B, Hartkoorn RC, Cole ST.

Antimicrob Agents Chemother. 2012 Nov;56(11):5790-3. doi: 10.1128/AAC.01476-12. Epub 2012 Aug 27.

9.

The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis.

Makarov V, Neres J, Hartkoorn RC, Ryabova OB, Kazakova E, Šarkan M, Huszár S, Piton J, Kolly GS, Vocat A, Conroy TM, Mikušová K, Cole ST.

Antimicrob Agents Chemother. 2015 Aug;59(8):4446-52. doi: 10.1128/AAC.00778-15. Epub 2015 May 18.

10.

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1.

Neres J, Hartkoorn RC, Chiarelli LR, Gadupudi R, Pasca MR, Mori G, Venturelli A, Savina S, Makarov V, Kolly GS, Molteni E, Binda C, Dhar N, Ferrari S, Brodin P, Delorme V, Landry V, de Jesus Lopes Ribeiro AL, Farina D, Saxena P, Pojer F, Carta A, Luciani R, Porta A, Zanoni G, De Rossi E, Costi MP, Riccardi G, Cole ST.

ACS Chem Biol. 2015 Mar 20;10(3):705-14. doi: 10.1021/cb5007163. Epub 2014 Dec 9.

PMID:
25427196
11.

Clinical isolates of Mycobacterium tuberculosis in four European hospitals are uniformly susceptible to benzothiazinones.

Pasca MR, Degiacomi G, Ribeiro AL, Zara F, De Mori P, Heym B, Mirrione M, Brerra R, Pagani L, Pucillo L, Troupioti P, Makarov V, Cole ST, Riccardi G.

Antimicrob Agents Chemother. 2010 Apr;54(4):1616-8. doi: 10.1128/AAC.01676-09. Epub 2010 Jan 19.

12.

Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1.

Trefzer C, Škovierová H, Buroni S, Bobovská A, Nenci S, Molteni E, Pojer F, Pasca MR, Makarov V, Cole ST, Riccardi G, Mikušová K, Johnsson K.

J Am Chem Soc. 2012 Jan 18;134(2):912-5. doi: 10.1021/ja211042r. Epub 2011 Dec 21.

PMID:
22188377
13.

Fluorescent Benzothiazinone Analogues Efficiently and Selectively Label Dpre1 in Mycobacteria and Actinobacteria.

Sommer R, Neres J, Piton J, Dhar N, van der Sar A, Mukherjee R, Laroche T, Dyson PJ, McKinney JD, Bitter W, Makarov V, Cole ST.

ACS Chem Biol. 2018 Nov 16;13(11):3184-3192. doi: 10.1021/acschembio.8b00790. Epub 2018 Oct 25.

PMID:
30289689
14.

Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis.

Makarov V, Manina G, Mikusova K, Möllmann U, Ryabova O, Saint-Joanis B, Dhar N, Pasca MR, Buroni S, Lucarelli AP, Milano A, De Rossi E, Belanova M, Bobovska A, Dianiskova P, Kordulakova J, Sala C, Fullam E, Schneider P, McKinney JD, Brodin P, Christophe T, Waddell S, Butcher P, Albrethsen J, Rosenkrands I, Brosch R, Nandi V, Bharath S, Gaonkar S, Shandil RK, Balasubramanian V, Balganesh T, Tyagi S, Grosset J, Riccardi G, Cole ST.

Science. 2009 May 8;324(5928):801-4. doi: 10.1126/science.1171583. Epub 2009 Mar 19.

15.

Benzothiazinones mediate killing of Corynebacterineae by blocking decaprenyl phosphate recycling involved in cell wall biosynthesis.

Grover S, Alderwick LJ, Mishra AK, Krumbach K, Marienhagen J, Eggeling L, Bhatt A, Besra GS.

J Biol Chem. 2014 Feb 28;289(9):6177-87. doi: 10.1074/jbc.M113.522623. Epub 2014 Jan 20.

16.

Benzothiazinones: prodrugs that covalently modify the decaprenylphosphoryl-β-D-ribose 2'-epimerase DprE1 of Mycobacterium tuberculosis.

Trefzer C, Rengifo-Gonzalez M, Hinner MJ, Schneider P, Makarov V, Cole ST, Johnsson K.

J Am Chem Soc. 2010 Oct 6;132(39):13663-5. doi: 10.1021/ja106357w.

PMID:
20828197
17.

Structural basis of inhibition of Mycobacterium tuberculosis DprE1 by benzothiazinone inhibitors.

Batt SM, Jabeen T, Bhowruth V, Quill L, Lund PA, Eggeling L, Alderwick LJ, Fütterer K, Besra GS.

Proc Natl Acad Sci U S A. 2012 Jul 10;109(28):11354-9. doi: 10.1073/pnas.1205735109. Epub 2012 Jun 25.

18.

Development of selective DprE1 inhibitors: Design, synthesis, crystal structure and antitubercular activity of benzothiazolylpyrimidine-5-carboxamides.

Chikhale R, Menghani S, Babu R, Bansode R, Bhargavi G, Karodia N, Rajasekharan MV, Paradkar A, Khedekar P.

Eur J Med Chem. 2015;96:30-46. doi: 10.1016/j.ejmech.2015.04.011. Epub 2015 Apr 7.

PMID:
25874329
19.

Bridging the gap between a TB drug and its target.

Cook GM, Heikal A.

Sci Transl Med. 2012 Sep 5;4(150):150fs33. doi: 10.1126/scitranslmed.3004816.

PMID:
22956196
20.

4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.

Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR.

J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11.

PMID:
24871036

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