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1.

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
2.

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
3.

Antituberculars which target decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1: state of art.

Buroni S, Pasca MR, de Jesus Lopes Ribeiro AL, Degiacomi G, Molteni E, Riccardi G.

Appl Microbiol Biotechnol. 2012 May;94(4):907-16. doi: 10.1007/s00253-012-4013-4. Epub 2012 Apr 18. Review. Retraction in: Appl Microbiol Biotechnol. 2012 Sep;95(5):1369.

PMID:
22526781
4.

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
5.

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.

6.

Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.

Panda M, Ramachandran S, Ramachandran V, Shirude PS, Humnabadkar V, Nagalapur K, Sharma S, Kaur P, Guptha S, Narayan A, Mahadevaswamy J, Ambady A, Hegde N, Rudrapatna SS, Hosagrahara VP, Sambandamurthy VK, Raichurkar A.

J Med Chem. 2014 Jun 12;57(11):4761-71. doi: 10.1021/jm5002937. Epub 2014 May 22.

PMID:
24818517
7.

Decaprenylphosphoryl-β-D-ribose 2'-epimerase from Mycobacterium tuberculosis is a magic drug target.

Manina G, Pasca MR, Buroni S, De Rossi E, Riccardi G.

Curr Med Chem. 2010;17(27):3099-108. Review.

PMID:
20629622
8.

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
9.

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.

10.

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.

11.
12.

Azaindoles: noncovalent DprE1 inhibitors from scaffold morphing efforts, kill Mycobacterium tuberculosis and are efficacious in vivo.

Shirude PS, Shandil R, Sadler C, Naik M, Hosagrahara V, Hameed S, Shinde V, Bathula C, Humnabadkar V, Kumar N, Reddy J, Panduga V, Sharma S, Ambady A, Hegde N, Whiteaker J, McLaughlin RE, Gardner H, Madhavapeddi P, Ramachandran V, Kaur P, Narayan A, Guptha S, Awasthy D, Narayan C, Mahadevaswamy J, Vishwas KG, Ahuja V, Srivastava A, Prabhakar KR, Bharath S, Kale R, Ramaiah M, Choudhury NR, Sambandamurthy VK, Solapure S, Iyer PS, Narayanan S, Chatterji M.

J Med Chem. 2013 Dec 12;56(23):9701-8. doi: 10.1021/jm401382v. Epub 2013 Nov 21.

PMID:
24215368
13.

8-Pyrrole-benzothiazinones non-covalent 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 May 18. pii: AAC.00778-15. [Epub ahead of print]

PMID:
25987616
14.

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.

PMID:
20624223
15.

Identification of a small molecule with activity against drug-resistant and persistent tuberculosis.

Wang F, Sambandan D, Halder R, Wang J, Batt SM, Weinrick B, Ahmad I, Yang P, Zhang Y, Kim J, Hassani M, Huszar S, Trefzer C, Ma Z, Kaneko T, Mdluli KE, Franzblau S, Chatterjee AK, Johnsson K, Mikusova K, Besra GS, Fütterer K, Robbins SH, Barnes SW, Walker JR, Jacobs WR Jr, Schultz PG.

Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):E2510-7. doi: 10.1073/pnas.1309171110. Epub 2013 Jun 17. Erratum in: Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15848. Robbins, Scott H [added]; Barnes, S Whitney [added]; Walker, John R [added]; Johnson, Kai [corrected to Johnsson, Kai].

16.

Thiolates chemically induce redox activation of BTZ043 and related potent nitroaromatic anti-tuberculosis agents.

Tiwari R, Moraski GC, Krchňák V, Miller PA, Colon-Martinez M, Herrero E, Oliver AG, Miller MJ.

J Am Chem Soc. 2013 Mar 6;135(9):3539-49. doi: 10.1021/ja311058q. Epub 2013 Feb 25.

17.

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.

18.

The DprE1 enzyme, one of the most vulnerable targets of Mycobacterium tuberculosis.

Riccardi G, Pasca MR, Chiarelli LR, Manina G, Mattevi A, Binda C.

Appl Microbiol Biotechnol. 2013 Oct;97(20):8841-8. doi: 10.1007/s00253-013-5218-x. Epub 2013 Sep 14. Review.

PMID:
24037308
19.

Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis.

Ribeiro AL, Degiacomi G, Ewann F, Buroni S, Incandela ML, Chiarelli LR, Mori G, Kim J, Contreras-Dominguez M, Park YS, Han SJ, Brodin P, Valentini G, Rizzi M, Riccardi G, Pasca MR.

PLoS One. 2011;6(11):e26675. doi: 10.1371/journal.pone.0026675. Epub 2011 Nov 1.

20.

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.

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