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Publications

 

2011

 

1.     Cole, S.T. and Riccardi, G. (2011). New tuberculosis drugs on the horizon. Current opinion in microbiology 14: 570-576.

 

2.     Ribeiro A.L., Degiacomi G., Ewann F., Buroni S., Incandela M.L., Chiarelli L.R., Mori G., Kim J., Contreras-Dominguez M., Park Y.S., Han .SJ., Brodin P., Valentini G., Rizzi M., Riccardi G., Pasca M.R.. (2011). Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis.  PLoS One.; 6 (11):e26675.

 

2012

 

3.     Buroni, S., Pasca, M.R., de Jesus Lopes Ribeiro, A.L., Degiacomi, G., Molteni, E., and Riccardi, G. (2012) Antituberculars which target decaprenylphosphoryl-[beta]-D-ribofuranose 2'-oxidase DprE1: state of art. App. Microbiol. Biotechnol. 94: 907-916.

 

4.      Di Luca M., Bottai D., Batoni G., Orgeur M., Aulicino A., Counoupas C., Campa M., Brosch R., and Esin S. (2012). The ESX-5 associated eccB-eccC locus is essential for Mycobacterium tuberculosis viability. PLoS One. 7(12):e52059.

 

5.     Fullam, E., F. Pojer, T. Bergfors, T. A. Jones and Cole, S. T.  (2012). Structure and function of the transketolase from Mycobacterium tuberculosis and comparison with the human enzyme. Open biology 2: 110026.

 

6.     Glaus F., and Altmann K.H. (2012). Total synthesis of the bacterial RNA polymerase inhibitor ripostatin B. Angew Chem Int Ed Engl. 2;51(14):3405-3409.

 

7.     Godbole, A.A., Leelaram, M.N., Bhat, A.G., Jain, P and Nagaraja, V. (2012). Characterization of DNA topoisomerase I from Mycobacterium tuberculosis: DNA cleavage and religation properties and inhibition of its activity.  Arch. Biochem.Biophys. 528, 197-203.

 

8.     Hartkoorn, R. C., C. Sala, J. Neres, F. Pojer, S. Magnet, R. Mukherjee, S. Uplekar, S. Boy-Rottger, K. H. Altmann and S. T. Cole, (2012). Towards a new tuberculosis drug: pyridomycin - nature's isoniazid. EMBO molecular medicine 4: 1032-1042.

 

9.     Horlacher O.P., Hartkoorn R.C., Cole S.T., and Altmann K.H. (2012). Synthesis and antimycobacterial activity of 2,1'-dihydropyridomycins. ACS Med Chem Lett. 18;4(2):264-268.

 

10.  James J.N., Hasan Z.U., Ioerger T.R., Brown A.C., Personne Y., Carroll P., Ikeh M., Tilston-Lunel N.L., Palavecino C., Sacchettini J.C., and Parish T. (2012). Deletion of SenX3-RegX3, a key two-component regulatory system of Mycobacterium smegmatis, results in growth defects under phosphate-limiting conditions. Microbiology. 158(Pt 11):2724-2731.

 

11.  Komarova, E.S., Makarov, V.A., and Granik, V.G. (2012). Synthesis of Pyrazolo[3,4-b]pyridin-6-ones. J. Hetrocyclic Chem. 49(5):969-998.

 

12.  Lechartier, B., R. C. Hartkoorn & S. T. Cole, (2012). In vitro combination studies of benzothiazinone lead compound BTZ043 against Mycobacterium tuberculosis. Antimicrobial agents and chemotherapy 56: 5790-5793.

 

13.  Leelaram, M.N., Bhat, A.G., Hegde, S.M., Manjunath, R. and Nagaraja, V. (2012) Inhibition of type IA topoisomerase by perturbation of DNA cleavage-religation equilibrium. FEBS J. 279, 55-65.

 

14.  Moser SJohnsson K. (2012). Yeast three-hybrid screening for identifying anti-tuberculosis drug targets. Chembiochem.  25;14(17):2239-2242.

 

15.  Neres, J., F. Pojer, E. Molteni, L. R. Chiarelli, N. Dhar, S. Boy-Rottger, S. Buroni, E. Fullam, G. Degiacomi, A. P. Lucarelli, R. J. Read, G. Zanoni, D. E. Edmondson, E. De Rossi, M. R. Pasca, J. D. McKinney, P. J. Dyson, G. Riccardi, A. Mattevi, S. T. Cole & C. Binda, (2012). Structural basis for benzothiazinone-mediated killing of Mycobacterium tuberculosis. Science translational medicine 4: 150ra121.

 

16.  Ramon-Garcia S., Mick V., Dainese E., Martin C., Thompson C.J., De Rossi E., Manganelli R., and Ainsa J.A. (2012). Functional and genetic characterization of the tap efflux pump in Mycobacterium bovis BCG. Antimicrob Agents Chemother. 56(4):2074-2083.

 

17.  Trefzer, C., H. Skovierova, S. Buroni, A. Bobovska, S. Nenci, E. Molteni, F. Pojer, M. R. Pasca, V. Makarov, S. T. Cole, G. Riccardi, K. Mikusova & K. Johnsson, (2012). Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-beta-D-ribofuranose 2'-oxidase DprE1. Journal of the American Chemical Society 134: 912-915.

 

18.  Urresti S, Albesa-Jove D., Schaeffer F., Pham H.T., Kaur D., Gest P, van der Woerd M.J., Carreras-Gonzalez A., Lopez-Fernandez S., Alzari P.M., Brennan P.J., Jackson M., and Guerin M.E. (2012). Mechanistic insights into the retaining glucosyl-3-phosphoglycerate synthase from mycobacteria. J. Biol. Chem.  287(29):24649-24661.

 

19.  Zhang, M., C. Sala, R. C. Hartkoorn, N. Dhar, A. Mendoza-Losana and S. T. Cole, (2012) Streptomycin-starved Mycobacterium tuberculosis 18b, a drug discovery tool for latent tuberculosis. Antimicrobial agents and chemotherapy 56: 5782-5789.

 

2013

20.  Ahmed, W., Bhat, A.G., Leelaram, M.N., Menon, S. and Nagaraja, V. (2013). Carboxyl terminal domain basic amino acids of mycobacterial topoisomerase I bind DNA to promote strand passage. Nucleic Acids Res. 4, 7462-7471.

 

21.  Giganti D, Alegre-Cebollada J, Urresti S, Albesa-Jove D, Rodrigo-Unzueta A, Comino N, Kachala M, Lopez-Fernandez S, Svergun DI, Fernandez JM, Guerin ME. (2013). Conformational plasticity of the essential membrane-associated mannosyltransferase PimA from mycobacteria. J. Biol. Chem.  288(41):29797-29808.

 

22.  Horlacher, O. P., R. C. Hartkoorn, S. T. Cole & K. H. Altmann, (2013) Synthesis and antimycobacterial activity of 2,1'-dihydropyridomycins. ACS medicinal chemistry letters 4: 264-268.

 

23.  Incandela M.L., Perrin E., Fondi M., de Jesus Lopes Ribeiro A.L., Mori G., Moiana A., Gramegna M., Fani R., Riccardi G., and Pasca M.R. (2013). DprE1, a new taxonomic marker in mycobacteria. FEMS Microbiol Lett. 348:66-73.

 

24.  Karkare, S., Brown, A. C., Parish, T. and Maxwell, A. (2013). Identification of the transcriptional start of Mycobacterium tuberculosis GyrB. BMC Res Notes 6, 274.

 

25.  Karkare, S., Chung, T. T., Collin, F., Mitchenall, L. A., McKay, A. R., Greive, S. J., Meyer, J. J., Lall, N. and Maxwell, A. (2013). The naphthoquinone diospyrin is an inhibitor of DNA gyrase with a novel mechanism of action. J Biol Chem 288, 5149-5156.

 

26.  Lattova, E., Svetlikova, Z., and Mikusova, K. (2013). Novel synthetic (1 -> 6)-alpha-D-mannodisaccharide substrates support processive mannosylation catalysed by the mycobacterial cell envelope enzyme fraction. RSC Advances 3(39):17784-17792.

 

27.  Leelaram, M.N., Bhat, A.G., Godbole, A. A., Bhat, R., Manjunath, R. and Nagaraja, V. (2013) Type IA topoisomerase inhibition by clamp closure. FASEB J, 27, 3030-3038.

 

28.  Riccardi G, Pasca MR, Chiarelli LR, Manina G, Mattevi A, and Binda C. (2013). The DprE1 enzyme, one of the most vulnerable targets of Mycobacterium tuberculosis. Appl Microbiol Biotechnol. 97:8841-8848.

 

29.  Rodrigues L., Villellas C., Bailo R., Viveiros M., and Ainsa J.A.. (2013). Role of the Mmr efflux pump in drug resistance in Mycobacterium tuberculosis. Antimicrob Agents Chemother. 57(2):751-757.

 

30.  Ruggiero A., Marchant J., Squeglia F., Makarov V., De Simone A., and Berisio R. (2013). Molecular determinants of inactivation of the resuscitation promoting factor B from Mycobacterium tuberculosis. J Biomol Struct Dyn. 31(2):195-205.

 

31.  Supply P., Marceau M., Mangenot S., Roche D., Rouanet C., Khanna V., Majlessi L., Criscuolo A., Tap J., Pawlik A., Fiette L., Orgeur M., Fabre M., Parmentier C., Frigui W., Simeone R., Boritsch E.C., Debrie A.S., Willery E., Walker D., Quail M.A., Ma L., Bouchier C., Salvignol G., Sayes F., Cascioferro A., Seemann T., Barbe V., Locht C., Gutierrez M.C., Leclerc C., Bentley S.D., Stinear T.P., Brisse S., Medigue C., Parkhill J., Cruveiller S., and Brosch R. (2013). Genomic analysis of smooth tubercle bacilli provides insights into ancestry and pathoadaptation of Mycobacterium tuberculosis. Nat Genet. 45(2):172-179.

 

32.  Uplekar S., Rougemont J., Cole S.T., and Sala C. (2013). High-resolution transcriptome and genome-wide dynamics of RNA polymerase and NusA in Mycobacterium tuberculosis. Nucleic Acids Res. 41(2):961-977.

 

33.  Ventura M., Rieck B., Boldrin F., Degiacomi G., Bellinzoni M., Barilone N., Alzaidi F., Alzari P.M., Manganelli R., and O'Hare H.M. (2013) GarA is an essential regulator of metabolism in Mycobacterium tuberculosis. Mol Microbiol. 90:356-366.

 

34.  Wang F., Sambandan D., Halder R., Wang J., Batt S.M., Weinrick B., Ahmad I., Yang P., Zhang Y., Kim J., Hassani M., Huszar S., Trefzer C., Ma Z., Kaneko T., Mdluli K.E., Franzblau S., Chatterjee A.K., Johnsson K., Mikusova K., Besra G.S., Futterer K., Robbins S.H., Barnes S.W., Walker J.R., Jacobs W.R. Jr, and Schultz P.G. (2013). Identification of a small molecule with activity against drug-resistant and persistent tuberculosis. Proc Natl Acad Sci USA. 110(27):E2510-2517.

 

35.  Zumla, A., P. Nahid & S. T. Cole, (2013). Advances in the development of new tuberculosis drugs and treatment regimens. Nature Reviews. Drug Discovery 12: 388-404.

 

2014

 

36.  Ahmed, W., Menon, S., Godbole, A.A., Karthik, P.V. and Nagaraja, V. (2014). Conditional silencing of topoisomerase I gene of Mycobacterium tuberculosis validates its essentiality for cell survival. FEMS Microbiol Lett. 353, 116-23.

 

37.  Ahmed, W., Menon, S., Karthik, P.V. and Nagaraja, V. (2014). Reduction in DNA topoisomerase I level affects growth, phenotype and nucleoid architecture of Mycobacterium smegmatis. Microbiology (revised).

 

38.  Albesa-Jove, D., L. R., Chiarelli, V., Makarov, M. R., Pasca, S. Urresti, G. Mori, E. Salina, A. Vocat, N. Comino, E. Mohorko, S. Ryabova, B. Pfieiffer, A. L., Lopes Ribeiro, A. Rodrigo-Unzueta, M. Tersa, G. Zanoni, S. Buroni, K. H., Altmann, R. C. Hartkoorn, R. Glockshuber, S. T. Cole, G. Riccardi and M. E. Guerin, (2014). Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis. ACS chemical biology 9: 1567-1575.

 

39.  Andres E., Albesa-Jove D., Biarnes X., Moerschbacher B.M., Guerin M.E., and Planas A. (2014) Structural basis of chitin oligosaccharide deacetylation. Angew Chem Int Ed Engl. 53(27):6882-6887.

 

40.  Albesa-Jove D., Giganti D., Jackson M., Alzari P.M., and Guerin M.E. (2014) Structure-function relationships of membrane-associated GT-B glycosyltransferases. Glycobiology. 24(2):108-124.

 

41.  Boldrin, F., M. Ventura, G. Degiacomi, S. Ravishankar, C. Sala, Z. Svetlikova, A. Ambady, N. Dhar, J. Kordulakova, M. Zhang, A. Serafini, V. G. Vishwas, G. S. Kolly, N. Kumar, G. Palu, M. E. Guerin, K. Mikusova, S. T. Cole and R. Manganelli, (2014) The phosphatidyl-myo-inositol mannosyltransferase PimA is essential for Mycobacterium tuberculosis growth in vitro and in vivo. Journal of bacteriology 196: 3441-3451.

 

42.  Boritsch, E.C., Supply, P., Honore, N., Seemann, T., Stinear, T.P., and Brosch, R. (2014) A glimpse into the past and predictions for the future: The molecular evolution of the tuberculosis agent. Mol Microbiol. 93:835-52  

 

43.  Bottai D, Serafini A, Cascioferro A, Brosch R, and Manganelli R. (2014) Targeting Type VII/ESX Secretion Systems for Development of Novel Antimycobacterial Drugs. Curr Pharm Des. 20:4346-56.

 

44.  Bottai, D., Stinear, T.P., Supply, P., and Brosch, R. (2014) Mycobacterial Pathogenomics and Evolution. Microbiol Spectrum 2:MGM2-0025-2013.

 

45.  Cole, S. T., (2014) Who will develop new antibacterial agents? Philosophical transactions of the Royal Society of London. Series B, Biological sciences 369(1645): 20130430.

 

46.  Delogu G., Manganelli R., and Brennan M.J. (2014). Critical research concepts in tuberculosis vaccine development. Clin Microbiol Infect. 20 Suppl 5:59-65.

 

47.  Giganti D, Albesa-Jove D, Urresti S, Rodrigo-Unzueta A, Martinez MA, Comino N, Barilone N, Bellinzoni M, Chenal A, Guerin ME, Alzari PM. (2014) Secondary structure reshuffling modulates glycosyltransferase function at the membrane. Nat. Chem. Biol. Nov 17. doi: 10.1038/nchembio.1694.

 

48.  Godbole, A.A., Ahmed, W., Bhat, R.S., Bradley, E.K., Ekins, S. and Nagaraja, V. (2014) Inhibition of Mycobacterium tuberculosis topoisomerase I by m-AMSA, a eukaryotic type II topoisomerase poison. Biochem. Biophys. Res. Commun. 446, 916-920.

 

49.  Godbole A.A., Ahmed W., Bhat R.S., Bradley E.K., Ekins S. and Nagaraja V. (2014) Targeting Mycobacterium tuberculosis topoisomerase I by small molecule inhibitors. Antimicrob.Agents and Chemother (revised).

 

50.  Gonzalo-Asensio, J., Malaga, W., Pawlik, A., Astarie-Dequeker, C., Passemar, C., Moreau, F., Laval., F., Daffe, M., Martin, C., Brosch, R., and Guilhot C. (2014) Evolutionary history of tuberculosis shaped by conserved mutations in the PhoPR virulence regulator. Proc Natl Acad Sci U S A. 111:11491-6.

 

51.  Hartkoorn, R. C., F. Pojer, J. A. Read, H. Gingell, J. Neres, O. P. Horlacher, K. H. Altmann & S. T. Cole, (2014) Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA. Nature chemical biology 10: 96-98.

 

52.  Hartkoorn R.C., Ryabova O.B., Chiarelli L.R., Riccardi G., Makarov V., Cole S.T. (2014). Mechanism of action of 5-nitrothiophenes against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 58(5): 2944-2947.

 

53.  Hartkoorn, R. C., S. Uplekar & S. T. Cole, (2014) Cross-resistance between clofazimine and bedaquiline through upregulation of MmpL5 in Mycobacterium tuberculosis. Antimicrobial agents and chemotherapy 58: 2979-2981.

 

54.  Kolly, G. S., C. Sala, A. Vocat & S. T. Cole, (2014) Assessing essentiality of transketolase in Mycobacterium tuberculosis using an inducible protein degradation system. FEMS Microbiology Letters 358: 30-35.

 

55.  Lechartier, B., J. Rybniker, A. Zumla & S. T. Cole, (2014) Tuberculosis drug discovery in the post-post-genomic era. EMBO molecular medicine 6: 158-168.

 

56.  Le Chevalier, F., Cascioferro, A., Majlessi, L., Herrmann, J.L., and Brosch, R. (2014) Mycobacterium tuberculosis evolutionary pathogenesis and its putative impact on drug development. Future Microbiol. 9:969-85 .

 

57.  Li, K., L. A. Schurig-Briccio, X. Feng, A. Upadhyay, V. Pujari, B. Lechartier, F. L. Fontes, H. Yang, G. Rao, W. Zhu, A. Gulati, J. H. No, G. Cintra, S. Bogue, Y. L. Liu, K. Molohon, P. Orlean, D. A. Mitchell, L. Freitas-Junior, F. Ren, H. Sun, T. Jiang, Y. Li, R. T. Guo, S. T. Cole, R. B. Gennis, D. C. Crick & E. Oldfield, (2014) Multitarget drug discovery for tuberculosis and other infectious diseases. Journal of medicinal chemistry 57: 3126-3139.

 

58.  Makarov V., Lechartier B., Zhang M., Neres J., van der Sar A.M., Raadsen S.A., Hartkoorn R.C., Ryabova O.B., Vocat A., Decosterd L.A., Widmer N., Buclin T., Bitter W., Andries K., Pojer F., Dyson P.J., Cole S.T. Towards a new combination therapy for tuberculosis with next generation benzothiazinones. EMBO Mol Med. (2014), 6(3):372-383.

 

59.  Marion E, Song OR, Christophe T, Babonneau J, Fenistein D, Eyer J, Letournel F, Henrion D, Clere N, Paille V, Guerineau NC, Saint Andre JP, Gersbach P, Altmann KH, Stinear T, Comoglio Y, Guillaume Sandoz G, Preisser L, Delneste Y, Yeramian E, Marsollier L, Brodin P. (2014) Mycobacterial Toxin Induces Analgesia in Buruli Ulcer by Targeting the Angiotensin Pathways. Cell 157(7):1565-1576.

 

60.  Mikušova K., Makarov V., Neres J. DprE1 - from the Discovery to the Promising Tuberculosis Drug Target, Curr. Pharm. Des., (2014), 20, 4249-4273.

 

61.  Naik M,Humnabadkar V, Tantry S.J., Panda M., Narayan A., Guptha S., Panduga V., Manjrekar P., Jena .LK., Koushik K., Shanbagh G., Ramaiah M., Gorai G., Rudrapatna S., Ambady A., Hegde N., Mahadevaswamy J., Kaur P., Sambandamurthy V.K., Awasthy D., Narayan C., Madhavapeddi P., Reddy J., Prabhakar K.R., Kumar C.N.N., Chatterji M., Whiteaker J., McLaughlin B., Chiarelli L.R., Riccardi G., Pasca M.R., Binda C., Ramachandran V., Shandil R., Tommasi R., Iyer P.S., Narayanan S., Hosagrahara V., Kavanagh S., Dinesh N., and Ghorpade S.R. (2014). 4-Aminoquinolone Piperidine Amides: Non-Covalent Inhibitors of DprE1 with Long Residence Time and Potent Antimycobacterial Activity. J Med Chem. 57:5419-5434.

 

62.  Neres J., Hartkoorn R.C., Chiarelli L.R., Gadupudi R., Pasca M.R., Mori G., Farina D., Savina S., Makarov V., Kolly G.S., Molteni E., Binda C., Dhar N., Ferrari S., Brodin P., Delorme V., Landry V., Ribeiro A.L., Venturelli A., Saxena P., Pojer F., Carta A., Luciani R., Porta A., Zanoni G., De Rossi E., Costi M.P., Riccardi G., and Cole S.T. (2014).  2-Carboxyquinoxalines kill Mycobacterium tuberculosis through non-covalent inhibition of DprE1. ACS Chem Biol. Nov 26. [Epub ahead of print] PubMed PMID: 25427196.

 

63.  Paeschke R., Woskobojnik I., Makarov V., Schmidtke M., and Bogner E. (2014). DSTP-27 prevents entry of human cytomegalovirus. Antimicrob Agents Chemother.  58(4):1963-1971.

 

64.  Riccardi G, and Pasca MR. (2014). Trends in discovery of new drugs for tuberculosis therapy. J Antibiot.. 67:655-9.

 

65.  Queval CJ, Song OR, Delorme V, Iantomasi R, Veyron-Churlet R, Deboosere N, Landry V, Baulard A, and Brodin P. A (2014). A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening. J Vis Exp. 17:e51114

 

66.  Salina E, Ryabova O, Kaprelyants A, and Makarov V., (2014). New 2-Thiopyridines as Potential Candidates for Killing both Actively Growing and Dormant Mycobacterium tuberculosis Cells. Antimicrob Agents Chemother. 58(1):55-60.

 

67.  Scoffone V.C., Spadaro F., Udine C., Makarov V., Fondi M., Fani R., De Rossi E., Riccardi G., and Buroni S. (2014). The Antitubercular 2-thiopyridine Derivative is Active Also against Burkholderia cenocepacia: Characterization of a Mechanism of Resistance, Antimicrob Agents Chemother. 58(4):2415-2417.

 

68.  Solans, L., Aguilo, N., Samper, S., Pawlik, A., Frigui, W., Martin, C., Brosch, R., and Gonzalo-Asensio J. (2014) A specific polymorphism in Mycobacterium tuberculosis H37Rv causes differential ESAT-6 expression and identifies WhiB6 as a novel ESX-1 component. Infect Immun. 82:3446-56.

 

69.  Singh V., Brecik M., Mukherjee R., Evans J.C., Svetlikova Z., Blaško J., Surade S., Blackburn J., Warner D.F., Mikušova K., and Mizrahi V. (2014). The Complex Mechanism of Antimycobacterial Action of 5-Fluorouracil. Chemistry & Biology S1074-5521(14)00414-1.

 

70.  Surade, S., N. Ty, N. Hengrung, B. Lechartier, S. T. Cole, C. Abell and T. L. Blundell, (2014). A structure-guided fragment-based approach for the discovery of allosteric inhibitors targeting the lipophilic binding site of transcription factor EthR from Mycobacterium tuberculosis. The Biochemical journal 458: 387-394.

 

71.  Svetlikova Z, Barath P, Jackson M, Kordulakova J, Mikusova K. (2014). Purification and characterization of the acyltransferase involved in biosynthesis of the major mycobacterial cell envelope glycolipid--monoacylated phosphatidylinositol dimannoside.  Protein Expr Purif. 100: 33-9.

 

72.  Zhang, M., C. Sala, N. Dhar, A. Vocat, V. K. Sambandamurthy, S. Sharma, G. Marriner, V. Balasubramanian and Cole, S.T.  (2014) In vitro and in vivo activities of three oxazolidinones against nonreplicating Mycobacterium tuberculosis. Antimicrobial agents and chemotherapy 58: 3217-3223.

 

73.  Zumla A.I., Gillespie S.H., Hoelscher M., Philips P.P, Cole S.T., Abubakar I., McHugh T.D., Schito M., Maeurer M., and Nunn A.J. (2014). New antituberculosis drugs, regimens, and adjunct therapies: needs, advances, and future prospects. Lancet Infect Dis. 14(4):327-340.

 

2015

 

74.  Albesa-Jove D., Comino N., Tersa M., Mohorko E,. Urresti S., Dainese E., Chiarelli L.R., Pasca M.R., Manganelli R., Makarov V., Riccardi G., Svergun D.I., Glockshuber R,, and Guerin M.E., (2015). The redox state regulates the conformation of Rv2466c to activate the antitubercular prodrug TP053. J Biol Chem. 22:917-927.

 

75.  Ahmed, W., Menon, S., Karthik, P.V. and Nagaraja, V. (2015). Reduction in DNA topoisomerase I level affects growth, phenotype and nucleoid architecture of Mycobacterium smegmatis.  Microbiology 161:341-353.

 

76.  Bailo R., Bhatt A. and Ainsa J.A. (2015). Lipid transport in Mycobacterium tuberculosis and its implications in virulence and drug development. Biochem Pharmacol. 1;96(3):159-67.

 

77.  Brecik, M., Centarova, I., Mukherjee, R., Kolly, G.S., Huszar, S., Bobovska, A., Kilacskova, E., Mokošova, V., Svetlikova, S., Šarkan, M., Neres, J., Kordulakova, J., Cole, S.T., and Mikušova K. (2015). DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization. ACS Chem. Biol., 10 (7), 1631–1636.

 

78.  Brodin P, DelNery E, Soleilhac E. (2015). High content screening in chemical biology: overview and main challenges. Med Sci (Paris). 31(2): 187-196.

 

79.  Delogu G., Provvedi R., Sali M., and Manganelli R. (2015) Mycobacterium tuberculosis virulence: insights and impact on vaccine development. Future Microbiol. 10(7):1177-1194

 

80.  Delorme V, Song OR, Baulard A, Brodin P. (2015). Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. Methods Mol Biol. 1285:387-411.

 

81.  Giganti D., Albesa-Jove D., Urresti S., Rodrigo-Unzueta A., Martinez A., Comino N., Barilone N., Bellinzoni M., Chenal A., Guerin E., and Alzari P.M. (2015). Secondary structure reshuffling modulates glycosyltransferase function at the membrane. Nat Chem Biol. 11(1):16-8.

 

82.  Glaus F., and Altmann K.H. (2015). Total synthesis of the tiacumicin B (lipiarmycin A3/fidaxomicin) aglycone. Angew Chem Int Ed Engl. 2;54(6):1937-40.

 

83.  Godbole A.A., Ahmed W., Bhat R.S., Bradley E.K., Ekins S. and Nagaraja V. (2015). Targeting Mycobacterium tuberculosis topoisomerase I by small molecule inhibitors. Antimicrob Agents and Chemother. 59, 1549-1557.

 

84.  Kolly G.S., Mukherjee R., Kilacskova E., Abriata L.A., Raccaud M., Blaško J., Sala C., Dal Peraro M., Mikušova K., and Cole S.T. (2015). GtrA Protein Rv3789 Is Required for Arabinosylation of Arabinogalactan in Mycobacterium tuberculosis. J Bacteriol. 197(23) 3686-97.

 

85.  Lechartier, B., and Cole S.T. (2015). Mode of Action of Clofazimine and Combination Therapy with Benzothiazinones against Mycobacterium tuberculosis. Antimicrob Agents and Chemother. 59, 4457-4463.

 

86.  Lisa M.N., Gil M., Andre-Leroux G., Barilone N., Duran R., Biondi R.M., and Alzari P.M. (2015). Molecular Basis of the Activity and the Regulation of the Eukaryotic-like S/T Protein Kinase PknG from Mycobacterium tuberculosis. Structure. 2;23(6):1039-1048.

 

87.  Makarov, V., Neres J., Hartkoorn R.C., Ryabova O.B., Kazakova E., Šarkan M., Huszar S., Piton J., Kolly G.S., Vocat A., Conroy T.M., Mikušova K., Cole S.T. (2015). The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis. Antimicrob Agents Chemother. 59(8): 4446-4452.

 

88.  Makarov V.A., Braun H., Richter M., Riabova O.B., Kirchmair J., Kazakova E.S., Seidel N., Wutzler P., and Schmidtke M. (2015). Pyrazolopyrimidines: Potent Inhibitors Targeting the Capsid of Rhino- and Enteroviruses, Chem Med Chem, 10, 1629-34.

 

89.  Mori G., Chiarelli L.R., Esposito M., Makarov V., Bellinzoni M., Hartkoorn R.C., Degiacomi G., Boldrin F., Ekins S., de Jesus Lopes Ribeiro A.L., Marino L.B., Centarova I., Svetlikova Z., Blaško J., Kazakova E., Lepioshkin A., Barilone N., Zanoni G., Porta A., Fondi M., Fani R., Baulard A.R., Mikušova K., Alzari P.M., Manganelli R., de Carvalho L.P.S., Riccardi G., Cole S.T., and Pasca M.R. (2015). Thiophenecarboxamide derivatives activated by EthA kill Mycobacterium tuberculosis by inhibiting the CTP synthetase PyrG. Chem Biol. 22:917-27.

 

90.   Monakhova N., Ryabova S., Makarov V. (2015). Synthesis and biological properties of pyrrolo[1,2-a]indoles, Journal of Heterocyclic Chemistry. DOI: 10.1002/jhet.2312.

 

91.  Neres J., Hartkoorn R.C., Chiarelli R., Gadupudi R., Pasca M.R., Mori G., Venturelli A., Savina S., Makarov V., Kolly G.S., Molteni E., Binda C., Dhar N., Ferrari S., Brodin P., Delorme V., Landry V., de Jesus Lopes Ribeiro A.L., Farina D., Saxena P., Pojer F., Carta A., Luciani R., Porta A., Zanoni G., De Rossi E., Costi M.P., Riccardi G., and Cole S.T. (2015). 2-Carboxyquinoxalines kill Mycobacterium tuberculosis through noncovalent inhibition of DprE1. ACS Chem Biol. 20;10(3):705-14.

 

92.  Rodrigues L., Viveiros M., and Ainsa J.A. (2015). Measuring efflux and permeability in mycobacteria. Methods Mol Biol. 1285, 227-239.

 

93.  Silva-Miranda M., Ekaza E., Breiman A., Asehnoune K., Barros-Aguirre D., Pethe K., Ewann F., Brodin P., Ballell-Pages L., and Altare F. (2015). High-content screening technology combined with a human granuloma model as a new approach to evaluate the activities of drugs against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 59(1):693-697.

 

94.  Scoffone V.C., Ryabova O., Makarov V., Iadarola P., Fumagalli M., Fondi M., Fani R., De Rossi E., Riccardi G., and Buroni S., (2015). Efflux-mediated resistance to a benzothiadiazol derivative effective against Burkholderia cenocepacia. Frontiers in Microbiology, 6, 815.

 

95.  Simeone R., Sayes F., Song O., Groschel M.I., Brodin P., Brosch R., and Majlessi L. (2015). Cytosolic Access of Mycobacterium tuberculosis: Critical Impact of Phagosomal Acidification Control and Demonstration of Occurrence In Vivo. PLoS Pathog. 2;11(2):e1004650.

 

96.  Sipos, A., Pato J., Szekely, R., Hartkoorn, R., Kekesi L., Őrfi, L., Szantai-Kis, C., Mikusova, K., Svetlikova, Z., Kordulakova, J., Godbole, A.A., Bhat, R.S., Nagaraja, V., Bush, N.G., Collin, F., Maxwell, A., Cole, S. and Keri G. (2015). Lead selection and characterization of antitubercular compounds using the nested chemical library. Tuberculosis (Edib), 95,S200-206.

 

97.  Slama N, Jamet S, Frigui W, Pawlik A, Bottai D, Laval F, Constant P, Lemassu A, Cam K, Daffe M, Brosch R, Eynard N, and Quemard A. (2015). The changes in mycolic acid structures caused by hadC mutation have a dramatic effect on the virulence of Mycobacterium tuberculosis. Mol Microbiol. Nov 5. doi: 10.1111/mmi.13266.

 

98.  Singh V., Brecik M., Mukherjee R., Evans J.C., Svetlikova Z., Blaško J., Surade S., Blackburn J., Warner D.F., Mikušova K., and Mizrahi V. (2015). The complex mechanism of antimycobacterial action of 5-fluorouracil. Chem Biol. 22(1):63-75.

 

99.  Tantry S.J., Degiacomi G., Sharma S., Jena L.K., Narayan A., Guptha S., Shanbhag G., Menasinakai S., Mallya M., Awasthy D., Balakrishnan G., Kaur P., Bhattacharjee D., Narayan C., Reddy J., Naveen Kumar C.N., Shandil R., Boldrin F., Ventura M., Manganelli R., Hartkoorn R.C., Cole S.T., Panda M., Markad S.D., Ramachandran V., Ghorpade S.R., and Dinesh N. (2015). Whole cell screen based identification of spiropiperidines with potent antitubercular properties. Bioorg Med Chem Lett. 15;25(16):3234-3245.

 

100.        Vera-Cabrera L., Gonzalez-Martinez N.A., Lozano-Garza H.G., Castro-Garza J., Vargas-Vilarrea J., Cavazos-Rocha N., Ocampo-Candiani J., Makarov V., and Cole S. (2015). In Vivo Activity of the Benzothiazinones PBTZ169 and BTZ043 against Nocardia brasiliensis. PLOS Neglected Tropical Diseases, 9(10), e0004022.

 

101.        Vocat A., Hartkoorn R.C., Lechartier B., Zhang M., Dhar N., Cole S.T., and Sala C. (2015). Bioluminescence for assessing drug potency against non-replicating Mycobacterium tuberculosis. Antimicrob Agents Chemother. 59(7):4012-4009.

 

2016

 

102.        Albesa-Jove D., Comino N., Tersa M., Mohorko E., Urresti S., Dainese E., Chiarelli L.R., Pasca M.R., Manganelli R., Makarov V., Riccardi G., Svergun D.I., Glockshuber R., and Guerin M.E.. (2016). The Redox State Regulates the Conformation of Rv2466c to Activate the Antitubercular Prodrug TP053. J Biol Chem. 290(52):31077-31089.

 

103.        Albesa-Jove, D., and Guerin M.E. (2016). The conformational plasticity of glycosyltransferases. Curr Opin Struct Biol. 40:23-32.

 

104.        Albesa-Jove D., Svetlikova Z., Tersa M., Sancho-Vaello E., Carreras-Gonzalez A., Bonnet P., Arrasate P., Eguskiza A., Cifuente O., Kordulakova J., Jackson M., Mikušova K., and Guerin E. (2016). Structural basis for selective recognition of acyl chains by the membrane-associated acyltransferase PatA. Nat Commun. 7:10906.

 

105.        Barthe P., Veyron-Churlet R., de Visch A., Gilleron M., Saliou M., Tomavo S., Nigou J., Brodin P., and Cohen-Gonsaud M. (2016). Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization. Structure. 2016 Aug 23. pii: S0969-2126(16)30220-30229.

 

106.        Benjak A., Uplekar S., Zhang M., Piton J., Cole S.T., and Sala C. (2016). Genomic and transcriptomic analysis of the streptomycin-dependent Mycobacterium tuberculosis strain 18b. BMC Genomics. 17:190.

 

107.        Boritsch, E.C., W. Frigui, A., Cascioferro, W., Malaga, G., Etienne, G. Laval, A., Pawlik, F., Le Chevalier, M., Orgeur, L., Ma, C., Bouchier, T.P., Stinear, P., Supply, L., Majlessi, M., Daffe, C., Guilhot and Brosch, R., (2016) pks5 recombination-mediated surface remodelling in Mycobacterium tuberculosis emergence. Nat. Microbiology. DOI :10.1038/NMICROBIOL.2015.19.

 

108.        Cifuente J.O., Comino N., Madariaga-Marcos J., Lopez-Fernandez S., Garcia-Alija M., Agirre J., Albesa-Jove D., and Guerin M.E. (2016). Structural Basis of Glycogen Biosynthesis Regulation in Bacteria. Structure. 24(9):1613-1622.

 

109.        Deboosere N., Iantomasi R., Queval J., Song O.R., Deloison G., Jouny S., Debrie A.S., Chamaillard M., Nigou J., Cohen-Gonsaud M., Locht C., Brodin P., and Veyron-Churlet R. (2016). LppM impact on the colonization of macrophages by Mycobacterium tuberculosis. Cell Microbiol. May 24. doi: 10.1111/cmi.12619.

 

110.        Degiacomi G., Personne Y., Mondesert G., Ge X., Mandava S., Hartkoorn C., Boldrin F., Goel P., Peisker K., Benjak A., Barrio M.B., Ventura M., Brown A.C., Leblanc V., Bauer A., Sanyal S., Cole S.T., Lagrange S., Parish T., and Manganelli R.. (2016). Micrococcin P1 - A bactericidal thiopeptide active against Mycobacterium tuberculosis. Tuberculosis (Edinb). 100:95-101.

 

111.        Djaout K., Singh V., Boum Y., Katawera V., Becker HF, Bush NG, Hearnshaw SJ, Pritchard JE, Bourbon P, Madrid PB, Maxwell A, Mizrahi V, Myllykallio H, Ekins S, (2016). Predictive modeling identifies selective inhibitors of thymidylate synthase ThyX in Mycobacterium tuberculosis. Sci Rep., 6, 27792.

 

112.        Dumas E., Christina Boritsch E., Vandenbogaert M., Rodriguez de la Vega R.C., Thiberge J.M., Caro V., Gaillard J.L., Heym B., Girard-Misguich F., Brosch R., Sapriel G.. (2016). Mycobacterial Pan-Genome Analysis Suggests Important Role of Plasmids in the Radiation of Type VII Secretion Systems. Genome Biol Evol. 8(2):387-402.

 

113.        Ekins S., Godbole A.A., Keri G., Orfi L., Pato J., Bhat R.S., Verma R., Bradley E.K., Nagaraja V., (2016) Machine Learning and Docking Models for Mycobacterium tuberculosis Topoisomerase I. J. Chem. Info. Mod. 56(7):1332-1343.

 

114.        Foo S., Lechartier B., Kolly S., Boy-Rottger S., Neres J., Rybniker J., Lupien A., Sala C., Piton J., and Cole S.T. (2016). Characterization of DprE1-mediated benzothiazinone resistance in Mycobacterium tuberculosis. Antimicrob Agents Chemother. Aug 15. pii: AAC.01523-16.

 

115.        Karabanovich G., Zemanova J., Smutný T., Szekely R., Šarkan M., Centarova I., Vocat A3, Pavkova I., Čonka P., Němeček J., Stolařikova J., Vejsova M., Vavrova K., Klimešova V., Hrabalek A., Pavek P., Cole S.T. Mikušova K., and Roh J. (2016). Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis. J Med Chem. 59(6):2362-2380.

 

116.        Luciani R., Saxena P., Surade S., Santucci M., Venturelli A., Borsari C., Marverti G., Ponterini G., Ferrari S., Blundell T.L., and Costi M.P. (2016). Virtual screening and X-ray crystallography Identify non-substrate analog inhibitors of Flavin-dependent Thymidylate Synthase. J Med Chem. Sep 2. [Epub ahead of print].

 

117.        Monakhova, N., Ryabova, S., and Makarov, V. (2016). Synthesis and Some Biological properties of Pyrrolo[1,2-a]indoles. J. Hetro. Chem. 53(3):685-709.

 

118.        Mori, G., Chiarelli, L.R., Riccardi, G., and Pasca, M.R. (2016). New prodrugs against tuberculosis. Drug Discovery Today. http://dx.doi.org/10.1016/j.drudis.2016.09.006.

 

119.        Nikiforov 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(7):2318-2326.

 

120.        Nikiforov, P.O., Blaszczyk, M., Surade, S., Boshoff, H. I., Sajid, A., Delorme, V., Brodin, P., et al. (2016). Research data supporting "Fragment-sized EthR inhibitors exhibit exceptionally strong ethionamide boosting effect in whole cell Mycobacterium tuberculosis assays" [dataset]. https://www.repository.cam.ac.uk/handle/1810/254768.

 

 

121.        Pieton, J., Foo, C.S.Y., and Cole, S.T. Structural studies of Mycobacterium tuberculosis DprE1 interacting with its inhibitors. Drug Discovery Today. http://dx.doi.org/10.1016/j.drudis.2016.09.014.

 

122.        Queval C.J., Song O.R., Deboosere N., Delorme V., Debrie A.S., Iantomasi R., Veyron-Churlet R., Jouny S., Redhage K., Deloison G., Baulard A., Chamaillard M., Locht C., and Brodin P. (2016). STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection. Sci Rep. 6:29297.

 

123.        Riccardi, G., Old, I.G., and Ekins, S. (2016). Raising awareness of the importance of funding for tuberculosis small-molecule research. Drug. Discovery Today. http://dx.doi.org/10.1016/j.drudis.2016.09.012.

 

124.        Rodrigo-Unzueta A., Martinez MA., Comino N., Alzari P.M., Chenal A., and Guerin M.E. (2016). Molecular Basis of Membrane Association by the Phosphatidylinositol Mannosyltransferase PimA Enzyme from Mycobacteria. J Biol Chem. 291(27):13955-13963.

 

125.        Rožman, K., Sosič, I., Fernandez, R., Young, R., Mendoza, A., Gobec, S., and Encinas, L. (2016). A new 'golden age' for the antitubercular target InhA. Drug Discovery Today. http://dx.doi.org/10.1016/j.drudis.2016.09.009

 

126.        Rybniker J, Chen JM, Sala C, Hartkoorn RC, Vocat A, Benjak A, Boy-Rottger S, Zhang M, Szekely R, Greff Z, Őrfi L, Szabadkai I, Pato J, Keri G, and Cole ST. (2016). Anticytolytic Screen Identifies Inhibitors of Mycobacterial Virulence Protein Secretion. Cell Host & Microbe DOI: http://dx.doi.org/10.1016/j.chom.2014.09.008

 

127.        Singh, V., Donini, S., Pacitto, A., Sala, C., Hartkoorn, R.C., Dhar, N., Keri, G., Ascher, D.B., Mondesert, G., Vocat, A., Lupien, A., Sommer, R., Vermet, H., Lagrange, S., Buechler, J., Warner, D.F., McKinney, J.D., Pato, J., Cole, S.T.,  Blundell, T.L., Rizzi, M., and Mizrahi, V.  (2016). The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis. ACS Inf. Dis. DOI: 10.1021/acsinfecdis.6b00102.

 

128.        Singh, V. & Mizrahi, V. (2016). Identification and validation of novel drug targets in Mycobacterium tuberculosis. Drug. Discovery Today. http://dx.doi.org/10.1016/j.drudis.2016.09.010.

 

129.        Slama N., Jamet S., Frigui W., Pawlik A., Bottai D., Laval F., Constant P., Lemassu A., Cam K., Daffe M., Brosch R., Eynard N., and Quemard A. (2016). The changes in mycolic acid structures caused by hadC mutation have a dramatic effect on the virulence of Mycobacterium tuberculosis. Mol Microbiol. 99(4):794-807.

 

130.        Sipos, A., J. Pato, R. Szekely, R. Hartkoorn, L. Kekesi, L. Őrfi, Cs. Szantai-Kis, K. Mikušova, Z. Svetlikova, J. Kordulakova, V. Nagaraja, A. Godbole, N.G. Bush, F. Collin, A. Maxwell, S. Cole and Keri. G. (2016). Lead selection and characterization of antitubercular compounds using the Nested Chemical Library. in Special Issue of the Journal Tuberculosis (Elsevier). Guest-editors: Palfi G., Dutour O., Perrin P., Sola C. Zink A.  95:S200-206.

 

131.        Tiwari R., Miller P.A., Chiarelli L.R., Mori G., Šarkan M., Centarova I, Cho S., Mikušova K., Franzblau S.G., Oliver A.G., and Miller M.J. (2016). Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043. ACS Med Chem Lett. 7(3):266-70.