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Items: 16

1.

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK.

Chiarelli LR, Mori G, Orena BS, Esposito M, Lane T, de Jesus Lopes Ribeiro AL, Degiacomi G, Zemanová J, Szádocka S, Huszár S, Palčeková Z, Manfredi M, Gosetti F, Lelièvre J, Ballell L, Kazakova E, Makarov V, Marengo E, Mikusova K, Cole ST, Riccardi G, Ekins S, Pasca MR.

Sci Rep. 2018 Feb 16;8(1):3187. doi: 10.1038/s41598-018-21614-4.

2.

Promoter mutagenesis for fine-tuning expression of essential genes in Mycobacterium tuberculosis.

Boldrin F, Degiacomi G, Serafini A, Kolly GS, Ventura M, Sala C, Provvedi R, Palù G, Cole ST, Manganelli R.

Microb Biotechnol. 2018 Jan;11(1):238-247. doi: 10.1111/1751-7915.12875. Epub 2017 Oct 27.

3.

The antibacterial prodrug activator Rv2466c is a mycothiol-dependent reductase in the oxidative stress response of Mycobacterium tuberculosis.

Rosado LA, Wahni K, Degiacomi G, Pedre B, Young D, de la Rubia AG, Boldrin F, Martens E, Marcos-Pascual L, Sancho-Vaello E, Albesa-Jové D, Provvedi R, Martin C, Makarov V, Versées W, Verniest G, Guerin ME, Mateos LM, Manganelli R, Messens J.

J Biol Chem. 2017 Aug 11;292(32):13097-13110. doi: 10.1074/jbc.M117.797837. Epub 2017 Jun 15.

4.

PknG senses amino acid availability to control metabolism and virulence of Mycobacterium tuberculosis.

Rieck B, Degiacomi G, Zimmermann M, Cascioferro A, Boldrin F, Lazar-Adler NR, Bottrill AR, le Chevalier F, Frigui W, Bellinzoni M, Lisa MN, Alzari PM, Nguyen L, Brosch R, Sauer U, Manganelli R, O'Hare HM.

PLoS Pathog. 2017 May 17;13(5):e1006399. doi: 10.1371/journal.ppat.1006399. eCollection 2017 May.

5.

A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors.

Esposito M, Szadocka S, Degiacomi G, Orena BS, Mori G, Piano V, Boldrin F, Zemanová J, Huszár S, Barros D, Ekins S, Lelièvre J, Manganelli R, Mattevi A, Pasca MR, Riccardi G, Ballell L, Mikušová K, Chiarelli LR.

ACS Infect Dis. 2017 Jun 9;3(6):428-437. doi: 10.1021/acsinfecdis.7b00006. Epub 2017 May 11.

PMID:
28475832
6.

Essentiality of mmpL3 and impact of its silencing on Mycobacterium tuberculosis gene expression.

Degiacomi G, Benjak A, Madacki J, Boldrin F, Provvedi R, Palù G, Kordulakova J, Cole ST, Manganelli R.

Sci Rep. 2017 Feb 27;7:43495. doi: 10.1038/srep43495.

7.

Micrococcin P1 - A bactericidal thiopeptide active against Mycobacterium tuberculosis.

Degiacomi G, Personne Y, Mondésert G, Ge X, Mandava CS, Hartkoorn RC, Boldrin F, Goel P, Peisker K, Benjak A, Barrio MB, Ventura M, Brown AC, Leblanc V, Bauer A, Sanyal S, Cole ST, Lagrange S, Parish T, Manganelli R.

Tuberculosis (Edinb). 2016 Sep;100:95-101. doi: 10.1016/j.tube.2016.07.011. Epub 2016 Jul 27.

PMID:
27553416
8.

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG.

Mori G, Chiarelli LR, Esposito M, Makarov V, Bellinzoni M, Hartkoorn RC, Degiacomi G, Boldrin F, Ekins S, de Jesus Lopes Ribeiro AL, Marino LB, Centárová I, Svetlíková Z, Blaško J, Kazakova E, Lepioshkin A, Barilone N, Zanoni G, Porta A, Fondi M, Fani R, Baulard AR, Mikušová K, Alzari PM, Manganelli R, de Carvalho LP, Riccardi G, Cole ST, Pasca MR.

Chem Biol. 2015 Jul 23;22(7):917-27. doi: 10.1016/j.chembiol.2015.05.016. Epub 2015 Jun 18.

9.

Whole cell screen based identification of spiropiperidines with potent antitubercular properties.

Tantry SJ, Degiacomi G, Sharma S, Jena LK, Narayan A, Guptha S, Shanbhag G, Menasinakai S, Mallya M, Awasthy D, Balakrishnan G, Kaur P, Bhattacharjee D, Narayan C, Reddy J, Naveen Kumar CN, Shandil R, Boldrin F, Ventura M, Manganelli R, Hartkoorn RC, Cole ST, Panda M, Markad SD, Ramachandran V, Ghorpade SR, Dinesh N.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3234-45. doi: 10.1016/j.bmcl.2015.05.087. Epub 2015 Jun 3.

PMID:
26087937
10.

The phosphatidyl-myo-inositol mannosyltransferase PimA is essential for Mycobacterium tuberculosis growth in vitro and in vivo.

Boldrin F, Ventura M, Degiacomi G, Ravishankar S, Sala C, Svetlikova Z, Ambady A, Dhar N, Kordulakova J, Zhang M, Serafini A, Vishwas KG, Kolly GS, Kumar N, Palù G, Guerin ME, Mikusova K, Cole ST, Manganelli R.

J Bacteriol. 2014 Oct;196(19):3441-51. doi: 10.1128/JB.01346-13. Epub 2014 Jul 21. Erratum in: J Bacteriol. 2014 Dec;196(23):4197. Vishwas, V G [Corrected to Vishwas, K G].

11.

GarA is an essential regulator of metabolism in Mycobacterium tuberculosis.

Ventura M, Rieck B, Boldrin F, Degiacomi G, Bellinzoni M, Barilone N, Alzaidi F, Alzari PM, Manganelli R, O'Hare HM.

Mol Microbiol. 2013 Oct;90(2):356-66. doi: 10.1111/mmi.12368. Epub 2013 Sep 8.

12.

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.

13.

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
14.

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.

15.

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.

16.

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.

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