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Items: 1 to 50 of 55

1.

The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase.

Mori G, Orena BS, Franch C, Mitchenall LA, Godbole AA, Rodrigues L, Aguilar-Pérez C, Zemanová J, Huszár S, Forbak M, Lane TR, Sabbah M, Deboosere N, Frita R, Vandeputte A, Hoffmann E, Russo R, Connell N, Veilleux C, Jha RK, Kumar P, Freundlich JS, Brodin P, Aínsa JA, Nagaraja V, Maxwell A, Mikušová K, Pasca MR, Ekins S.

Tuberculosis (Edinb). 2018 Sep;112:98-109. doi: 10.1016/j.tube.2018.08.004. Epub 2018 Aug 11.

PMID:
30205975
2.

Shifts of Faecal Microbiota During Sporadic Colorectal Carcinogenesis.

Mori G, Rampelli S, Orena BS, Rengucci C, De Maio G, Barbieri G, Passardi A, Casadei Gardini A, Frassineti GL, Gaiarsa S, Albertini AM, Ranzani GN, Calistri D, Pasca MR.

Sci Rep. 2018 Jul 9;8(1):10329. doi: 10.1038/s41598-018-28671-9.

3.

Pyrazole and imidazo[1,2-b]pyrazole Derivatives as New Potential Antituberculosis Agents.

Meta E, Brullo C, Tonelli M, Franzblau SG, Wang Y, Ma R, Baojie W, Orena BS, Pasca MR, Bruno O.

Med Chem. 2019;15(1):17-27. doi: 10.2174/1573406414666180524084023.

PMID:
29792151
4.

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.

5.

Mechanochemical Synthesis and Biological Evaluation of Novel Isoniazid Derivatives with Potent Antitubercular Activity.

Oliveira PFM, Guidetti B, Chamayou A, André-Barrès C, Madacki J, Korduláková J, Mori G, Orena BS, Chiarelli LR, Pasca MR, Lherbet C, Carayon C, Massou S, Baron M, Baltas M.

Molecules. 2017 Sep 1;22(9). pii: E1457. doi: 10.3390/molecules22091457.

6.

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
7.

New and Old Hot Drug Targets in Tuberculosis.

Chiarelli LR, Mori G, Esposito M, Orena BS, Pasca MR.

Curr Med Chem. 2016;23(33):3813-3846. Review.

PMID:
27666933
8.

New prodrugs against tuberculosis.

Mori G, Chiarelli LR, Riccardi G, Pasca MR.

Drug Discov Today. 2017 Mar;22(3):519-525. doi: 10.1016/j.drudis.2016.09.006. Epub 2016 Sep 17. Review.

PMID:
27649942
9.

Pyrrolidinone and pyrrolidine derivatives: Evaluation as inhibitors of InhA and Mycobacterium tuberculosis.

Matviiuk T, Madacki J, Mori G, Orena BS, Menendez C, Kysil A, André-Barrès C, Rodriguez F, Korduláková J, Mallet-Ladeira S, Voitenko Z, Pasca MR, Lherbet C, Baltas M.

Eur J Med Chem. 2016 Nov 10;123:462-475. doi: 10.1016/j.ejmech.2016.07.028. Epub 2016 Jul 16.

PMID:
27490025
10.

Evaluation of the inhibitory activity of (aza)isoindolinone-type compounds: toward in vitro InhA action, Mycobacterium tuberculosis growth and mycolic acid biosynthesis.

Chollet A, Stigliani JL, Pasca MR, Mori G, Lherbet C, Constant P, Quémard A, Bernadou J, Pratviel G, Bernardes-Génisson V.

Chem Biol Drug Des. 2016 Nov;88(5):740-755. doi: 10.1111/cbdd.12804. Epub 2016 Jul 16.

PMID:
27301022
11.

Iron Acquisition Pathways as Targets for Antitubercular Drugs.

Meneghetti F, Villa S, Gelain A, Barlocco D, Chiarelli LR, Pasca MR, Costantino L.

Curr Med Chem. 2016;23(35):4009-4026. Review.

PMID:
27281295
12.

Triazolophthalazines: Easily Accessible Compounds with Potent Antitubercular Activity.

Veau D, Krykun S, Mori G, Orena BS, Pasca MR, Frongia C, Lobjois V, Chassaing S, Lherbet C, Baltas M.

ChemMedChem. 2016 May 19;11(10):1078-89. doi: 10.1002/cmdc.201600085. Epub 2016 Apr 21.

PMID:
27097919
13.

The Redox State Regulates the Conformation of Rv2466c to Activate the Antitubercular Prodrug TP053.

Albesa-Jové D, Comino N, Tersa M, Mohorko E, Urresti S, Dainese E, Chiarelli LR, Pasca MR, Manganelli R, Makarov V, Riccardi G, Svergun DI, Glockshuber R, Guerin ME.

J Biol Chem. 2015 Dec 25;290(52):31077-89. doi: 10.1074/jbc.M115.677039. Epub 2015 Nov 6.

14.

Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth.

Chollet A, Mori G, Menendez C, Rodriguez F, Fabing I, Pasca MR, Madacki J, Korduláková J, Constant P, Quémard A, Bernardes-Génisson V, Lherbet C, Baltas M.

Eur J Med Chem. 2015 Aug 28;101:218-35. doi: 10.1016/j.ejmech.2015.06.035. Epub 2015 Jun 20.

PMID:
26142487
15.

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.

16.

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
17.

Differential roles of RND efflux pumps in antimicrobial drug resistance of sessile and planktonic Burkholderia cenocepacia cells.

Buroni S, Matthijs N, Spadaro F, Van Acker H, Scoffone VC, Pasca MR, Riccardi G, Coenye T.

Antimicrob Agents Chemother. 2014 Dec;58(12):7424-9. doi: 10.1128/AAC.03800-14. Epub 2014 Sep 29.

18.

Trends in discovery of new drugs for tuberculosis therapy.

Riccardi G, Pasca MR.

J Antibiot (Tokyo). 2014 Sep;67(9):655-9. doi: 10.1038/ja.2014.109. Epub 2014 Aug 6. Review.

PMID:
25095807
19.

Rv2466c mediates the activation of TP053 to kill replicating and non-replicating Mycobacterium tuberculosis.

Albesa-Jové D, Chiarelli LR, Makarov V, Pasca MR, Urresti S, Mori G, Salina E, Vocat A, Comino N, Mohorko E, Ryabova S, Pfieiffer B, Lopes Ribeiro AL, Rodrigo-Unzueta A, Tersa M, Zanoni G, Buroni S, Altmann KH, Hartkoorn RC, Glockshuber R, Cole ST, Riccardi G, Guerin ME.

ACS Chem Biol. 2014 Jul 18;9(7):1567-75. doi: 10.1021/cb500149m. Epub 2014 Jun 13.

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
21.

Synthesis of 3-heteryl substituted pyrrolidine-2,5-diones via catalytic Michael reaction and evaluation of their inhibitory activity against InhA and Mycobacterium tuberculosis.

Matviiuk T, Mori G, Lherbet C, Rodriguez F, Pasca MR, Gorichko M, Guidetti B, Voitenko Z, Baltas M.

Eur J Med Chem. 2014 Jan;71:46-52. doi: 10.1016/j.ejmech.2013.10.069. Epub 2013 Nov 4.

PMID:
24269516
22.

Design, chemical synthesis of 3-(9H-fluoren-9-yl)pyrrolidine-2,5-dione derivatives and biological activity against enoyl-ACP reductase (InhA) and Mycobacterium tuberculosis.

Matviiuk T, Rodriguez F, Saffon N, Mallet-Ladeira S, Gorichko M, de Jesus Lopes Ribeiro AL, Pasca MR, Lherbet C, Voitenko Z, Baltas M.

Eur J Med Chem. 2013;70:37-48. doi: 10.1016/j.ejmech.2013.09.041. Epub 2013 Oct 2.

PMID:
24140915
23.

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
24.

DprE1, a new taxonomic marker in mycobacteria.

Incandela ML, Perrin E, Fondi M, de Jesus Lopes Ribeiro AL, Mori G, Moiana A, Gramegna M, Fani R, Riccardi G, Pasca MR.

FEMS Microbiol Lett. 2013 Nov;348(1):66-73. doi: 10.1111/1574-6968.12246. Epub 2013 Sep 12.

25.

Synthesis and evaluation of α-ketotriazoles and α,β-diketotriazoles as inhibitors of Mycobacterium tuberculosis.

Menendez C, Rodriguez F, Ribeiro AL, Zara F, Frongia C, Lobjois V, Saffon N, Pasca MR, Lherbet C, Baltas M.

Eur J Med Chem. 2013 Nov;69:167-73. doi: 10.1016/j.ejmech.2013.06.042. Epub 2013 Jul 8.

PMID:
24016834
26.

A census of RND superfamily proteins in the Burkholderia genus.

Perrin E, Fondi M, Papaleo MC, Maida I, Emiliani G, Buroni S, Pasca MR, Riccardi G, Fani R.

Future Microbiol. 2013 Jul;8(7):923-37. doi: 10.2217/fmb.13.50.

PMID:
23841637
27.

Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection.

Poce G, Bates RH, Alfonso S, Cocozza M, Porretta GC, Ballell L, Rullas J, Ortega F, De Logu A, Agus E, La Rosa V, Pasca MR, De Rossi E, Wae B, Franzblau SG, Manetti F, Botta M, Biava M.

PLoS One. 2013;8(2):e56980. doi: 10.1371/journal.pone.0056980. Epub 2013 Feb 21.

28.

Phenotypic and genotypic characterisation of Burkholderia cenocepacia J2315 mutants affected in homoserine lactone and diffusible signal factor-based quorum sensing systems suggests interplay between both types of systems.

Udine C, Brackman G, Bazzini S, Buroni S, Van Acker H, Pasca MR, Riccardi G, Coenye T.

PLoS One. 2013;8(1):e55112. doi: 10.1371/journal.pone.0055112. Epub 2013 Jan 28.

29.

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.

30.

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
31.

Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents.

Menendez C, Chollet A, Rodriguez F, Inard C, Pasca MR, Lherbet C, Baltas M.

Eur J Med Chem. 2012 Jun;52:275-83. doi: 10.1016/j.ejmech.2012.03.029. Epub 2012 Mar 23.

PMID:
22483635
32.

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
33.

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.

34.

MmpL3 is the cellular target of the antitubercular pyrrole derivative BM212.

La Rosa V, Poce G, Canseco JO, Buroni S, Pasca MR, Biava M, Raju RM, Porretta GC, Alfonso S, Battilocchio C, Javid B, Sorrentino F, Ioerger TR, Sacchettini JC, Manetti F, Botta M, De Logu A, Rubin EJ, De Rossi E.

Antimicrob Agents Chemother. 2012 Jan;56(1):324-31. doi: 10.1128/AAC.05270-11. Epub 2011 Oct 24.

35.

Synthesis and biological activities of triazole derivatives as inhibitors of InhA and antituberculosis agents.

Menendez C, Gau S, Lherbet C, Rodriguez F, Inard C, Pasca MR, Baltas M.

Eur J Med Chem. 2011 Nov;46(11):5524-31. doi: 10.1016/j.ejmech.2011.09.013. Epub 2011 Sep 16.

PMID:
21944473
36.

Evaluation of fluoroquinolone resistance mechanisms in Pseudomonas aeruginosa multidrug resistance clinical isolates.

Pasca MR, Dalla Valle C, De Jesus Lopes Ribeiro AL, Buroni S, Papaleo MC, Bazzini S, Udine C, Incandela ML, Daffara S, Fani R, Riccardi G, Marone P.

Microb Drug Resist. 2012 Feb;18(1):23-32. doi: 10.1089/mdr.2011.0019. Epub 2011 Jul 28.

PMID:
21797666
37.

Deciphering the role of RND efflux transporters in Burkholderia cenocepacia.

Bazzini S, Udine C, Sass A, Pasca MR, Longo F, Emiliani G, Fondi M, Perrin E, Decorosi F, Viti C, Giovannetti L, Leoni L, Fani R, Riccardi G, Mahenthiralingam E, Buroni S.

PLoS One. 2011 Apr 19;6(4):e18902. doi: 10.1371/journal.pone.0018902.

38.

Mycobacterium tuberculosis phosphoribosylpyrophosphate synthetase: biochemical features of a crucial enzyme for mycobacterial cell wall biosynthesis.

Lucarelli AP, Buroni S, Pasca MR, Rizzi M, Cavagnino A, Valentini G, Riccardi G, Chiarelli LR.

PLoS One. 2010 Nov 15;5(11):e15494. doi: 10.1371/journal.pone.0015494.

39.

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
40.

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.

41.

Exploring the HME and HAE1 efflux systems in the genus Burkholderia.

Perrin E, Fondi M, Papaleo MC, Maida I, Buroni S, Pasca MR, Riccardi G, Fani R.

BMC Evol Biol. 2010 Jun 3;10:164. doi: 10.1186/1471-2148-10-164.

42.

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.

43.

Assessment of three Resistance-Nodulation-Cell Division drug efflux transporters of Burkholderia cenocepacia in intrinsic antibiotic resistance.

Buroni S, Pasca MR, Flannagan RS, Bazzini S, Milano A, Bertani I, Venturi V, Valvano MA, Riccardi G.

BMC Microbiol. 2009 Sep 17;9:200. doi: 10.1186/1471-2180-9-200.

44.

Control of MRSA infection and colonisation in an intensive care unit by GeneOhm MRSA assay and culture methods.

Dalla Valle C, Pasca MR, De Vitis D, Marzani FC, Emmi V, Marone P.

BMC Infect Dis. 2009 Aug 24;9:137. doi: 10.1186/1471-2334-9-137.

45.

Mycobacterium tuberculosis: drug resistance and future perspectives.

Riccardi G, Pasca MR, Buroni S.

Future Microbiol. 2009 Jun;4(5):597-614. doi: 10.2217/fmb.09.20. Review.

PMID:
19492969
46.

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.

47.

Azole resistance in Mycobacterium tuberculosis is mediated by the MmpS5-MmpL5 efflux system.

Milano A, Pasca MR, Provvedi R, Lucarelli AP, Manina G, Ribeiro AL, Manganelli R, Riccardi G.

Tuberculosis (Edinb). 2009 Jan;89(1):84-90. doi: 10.1016/j.tube.2008.08.003. Epub 2008 Oct 11.

PMID:
18851927
48.

Genomic analysis of zinc homeostasis in Mycobacterium tuberculosis.

Riccardi G, Milano A, Pasca MR, Nies DH.

FEMS Microbiol Lett. 2008 Oct;287(1):1-7. doi: 10.1111/j.1574-6968.2008.01320.x. Review.

49.

Global analysis of the Mycobacterium tuberculosis Zur (FurB) regulon.

Maciag A, Dainese E, Rodriguez GM, Milano A, Provvedi R, Pasca MR, Smith I, Palù G, Riccardi G, Manganelli R.

J Bacteriol. 2007 Feb;189(3):730-40. Epub 2006 Nov 10. Erratum in: J Bacteriol. 2007 Jul;189(13):4974.

50.

LfrR is a repressor that regulates expression of the efflux pump LfrA in Mycobacterium smegmatis.

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

Antimicrob Agents Chemother. 2006 Dec;50(12):4044-52. Epub 2006 Oct 16.

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