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Items: 1 to 50 of 55

1.

Competitive Fitness of Essential Gene Knockdowns Reveals a Broad-Spectrum Antibacterial Inhibitor of the Cell Division Protein FtsZ.

Hogan AM, Scoffone VC, Makarov V, Gislason AS, Tesfu H, Stietz MS, Brassinga AKC, Domaratzki M, Li X, Azzalin A, Biggiogera M, Riabova O, Monakhova N, Chiarelli LR, Riccardi G, Buroni S, Cardona ST.

Antimicrob Agents Chemother. 2018 Nov 26;62(12). pii: e01231-18. doi: 10.1128/AAC.01231-18. Print 2018 Dec.

2.

Investigating the Mechanism of Action of Diketopiperazines Inhibitors of the Burkholderia cenocepacia Quorum Sensing Synthase CepI: A Site-Directed Mutagenesis Study.

Buroni S, Scoffone VC, Fumagalli M, Makarov V, Cagnone M, Trespidi G, Rossi E, Forneris F, Riccardi G, Chiarelli LR.

Front Pharmacol. 2018 Jul 31;9:836. doi: 10.3389/fphar.2018.00836. eCollection 2018.

3.

Discovery and development of novel salicylate synthase (MbtI) furanic inhibitors as antitubercular agents.

Chiarelli LR, Mori M, Barlocco D, Beretta G, Gelain A, Pini E, Porcino M, Mori G, Stelitano G, Costantino L, Lapillo M, Bonanni D, Poli G, Tuccinardi T, Villa S, Meneghetti F.

Eur J Med Chem. 2018 Jul 15;155:754-763. doi: 10.1016/j.ejmech.2018.06.033. Epub 2018 Jun 18.

PMID:
29940465
4.

New Chromane-Based Derivatives as Inhibitors of Mycobacterium tuberculosis Salicylate Synthase (MbtI): Preliminary Biological Evaluation and Molecular Modeling Studies.

Pini E, Poli G, Tuccinardi T, Chiarelli LR, Mori M, Gelain A, Costantino L, Villa S, Meneghetti F, Barlocco D.

Molecules. 2018 Jun 21;23(7). pii: E1506. doi: 10.3390/molecules23071506.

5.

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.

6.

Burkholderia cenocepacia Infections in Cystic Fibrosis Patients: Drug Resistance and Therapeutic Approaches.

Scoffone VC, Chiarelli LR, Trespidi G, Mentasti M, Riccardi G, Buroni S.

Front Microbiol. 2017 Aug 22;8:1592. doi: 10.3389/fmicb.2017.01592. eCollection 2017. Review.

7.

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.

8.

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
9.

Biochemical Characterization of Glutamate Racemase-A New Candidate Drug Target against Burkholderia cenocepacia Infections.

Israyilova A, Buroni S, Forneris F, Scoffone VC, Shixaliyev NQ, Riccardi G, Chiarelli LR.

PLoS One. 2016 Nov 29;11(11):e0167350. doi: 10.1371/journal.pone.0167350. eCollection 2016.

10.

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
11.

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
12.

Discovery of new diketopiperazines inhibiting Burkholderia cenocepacia quorum sensing in vitro and in vivo.

Scoffone VC, Chiarelli LR, Makarov V, Brackman G, Israyilova A, Azzalin A, Forneris F, Riabova O, Savina S, Coenye T, Riccardi G, Buroni S.

Sci Rep. 2016 Sep 1;6:32487. doi: 10.1038/srep32487.

13.

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
14.

The Crystal Structure of Burkholderia cenocepacia DfsA Provides Insights into Substrate Recognition and Quorum Sensing Fatty Acid Biosynthesis.

Spadaro F, Scoffone VC, Chiarelli LR, Fumagalli M, Buroni S, Riccardi G, Forneris F.

Biochemistry. 2016 Jun 14;55(23):3241-50. doi: 10.1021/acs.biochem.6b00178. Epub 2016 Jun 2.

PMID:
27198181
15.

Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.

Tiwari R, Miller PA, Chiarelli LR, Mori G, Šarkan M, Centárová I, Cho S, Mikušová K, Franzblau SG, Oliver AG, Miller MJ.

ACS Med Chem Lett. 2016 Jan 4;7(3):266-70. doi: 10.1021/acsmedchemlett.5b00424. eCollection 2016 Mar 10.

16.

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.

17.

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.

18.

Tackling Critical Catalytic Residues in Helicobacter pylori L-Asparaginase.

Maggi M, Chiarelli LR, Valentini G, Scotti C.

Biomolecules. 2015 Mar 27;5(2):306-17. doi: 10.3390/biom5020306.

19.

Engineering of Helicobacter pylori L-asparaginase: characterization of two functionally distinct groups of mutants.

Maggi M, Chiarelli LR, Valentini G, Scotti C.

PLoS One. 2015 Feb 9;10(2):e0117025. doi: 10.1371/journal.pone.0117025. eCollection 2015.

20.

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
21.

Biochemistry of lipolytic enzymes secreted by Penicillium solitum and Cladosporium cladosporioides.

Chinaglia S, Chiarelli LR, Maggi M, Rodolfi M, Valentini G, Picco AM.

Biosci Biotechnol Biochem. 2014;78(2):245-54. doi: 10.1080/09168451.2014.882752. Epub 2014 Apr 16.

PMID:
25036677
22.

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.

23.

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
24.

Mechanism of action of 5-nitrothiophenes against Mycobacterium tuberculosis.

Hartkoorn RC, Ryabova OB, Chiarelli LR, Riccardi G, Makarov V, Cole ST.

Antimicrob Agents Chemother. 2014 May;58(5):2944-7. doi: 10.1128/AAC.02693-13. Epub 2014 Feb 18.

25.

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
26.

Protein recognition by short peptide reversible inhibitors of the chromatin-modifying LSD1/CoREST lysine demethylase.

Tortorici M, Borrello MT, Tardugno M, Chiarelli LR, Pilotto S, Ciossani G, Vellore NA, Bailey SG, Cowan J, O'Connell M, Crabb SJ, Packham G, Mai A, Baron R, Ganesan A, Mattevi A.

ACS Chem Biol. 2013 Aug 16;8(8):1677-82. doi: 10.1021/cb4001926. Epub 2013 Jun 11.

PMID:
23721412
27.

Structural and energetic basis of protein kinetic destabilization in human phosphoglycerate kinase 1 deficiency.

Pey AL, Mesa-Torres N, Chiarelli LR, Valentini G.

Biochemistry. 2013 Feb 19;52(7):1160-70. doi: 10.1021/bi301565m. Epub 2013 Feb 4.

PMID:
23336698
28.

BEL β-trefoil: a novel lectin with antineoplastic properties in king bolete (Boletus edulis) mushrooms.

Bovi M, Cenci L, Perduca M, Capaldi S, Carrizo ME, Civiero L, Chiarelli LR, Galliano M, Monaco HL.

Glycobiology. 2013 May;23(5):578-92. doi: 10.1093/glycob/cws164. Epub 2012 Dec 4.

PMID:
23213111
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.

Monitoring of inosine monophosphate dehydrogenase activity and expression during the early period of mycophenolate mofetil therapy in de novo renal transplant patients.

Molinaro M, Chiarelli LR, Biancone L, Castagneto M, Boschiero L, Pisani F, Sabbatini M, Sandrini S, Arbustini E, Tinelli C, Regazzi M, Schena FP, Segoloni GP.

Drug Metab Pharmacokinet. 2013;28(2):109-17. Epub 2012 Aug 14.

31.

A new variant of phosphoglycerate kinase deficiency (p.I371K) with multiple tissue involvement: molecular and functional characterization.

Fermo E, Bianchi P, Chiarelli LR, Maggi M, Mandarà GM, Vercellati C, Marcello AP, Barcellini W, Cortelezzi A, Valentini G, Zanella A.

Mol Genet Metab. 2012 Aug;106(4):455-61. doi: 10.1016/j.ymgme.2012.05.015. Epub 2012 May 30.

PMID:
22705348
32.

Letter to the editor regarding Shibayama et al.: Biochemical and pathophysiological characterization of Helicobacter pylori asparaginase.

Scotti C, Pasquetto MV, Covini D, Chiarelli LR, Valentini G.

Microbiol Immunol. 2012 Jun;56(6):420-1; author reply 422. doi: 10.1111/j.1348-0421.2012.00460.x. No abstract available.

33.

Molecular insights on pathogenic effects of mutations causing phosphoglycerate kinase deficiency.

Chiarelli LR, Morera SM, Bianchi P, Fermo E, Zanella A, Galizzi A, Valentini G.

PLoS One. 2012;7(2):e32065. doi: 10.1371/journal.pone.0032065. Epub 2012 Feb 14.

34.

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.

35.

Expanding targets for a metabolic therapy of cancer: L-asparaginase.

Covini D, Tardito S, Bussolati O, Chiarelli LR, Pasquetto MV, Digilio R, Valentini G, Scotti C.

Recent Pat Anticancer Drug Discov. 2012 Jan;7(1):4-13. Review.

PMID:
21854356
36.

Structure of a lectin with antitumoral properties in king bolete (Boletus edulis) mushrooms.

Bovi M, Carrizo ME, Capaldi S, Perduca M, Chiarelli LR, Galliano M, Monaco HL.

Glycobiology. 2011 Aug;21(8):1000-9. doi: 10.1093/glycob/cwr012. Epub 2011 Feb 8.

PMID:
21303815
37.

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.

38.

Cell-cycle inhibition by Helicobacter pylori L-asparaginase.

Scotti C, Sommi P, Pasquetto MV, Cappelletti D, Stivala S, Mignosi P, Savio M, Chiarelli LR, Valentini G, Bolanos-Garcia VM, Merrell DS, Franchini S, Verona ML, Bolis C, Solcia E, Manca R, Franciotta D, Casasco A, Filipazzi P, Zardini E, Vannini V.

PLoS One. 2010 Nov 9;5(11):e13892. doi: 10.1371/journal.pone.0013892. Erratum in: PLoS One. 2012;7(2). doi: 10.1371/annotation/c6c16a43-aadd-4cd3-a916-e935534dab38.

39.

Biochemical signatures of doppel protein in human astrocytomas to support prediction in tumor malignancy.

Rognoni P, Chiarelli LR, Comincini S, Azzalin A, Miracco C, Valentini G.

J Biomed Biotechnol. 2010;2010:301067. doi: 10.1155/2010/301067. Epub 2010 Oct 14.

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.

Inosine monophosphate dehydrogenase variability in renal transplant patients on long-term mycophenolate mofetil therapy.

Chiarelli LR, Molinaro M, Libetta C, Tinelli C, Cosmai L, Valentini G, Dal Canton A, Regazzi M.

Br J Clin Pharmacol. 2010 Jan;69(1):38-50. doi: 10.1111/j.1365-2125.2009.03542.x.

42.

ThermoFAD, a Thermofluor-adapted flavin ad hoc detection system for protein folding and ligand binding.

Forneris F, Orru R, Bonivento D, Chiarelli LR, Mattevi A.

FEBS J. 2009 May;276(10):2833-40. doi: 10.1111/j.1742-4658.2009.07006.x.

43.

Helicobacter pyloril-asparaginase: a promising chemotherapeutic agent.

Cappelletti D, Chiarelli LR, Pasquetto MV, Stivala S, Valentini G, Scotti C.

Biochem Biophys Res Commun. 2008 Dec 26;377(4):1222-6. doi: 10.1016/j.bbrc.2008.10.118. Epub 2008 Nov 5.

PMID:
18983825
44.

Molecular basis of pyrimidine 5'-nucleotidase deficiency caused by 3 newly identified missense mutations (c.187T>C, c.469G>C and c.740T>C) and a tabulation of known mutations.

Chiarelli LR, Morera SM, Galizzi A, Fermo E, Zanella A, Valentini G.

Blood Cells Mol Dis. 2008 May-Jun;40(3):295-301.

PMID:
18499901
45.

Erythrocyte adenylate kinase deficiency: characterization of recombinant mutant forms and relationship with nonspherocytic hemolytic anemia.

Abrusci P, Chiarelli LR, Galizzi A, Fermo E, Bianchi P, Zanella A, Valentini G.

Exp Hematol. 2007 Aug;35(8):1182-9.

PMID:
17662886
46.

Pyruvate kinase deficiency: the genotype-phenotype association.

Zanella A, Fermo E, Bianchi P, Chiarelli LR, Valentini G.

Blood Rev. 2007 Jul;21(4):217-31. Epub 2007 Mar 13. Review.

PMID:
17360088
47.

Nuclear mRNA retention and aberrant doppel protein expression in human astrocytic tumor cells.

Comincini S, Chiarelli LR, Zelini P, Del Vecchio I, Azzalin A, Arias A, Ferrara V, Rognoni P, Dipoto A, Nano R, Valentini G, Ferretti L.

Oncol Rep. 2006 Dec;16(6):1325-32.

PMID:
17089057
48.

Two new mutations of the P5'N-1 gene found in Italian patients with hereditary hemolytic anemia: the molecular basis of the red cell enzyme disorder.

Chiarelli LR, Fermo E, Abrusci P, Bianchi P, Dellacasa CM, Galizzi A, Zanella A, Valentini G.

Haematologica. 2006 Sep;91(9):1244-7.

49.

Hereditary erythrocyte pyrimidine 5'-nucleotidase deficiency: a biochemical, genetic and clinical overview.

Chiarelli LR, Fermo E, Zanella A, Valentini G.

Hematology. 2006 Feb;11(1):67-72. Review.

PMID:
16522554
50.

Absence of interaction between doppel and GFAP, Grb2, PrPc proteins in human tumor astrocytic cells.

Azzalin A, Del Vecchio I, Chiarelli LR, Valentini G, Comincini S, Ferretti L.

Anticancer Res. 2005 Nov-Dec;25(6B):4369-74.

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