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Items: 41

1.

Pyrrolomycins are Potent Natural Protonophores.

Valderrama K, Pradel E, Firsov AM, Drobecq H, Bauderlique-le Roy H, Villemagne B, Antonenko YN, Hartkoorn RC.

Antimicrob Agents Chemother. 2019 Aug 12. pii: AAC.01450-19. doi: 10.1128/AAC.01450-19. [Epub ahead of print]

PMID:
31405863
2.

Characterization of new, efficient Mycobacterium tuberculosis topoisomerase-I inhibitors and their interaction with human ABC multidrug transporters.

Temesszentandrási-Ambrus C, Tóth S, Verma R, Bánhegyi P, Szabadkai I, Baska F, Szántai-Kis C, Hartkoorn RC, Lingerfelt MA, Sarkadi B, Szakács G, Őrfi L, Nagaraja V, Ekins S, Telbisz Á.

PLoS One. 2018 Sep 5;13(9):e0202749. doi: 10.1371/journal.pone.0202749. eCollection 2018.

3.

Accelerated microfluidic native chemical ligation at difficult amino acids toward cyclic peptides.

Ollivier N, Toupy T, Hartkoorn RC, Desmet R, Monbaliu JM, Melnyk O.

Nat Commun. 2018 Jul 20;9(1):2847. doi: 10.1038/s41467-018-05264-8.

4.

Total Synthesis of Ripostatin B and Structure-Activity Relationship Studies on Ripostatin Analogs.

Glaus F, Dedić D, Tare P, Nagaraja V, Rodrigues L, Aínsa JA, Kunze J, Schneider G, Hartkoorn RC, Cole ST, Altmann KH.

J Org Chem. 2018 Jul 6;83(13):7150-7172. doi: 10.1021/acs.joc.8b00193. Epub 2018 Mar 29.

PMID:
29542926
5.

A druggable secretory protein maturase of Toxoplasma essential for invasion and egress.

Dogga SK, Mukherjee B, Jacot D, Kockmann T, Molino L, Hammoudi PM, Hartkoorn RC, Hehl AB, Soldati-Favre D.

Elife. 2017 Sep 12;6. pii: e27480. doi: 10.7554/eLife.27480.

6.

Discovery and Biosynthesis of Gladiolin: A Burkholderia gladioli Antibiotic with Promising Activity against Mycobacterium tuberculosis.

Song L, Jenner M, Masschelein J, Jones C, Bull MJ, Harris SR, Hartkoorn RC, Vocat A, Romero-Canelon I, Coupland P, Webster G, Dunn M, Weiser R, Paisey C, Cole ST, Parkhill J, Mahenthiralingam E, Challis GL.

J Am Chem Soc. 2017 Jun 14;139(23):7974-7981. doi: 10.1021/jacs.7b03382. Epub 2017 Jun 5.

7.

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria.

Singh V, Dhar N, Pató J, Kolly GS, Korduláková J, Forbak M, Evans JC, Székely R, Rybniker J, Palčeková Z, Zemanová J, Santi I, Signorino-Gelo F, Rodrigues L, Vocat A, Covarrubias AS, Rengifo MG, Johnsson K, Mowbray S, Buechler J, Delorme V, Brodin P, Knott GW, Aínsa JA, Warner DF, Kéri G, Mikušová K, McKinney JD, Cole ST, Mizrahi V, Hartkoorn RC.

Mol Microbiol. 2017 Jan;103(1):13-25. doi: 10.1111/mmi.13535. Epub 2016 Oct 29.

8.

The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis.

Singh V, Donini S, Pacitto A, Sala C, Hartkoorn RC, Dhar N, Keri G, Ascher DB, Mondésert G, Vocat A, Lupien A, Sommer R, Vermet H, Lagrange S, Buechler J, Warner DF, McKinney JD, Pato J, Cole ST, Blundell TL, Rizzi M, Mizrahi V.

ACS Infect Dis. 2017 Jan 13;3(1):5-17. doi: 10.1021/acsinfecdis.6b00102. Epub 2016 Sep 8.

9.

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
10.

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.

11.

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
12.

The 8-Pyrrole-Benzothiazinones Are Noncovalent 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 Aug;59(8):4446-52. doi: 10.1128/AAC.00778-15. Epub 2015 May 18.

13.

Bioluminescence for assessing drug potency against nonreplicating Mycobacterium tuberculosis.

Vocat A, Hartkoorn RC, Lechartier B, Zhang M, Dhar N, Cole ST, Sala C.

Antimicrob Agents Chemother. 2015 Jul;59(7):4012-9. doi: 10.1128/AAC.00528-15. Epub 2015 Apr 20.

14.

Lead selection and characterization of antitubercular compounds using the Nested Chemical Library.

Sipos A, Pató J, Székely R, Hartkoorn RC, Kékesi L, Őrfi L, Szántai-Kis C, Mikušová K, Svetlíková Z, Korduláková J, Nagaraja V, Godbole AA, Bush N, Collin F, Maxwell A, Cole ST, Kéri G.

Tuberculosis (Edinb). 2015 Jun;95 Suppl 1:S200-6. doi: 10.1016/j.tube.2015.02.028. Epub 2015 Feb 28.

PMID:
25801335
15.

Whole-transcriptome sequencing for high-resolution transcriptomic analysis in Mycobacterium tuberculosis.

Benjak A, Sala C, Hartkoorn RC.

Methods Mol Biol. 2015;1285:17-30. doi: 10.1007/978-1-4939-2450-9_2.

PMID:
25779308
16.

Whole-genome sequencing for comparative genomics and de novo genome assembly.

Benjak A, Sala C, Hartkoorn RC.

Methods Mol Biol. 2015;1285:1-16. doi: 10.1007/978-1-4939-2450-9_1.

PMID:
25779307
17.

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
18.

Anticytolytic screen identifies inhibitors of mycobacterial virulence protein secretion.

Rybniker J, Chen JM, Sala C, Hartkoorn RC, Vocat A, Benjak A, Boy-Röttger S, Zhang M, Székely R, Greff Z, Orfi L, Szabadkai I, Pató J, Kéri G, Cole ST.

Cell Host Microbe. 2014 Oct 8;16(4):538-48. doi: 10.1016/j.chom.2014.09.008.

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.

Cross-resistance between clofazimine and bedaquiline through upregulation of MmpL5 in Mycobacterium tuberculosis.

Hartkoorn RC, Uplekar S, Cole ST.

Antimicrob Agents Chemother. 2014 May;58(5):2979-81. doi: 10.1128/AAC.00037-14. Epub 2014 Mar 3.

21.

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.

22.

Assessing the essentiality of the decaprenyl-phospho-d-arabinofuranose pathway in Mycobacterium tuberculosis using conditional mutants.

Kolly GS, Boldrin F, Sala C, Dhar N, Hartkoorn RC, Ventura M, Serafini A, McKinney JD, Manganelli R, Cole ST.

Mol Microbiol. 2014 Apr;92(1):194-211. doi: 10.1111/mmi.12546. Epub 2014 Mar 7.

23.

Towards a new combination therapy for tuberculosis with next generation benzothiazinones.

Makarov V, Lechartier B, Zhang M, Neres J, van der Sar AM, Raadsen SA, Hartkoorn RC, Ryabova OB, Vocat A, Decosterd LA, Widmer N, Buclin T, Bitter W, Andries K, Pojer F, Dyson PJ, Cole ST.

EMBO Mol Med. 2014 Mar;6(3):372-83. doi: 10.1002/emmm.201303575. Epub 2014 Feb 5.

24.

Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA.

Hartkoorn RC, Pojer F, Read JA, Gingell H, Neres J, Horlacher OP, Altmann KH, Cole ST.

Nat Chem Biol. 2014 Feb;10(2):96-8. doi: 10.1038/nchembio.1405. Epub 2013 Dec 1.

PMID:
24292073
25.

Synthesis and antimycobacterial activity of 2,1'-dihydropyridomycins.

Horlacher OP, Hartkoorn RC, Cole ST, Altmann KH.

ACS Med Chem Lett. 2012 Dec 18;4(2):264-8. doi: 10.1021/ml300385q. eCollection 2013 Feb 14.

26.

Towards a new tuberculosis drug: pyridomycin - nature's isoniazid.

Hartkoorn RC, Sala C, Neres J, Pojer F, Magnet S, Mukherjee R, Uplekar S, Boy-Röttger S, Altmann KH, Cole ST.

EMBO Mol Med. 2012 Oct;4(10):1032-42. doi: 10.1002/emmm.201201689. Epub 2012 Sep 17.

27.

In vitro combination studies of benzothiazinone lead compound BTZ043 against Mycobacterium tuberculosis.

Lechartier B, Hartkoorn RC, Cole ST.

Antimicrob Agents Chemother. 2012 Nov;56(11):5790-3. doi: 10.1128/AAC.01476-12. Epub 2012 Aug 27.

28.

Streptomycin-starved Mycobacterium tuberculosis 18b, a drug discovery tool for latent tuberculosis.

Zhang M, Sala C, Hartkoorn RC, Dhar N, Mendoza-Losana A, Cole ST.

Antimicrob Agents Chemother. 2012 Nov;56(11):5782-9. doi: 10.1128/AAC.01125-12. Epub 2012 Aug 27.

29.

Genome-wide definition of the SigF regulon in Mycobacterium tuberculosis.

Hartkoorn RC, Sala C, Uplekar S, Busso P, Rougemont J, Cole ST.

J Bacteriol. 2012 Apr;194(8):2001-9. doi: 10.1128/JB.06692-11. Epub 2012 Feb 3.

30.

Tuberculosis drugs: new candidates and how to find more.

Sala C, Hartkoorn RC.

Future Microbiol. 2011 Jun;6(6):617-33. doi: 10.2217/fmb.11.46. Review.

PMID:
21707310
31.

Leads for antitubercular compounds from kinase inhibitor library screens.

Magnet S, Hartkoorn RC, Székely R, Pató J, Triccas JA, Schneider P, Szántai-Kis C, Orfi L, Chambon M, Banfi D, Bueno M, Turcatti G, Kéri G, Cole ST.

Tuberculosis (Edinb). 2010 Nov;90(6):354-60. doi: 10.1016/j.tube.2010.09.001. Epub 2010 Oct 8.

PMID:
20934382
32.

Sigma factor F does not prevent rifampin inhibition of RNA polymerase or cause rifampin tolerance in Mycobacterium tuberculosis.

Hartkoorn RC, Sala C, Magnet SJ, Chen JM, Pojer F, Cole ST.

J Bacteriol. 2010 Oct;192(20):5472-9. doi: 10.1128/JB.00687-10. Epub 2010 Aug 20.

33.

Simple model for testing drugs against nonreplicating Mycobacterium tuberculosis.

Sala C, Dhar N, Hartkoorn RC, Zhang M, Ha YH, Schneider P, Cole ST.

Antimicrob Agents Chemother. 2010 Oct;54(10):4150-8. doi: 10.1128/AAC.00821-10. Epub 2010 Aug 2.

34.

HIV protease inhibitors are substrates for OATP1A2, OATP1B1 and OATP1B3 and lopinavir plasma concentrations are influenced by SLCO1B1 polymorphisms.

Hartkoorn RC, Kwan WS, Shallcross V, Chaikan A, Liptrott N, Egan D, Sora ES, James CE, Gibbons S, Bray PG, Back DJ, Khoo SH, Owen A.

Pharmacogenet Genomics. 2010 Feb;20(2):112-20. doi: 10.1097/FPC.0b013e328335b02d.

35.

Cultured CD4T cells and primary human lymphocytes express hOATPs: intracellular accumulation of saquinavir and lopinavir.

Janneh O, Hartkoorn RC, Jones E, Owen A, Ward SA, Davey R, Back DJ, Khoo SH.

Br J Pharmacol. 2008 Nov;155(6):875-83. doi: 10.1038/bjp.2008.320. Epub 2008 Aug 18.

36.

Effect of transporter modulation on the emergence of nelfinavir resistance in vitro.

Chandler B, Detsika M, Owen A, Evans S, Hartkoorn RC, Cane PA, Back DJ, Khoo SH.

Antivir Ther. 2007;12(5):831-4.

PMID:
17713167
37.

A rapid and sensitive HPLC-MS method for the detection of plasma and cellular rifampicin.

Hartkoorn RC, Khoo S, Back DJ, Tjia JF, Waitt CJ, Chaponda M, Davies G, Ardrey A, Ashleigh S, Ward SA.

J Chromatogr B Analyt Technol Biomed Life Sci. 2007 Sep 15;857(1):76-82. Epub 2007 Jul 10.

PMID:
17643357
38.

Differential drug susceptibility of intracellular and extracellular tuberculosis, and the impact of P-glycoprotein.

Hartkoorn RC, Chandler B, Owen A, Ward SA, Bertel Squire S, Back DJ, Khoo SH.

Tuberculosis (Edinb). 2007 May;87(3):248-55. Epub 2007 Jan 26.

PMID:
17258938
39.

Modulation of the intracellular accumulation of saquinavir in peripheral blood mononuclear cells by inhibitors of MRP1, MRP2, P-gp and BCRP.

Janneh O, Owen A, Chandler B, Hartkoorn RC, Hart CA, Bray PG, Ward SA, Back DJ, Khoo SH.

AIDS. 2005 Dec 2;19(18):2097-102.

PMID:
16284458
40.

In vitro synergy and enhanced murine brain penetration of saquinavir coadministered with mefloquine.

Owen A, Janneh O, Hartkoorn RC, Chandler B, Bray PG, Martin P, Ward SA, Hart CA, Khoo SH, Back DJ.

J Pharmacol Exp Ther. 2005 Sep;314(3):1202-9. Epub 2005 May 27.

PMID:
15923343
41.

Expression of P-glycoprotein, multidrug-resistance proteins 1 and 2 in CEM, CEM(VBL), CEM(E1000), MDCKII(MRP1) and MDCKII(MRP2) cell lines.

Owen A, Hartkoorn RC, Khoo S, Back D.

AIDS. 2003 Oct 17;17(15):2276-8. No abstract available.

PMID:
14523293

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