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Items: 19

1.

Fueling Open Innovation for Malaria Transmission-Blocking Drugs: Hundreds of Molecules Targeting Early Parasite Mosquito Stages.

Delves M, Lafuente-Monasterio MJ, Upton L, Ruecker A, Leroy D, Gamo FJ, Sinden R.

Front Microbiol. 2019 Sep 13;10:2134. doi: 10.3389/fmicb.2019.02134. eCollection 2019.

2.

Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target.

Alam MM, Sanchez-Azqueta A, Janha O, Flannery EL, Mahindra A, Mapesa K, Char AB, Sriranganadane D, Brancucci NMB, Antonova-Koch Y, Crouch K, Simwela NV, Millar SB, Akinwale J, Mitcheson D, Solyakov L, Dudek K, Jones C, Zapatero C, Doerig C, Nwakanma DC, Vázquez MJ, Colmenarejo G, Lafuente-Monasterio MJ, Leon ML, Godoi PHC, Elkins JM, Waters AP, Jamieson AG, Álvaro EF, Ranford-Cartwright LC, Marti M, Winzeler EA, Gamo FJ, Tobin AB.

Science. 2019 Aug 30;365(6456). pii: eaau1682. doi: 10.1126/science.aau1682.

PMID:
31467193
3.

Isoxazolopyrimidine-Based Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Antimalarial Activity.

Kokkonda S, El Mazouni F, White KL, White J, Shackleford DM, Lafuente-Monasterio MJ, Rowland P, Manjalanagara K, Joseph JT, Garcia-Pérez A, Fernandez J, Gamo FJ, Waterson D, Burrows JN, Palmer MJ, Charman SA, Rathod PK, Phillips MA.

ACS Omega. 2018 Aug 31;3(8):9227-9240. doi: 10.1021/acsomega.8b01573. Epub 2018 Aug 15.

4.

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.

Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K.

J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27.

PMID:
29665687
5.

Identification of Collateral Sensitivity to Dihydroorotate Dehydrogenase Inhibitors in Plasmodium falciparum.

Ross LS, Lafuente-Monasterio MJ, Sakata-Kato T, Mandt REK, Gamo FJ, Wirth DF, Lukens AK.

ACS Infect Dis. 2018 Apr 13;4(4):508-515. doi: 10.1021/acsinfecdis.7b00217. Epub 2018 Jan 22.

6.

Correction to The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold.

Sandoval E, Lafuente-Monasterio MJ, Almela MJ, Castañeda P, Jiménez Díaz MB, Martínez-Martínez MS, Vidal J, Angulo-Barturen Í, Bamborough P, Burrows J, Cammack N, Chaparro MJ, Coterón JM, de Cozar C, Crespo B, Díaz B, Drewes G, Fernández E, Ferrer-Bazaga S, Fraile MT, Gamo FJ, Ghidelli-Disse S, Gómez R, Haselden J, Huss S, León ML, de Mercado J, Macdonald SJF, Martín Hernando JI, Prats S, Puente M, Rodríguez A, de la Rosa JC, Rueda L, Selenski C, Willis P, Wilson DM, Witty M, Calderón F.

J Med Chem. 2017 Dec 14;60(23):9911. doi: 10.1021/acs.jmedchem.7b01491. Epub 2017 Nov 22. No abstract available.

PMID:
29164877
7.

Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.

Wilson CR, Gessner RK, Moosa A, Seldon R, Warner DF, Mizrahi V, Soares de Melo C, Simelane SB, Nchinda A, Abay E, Taylor D, Njoroge M, Brunschwig C, Lawrence N, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden P, Harris CJ, Gordon R, Ghidelli-Disse S, Pflaumer H, Boesche M, Drewes G, Sanz O, Santos G, Rebollo-Lopez MJ, Urones B, Selenski C, Lafuente-Monasterio MJ, Axtman M, Lelièvre J, Ballell L, Mueller R, Street LJ, Ghorpade SR, Chibale K.

J Med Chem. 2017 Dec 28;60(24):10118-10134. doi: 10.1021/acs.jmedchem.7b01347. Epub 2017 Dec 7.

8.

The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold.

Sandoval E, Lafuente-Monasterio MJ, Almela MJ, Castañeda P, Jiménez Díaz MB, Martínez-Martínez MS, Vidal J, Angulo-Barturen Í, Bamborough P, Burrows J, Cammack N, Chaparro MJ, Coterón JM, de Cozar C, Crespo B, Díaz B, Drewes G, Fernández E, Ferrer-Bazaga S, Fraile MT, Gamo FJ, Ghidelli-Disse S, Gómez R, Haselden J, Huss S, León ML, de Mercado J, Macdonald SJF, Martín Hernando JI, Prats S, Puente M, Rodríguez A, de la Rosa JC, Rueda L, Selenski C, Willis P, Wilson DM, Witty M, Calderón F.

J Med Chem. 2017 Aug 24;60(16):6880-6896. doi: 10.1021/acs.jmedchem.6b01441. Epub 2017 Aug 14. Erratum in: J Med Chem. 2017 Dec 14;60(23):9911.

PMID:
28806082
9.

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K.

Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735. doi: 10.1126/scitranslmed.aad9735.

10.

A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue.

Sonoiki E, Ng CL, Lee MC, Guo D, Zhang YK, Zhou Y, Alley MR, Ahyong V, Sanz LM, Lafuente-Monasterio MJ, Dong C, Schupp PG, Gut J, Legac J, Cooper RA, Gamo FJ, DeRisi J, Freund YR, Fidock DA, Rosenthal PJ.

Nat Commun. 2017 Mar 6;8:14574. doi: 10.1038/ncomms14574.

11.

Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles.

Williamson AE, Ylioja PM, Robertson MN, Antonova-Koch Y, Avery V, Baell JB, Batchu H, Batra S, Burrows JN, Bhattacharyya S, Calderon F, Charman SA, Clark J, Crespo B, Dean M, Debbert SL, Delves M, Dennis AS, Deroose F, Duffy S, Fletcher S, Giaever G, Hallyburton I, Gamo FJ, Gebbia M, Guy RK, Hungerford Z, Kirk K, Lafuente-Monasterio MJ, Lee A, Meister S, Nislow C, Overington JP, Papadatos G, Patiny L, Pham J, Ralph SA, Ruecker A, Ryan E, Southan C, Srivastava K, Swain C, Tarnowski MJ, Thomson P, Turner P, Wallace IM, Wells TN, White K, White L, Willis P, Winzeler EA, Wittlin S, Todd MH.

ACS Cent Sci. 2016 Oct 26;2(10):687-701. Epub 2016 Sep 14.

12.

Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.

Park Y, Pacitto A, Bayliss T, Cleghorn LA, Wang Z, Hartman T, Arora K, Ioerger TR, Sacchettini J, Rizzi M, Donini S, Blundell TL, Ascher DB, Rhee K, Breda A, Zhou N, Dartois V, Jonnala SR, Via LE, Mizrahi V, Epemolu O, Stojanovski L, Simeons F, Osuna-Cabello M, Ellis L, MacKenzie CJ, Smith AR, Davis SH, Murugesan D, Buchanan KI, Turner PA, Huggett M, Zuccotto F, Rebollo-Lopez MJ, Lafuente-Monasterio MJ, Sanz O, Diaz GS, Lelièvre J, Ballell L, Selenski C, Axtman M, Ghidelli-Disse S, Pflaumer H, Bösche M, Drewes G, Freiberg GM, Kurnick MD, Srikumaran M, Kempf DJ, Green SR, Ray PC, Read K, Wyatt P, Barry CE 3rd, Boshoff HI.

ACS Infect Dis. 2017 Jan 13;3(1):18-33. doi: 10.1021/acsinfecdis.6b00103. Epub 2016 Oct 17.

13.

A broad analysis of resistance development in the malaria parasite.

Corey VC, Lukens AK, Istvan ES, Lee MCS, Franco V, Magistrado P, Coburn-Flynn O, Sakata-Kato T, Fuchs O, Gnädig NF, Goldgof G, Linares M, Gomez-Lorenzo MG, De Cózar C, Lafuente-Monasterio MJ, Prats S, Meister S, Tanaseichuk O, Wree M, Zhou Y, Willis PA, Gamo FJ, Goldberg DE, Fidock DA, Wirth DF, Winzeler EA.

Nat Commun. 2016 Jun 15;7:11901. doi: 10.1038/ncomms11901.

14.

Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.

Crowther GJ, Hillesland HK, Keyloun KR, Reid MC, Lafuente-Monasterio MJ, Ghidelli-Disse S, Leonard SE, He P, Jones JC, Krahn MM, Mo JS, Dasari KS, Fox AM, Boesche M, El Bakkouri M, Rivas KL, Leroy D, Hui R, Drewes G, Maly DJ, Van Voorhis WC, Ojo KK.

PLoS One. 2016 Mar 2;11(3):e0149996. doi: 10.1371/journal.pone.0149996. eCollection 2016.

15.

Discovery of Dual-Stage Malaria Inhibitors with New Targets.

Raphemot R, Lafuente-Monasterio MJ, Gamo-Benito FJ, Clardy J, Derbyshire ER.

Antimicrob Agents Chemother. 2015 Dec 14;60(3):1430-7. doi: 10.1128/AAC.02110-15.

16.

In vitro resistance selections for Plasmodium falciparum dihydroorotate dehydrogenase inhibitors give mutants with multiple point mutations in the drug-binding site and altered growth.

Ross LS, Gamo FJ, Lafuente-Monasterio MJ, Singh OM, Rowland P, Wiegand RC, Wirth DF.

J Biol Chem. 2014 Jun 27;289(26):17980-95. doi: 10.1074/jbc.M114.558353. Epub 2014 Apr 29.

17.

Harnessing evolutionary fitness in Plasmodium falciparum for drug discovery and suppressing resistance.

Lukens AK, Ross LS, Heidebrecht R, Javier Gamo F, Lafuente-Monasterio MJ, Booker ML, Hartl DL, Wiegand RC, Wirth DF.

Proc Natl Acad Sci U S A. 2014 Jan 14;111(2):799-804. doi: 10.1073/pnas.1320886110. Epub 2013 Dec 31.

18.

Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.

Rodrigues T, da Cruz FP, Lafuente-Monasterio MJ, Gonçalves D, Ressurreição AS, Sitoe AR, Bronze MR, Gut J, Schneider G, Mota MM, Rosenthal PJ, Prudêncio M, Gamo FJ, Lopes F, Moreira R.

J Med Chem. 2013 Jun 13;56(11):4811-5. doi: 10.1021/jm400246e. Epub 2013 May 23.

PMID:
23701465
19.

Drug screen targeted at Plasmodium liver stages identifies a potent multistage antimalarial drug.

da Cruz FP, Martin C, Buchholz K, Lafuente-Monasterio MJ, Rodrigues T, Sönnichsen B, Moreira R, Gamo FJ, Marti M, Mota MM, Hannus M, Prudêncio M.

J Infect Dis. 2012 Apr 15;205(8):1278-86. doi: 10.1093/infdis/jis184. Epub 2012 Mar 6.

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