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1.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

2.

A high throughput screen for next-generation leads targeting malaria parasite transmission.

Delves MJ, Miguel-Blanco C, Matthews H, Molina I, Ruecker A, Yahiya S, Straschil U, Abraham M, León ML, Fischer OJ, Rueda-Zubiaurre A, Brandt JR, Cortés Á, Barnard A, Fuchter MJ, Calderón F, Winzeler EA, Sinden RE, Herreros E, Gamo FJ, Baum J.

Nat Commun. 2018 Sep 18;9(1):3805. doi: 10.1038/s41467-018-05777-2.

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.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

PMID:
29941635
5.

High-throughput microsphiltration to assess red blood cell deformability and screen for malaria transmission-blocking drugs.

Duez J, Carucci M, Garcia-Barbazan I, Corral M, Perez O, Presa JL, Henry B, Roussel C, Ndour PA, Rosa NB, Sanz L, Gamo FJ, Buffet P.

Nat Protoc. 2018 Jun;13(6):1362-1376. doi: 10.1038/nprot.2018.035. Epub 2018 May 24.

PMID:
29844524
6.

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.

7.

Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics.

Cowell AN, Istvan ES, Lukens AK, Gomez-Lorenzo MG, Vanaerschot M, Sakata-Kato T, Flannery EL, Magistrado P, Owen E, Abraham M, LaMonte G, Painter HJ, Williams RM, Franco V, Linares M, Arriaga I, Bopp S, Corey VC, Gnädig NF, Coburn-Flynn O, Reimer C, Gupta P, Murithi JM, Moura PA, Fuchs O, Sasaki E, Kim SW, Teng CH, Wang LT, Akidil A, Adjalley S, Willis PA, Siegel D, Tanaseichuk O, Zhong Y, Zhou Y, Llinás M, Ottilie S, Gamo FJ, Lee MCS, Goldberg DE, Fidock DA, Wirth DF, Winzeler EA.

Science. 2018 Jan 12;359(6372):191-199. doi: 10.1126/science.aan4472.

8.

Efforts Aimed To Reduce Attrition in Antimalarial Drug Discovery: A Systematic Evaluation of the Current Antimalarial Targets Portfolio.

Chaparro MJ, Calderón F, Castañeda P, Fernández-Alvaro E, Gabarró R, Gamo FJ, Gómez-Lorenzo MG, Martín J, Fernández E.

ACS Infect Dis. 2018 Apr 13;4(4):568-576. doi: 10.1021/acsinfecdis.7b00211. Epub 2018 Jan 24.

PMID:
29320160
9.

A human microdose study of the antimalarial drug GSK3191607 in healthy volunteers.

Okour M, Derimanov G, Barnett R, Fernandez E, Ferrer S, Gresham S, Hossain M, Gamo FJ, Koh G, Pereira A, Rolfe K, Wong D, Young G, Rami H, Haselden J.

Br J Clin Pharmacol. 2018 Mar;84(3):482-489. doi: 10.1111/bcp.13476. Epub 2017 Dec 29.

PMID:
29168205
10.

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
11.

A potent series targeting the malarial cGMP-dependent protein kinase clears infection and blocks transmission.

Baker DA, Stewart LB, Large JM, Bowyer PW, Ansell KH, Jiménez-Díaz MB, El Bakkouri M, Birchall K, Dechering KJ, Bouloc NS, Coombs PJ, Whalley D, Harding DJ, Smiljanic-Hurley E, Wheldon MC, Walker EM, Dessens JT, Lafuente MJ, Sanz LM, Gamo FJ, Ferrer SB, Hui R, Bousema T, Angulo-Barturén I, Merritt AT, Croft SL, Gutteridge WE, Kettleborough CA, Osborne SA.

Nat Commun. 2017 Sep 5;8(1):430. doi: 10.1038/s41467-017-00572-x.

12.

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.

PMID:
28806082
13.

Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate.

Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Freund YR, Berry P, Ciaravino V, Erve JCL, Rosenthal PJ, Campo B, Gamo FJ, Sanz LM, Cao J.

J Med Chem. 2017 Jul 13;60(13):5889-5908. doi: 10.1021/acs.jmedchem.7b00621. Epub 2017 Jun 29.

PMID:
28635296
14.

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance.

O'Neill PM, Amewu RK, Charman SA, Sabbani S, Gnädig NF, Straimer J, Fidock DA, Shore ER, Roberts NL, Wong MH, Hong WD, Pidathala C, Riley C, Murphy B, Aljayyoussi G, Gamo FJ, Sanz L, Rodrigues J, Cortes CG, Herreros E, Angulo-Barturén I, Jiménez-Díaz MB, Bazaga SF, Martínez-Martínez MS, Campo B, Sharma R, Ryan E, Shackleford DM, Campbell S, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Palmer MJ, Copple IM, Mercer AE, Ruecker A, Delves MJ, Sinden RE, Siegl P, Davies J, Rochford R, Kocken CHM, Zeeman AM, Nixon GL, Biagini GA, Ward SA.

Nat Commun. 2017 May 24;8:15159. doi: 10.1038/ncomms15159.

15.

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.

16.

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.

17.

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.

18.

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.

Van Voorhis WC, Adams JH, Adelfio R, Ahyong V, Akabas MH, Alano P, Alday A, Alemán Resto Y, Alsibaee A, Alzualde A, Andrews KT, Avery SV, Avery VM, Ayong L, Baker M, Baker S, Ben Mamoun C, Bhatia S, Bickle Q, Bounaadja L, Bowling T, Bosch J, Boucher LE, Boyom FF, Brea J, Brennan M, Burton A, Caffrey CR, Camarda G, Carrasquilla M, Carter D, Belen Cassera M, Chih-Chien Cheng K, Chindaudomsate W, Chubb A, Colon BL, Colón-López DD, Corbett Y, Crowther GJ, Cowan N, D'Alessandro S, Le Dang N, Delves M, DeRisi JL, Du AY, Duffy S, Abd El-Salam El-Sayed S, Ferdig MT, Fernández Robledo JA, Fidock DA, Florent I, Fokou PV, Galstian A, Gamo FJ, Gokool S, Gold B, Golub T, Goldgof GM, Guha R, Guiguemde WA, Gural N, Guy RK, Hansen MA, Hanson KK, Hemphill A, Hooft van Huijsduijnen R, Horii T, Horrocks P, Hughes TB, Huston C, Igarashi I, Ingram-Sieber K, Itoe MA, Jadhav A, Naranuntarat Jensen A, Jensen LT, Jiang RH, Kaiser A, Keiser J, Ketas T, Kicka S, Kim S, Kirk K, Kumar VP, Kyle DE, Lafuente MJ, Landfear S, Lee N, Lee S, Lehane AM, Li F, Little D, Liu L, Llinás M, Loza MI, Lubar A, Lucantoni L, Lucet I, Maes L, Mancama D, Mansour NR, March S, McGowan S, Medina Vera I, Meister S, Mercer L, Mestres J, Mfopa AN, Misra RN, Moon S, Moore JP, Morais Rodrigues da Costa F, Müller J, Muriana A, Nakazawa Hewitt S, Nare B, Nathan C, Narraidoo N, Nawaratna S, Ojo KK, Ortiz D, Panic G, Papadatos G, Parapini S, Patra K, Pham N, Prats S, Plouffe DM, Poulsen SA, Pradhan A, Quevedo C, Quinn RJ, Rice CA, Abdo Rizk M, Ruecker A, St Onge R, Salgado Ferreira R, Samra J, Robinett NG, Schlecht U, Schmitt M, Silva Villela F, Silvestrini F, Sinden R, Smith DA, Soldati T, Spitzmüller A, Stamm SM, Sullivan DJ, Sullivan W, Suresh S, Suzuki BM, Suzuki Y, Swamidass SJ, Taramelli D, Tchokouaha LR, Theron A, Thomas D, Tonissen KF, Townson S, Tripathi AK, Trofimov V, Udenze KO, Ullah I, Vallieres C, Vigil E, Vinetz JM, Voong Vinh P, Vu H, Watanabe NA, Weatherby K, White PM, Wilks AF, Winzeler EA, Wojcik E, Wree M, Wu W, Yokoyama N, Zollo PH, Abla N, Blasco B, Burrows J, Laleu B, Leroy D, Spangenberg T, Wells T, Willis PA.

PLoS Pathog. 2016 Jul 28;12(7):e1005763. doi: 10.1371/journal.ppat.1005763. eCollection 2016 Jul.

19.

Development of a Novel High-Density [3H]Hypoxanthine Scintillation Proximity Assay To Assess Plasmodium falciparum Growth.

de Cózar C, Caballero I, Colmenarejo G, Sanz LM, Álvarez-Ruiz E, Gamo FJ, Cid C.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):5949-56. doi: 10.1128/AAC.00433-16. Print 2016 Oct.

20.

A novel validated assay to support the discovery of new anti-malarial gametocytocidal agents.

Bahamontes-Rosa N, Gomez-Lorenzo MG, Lelièvre J, Rodriguez Alejandre A, Almela MJ, Lozano S, Herreros E, Gamo FJ.

Malar J. 2016 Jul 22;15(1):385. doi: 10.1186/s12936-016-1429-9.

21.

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.

Norcross NR, Baragaña B, Wilson C, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Porzelle A, Grimaldi R, Wittlin S, Duffy S, Avery VM, Meister S, Sanz L, Jiménez-Díaz B, Angulo-Barturen I, Ferrer S, Martínez MS, Gamo FJ, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH.

J Med Chem. 2016 Jul 14;59(13):6101-20. doi: 10.1021/acs.jmedchem.6b00028. Epub 2016 Jun 17.

22.

A broad analysis of resistance development in the malaria parasite.

Corey VC, Lukens AK, Istvan ES, Lee MC, 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.

23.

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Martínez MS, Bolscher JM, Woodland A, Luksch T, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2016 Sep 1;537(7618):122. doi: 10.1038/nature18280. Epub 2016 May 25. No abstract available.

24.

A high-throughput fluorescence-based assay for Plasmodium dihydroorotate dehydrogenase inhibitor screening.

Caballero I, Lafuente MJ, Gamo FJ, Cid C.

Anal Biochem. 2016 Aug 1;506:13-21. doi: 10.1016/j.ab.2016.04.013. Epub 2016 Apr 29.

PMID:
27133204
25.

Identifying rapidly parasiticidal anti-malarial drugs using a simple and reliable in vitro parasite viability fast assay.

Linares M, Viera S, Crespo B, Franco V, Gómez-Lorenzo MG, Jiménez-Díaz MB, Angulo-Barturen Í, Sanz LM, Gamo FJ.

Malar J. 2015 Nov 5;14:441. doi: 10.1186/s12936-015-0962-2.

26.

A novel multiple-stage antimalarial agent that inhibits protein synthesis.

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Luksch T, Martínez MS, Luksch T, Bolscher JM, Woodland A, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2015 Jun 18;522(7556):315-20. doi: 10.1038/nature14451. Erratum in: Nature. 2016 Sep 1;537(7618):122.

27.

Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.

Zhang YK, Plattner JJ, Easom EE, Jacobs RT, Guo D, Sanders V, Freund YR, Campo B, Rosenthal PJ, Bu W, Gamo FJ, Sanz LM, Ge M, Li L, Ding J, Yang Y.

J Med Chem. 2015 Jul 9;58(13):5344-54. doi: 10.1021/acs.jmedchem.5b00678. Epub 2015 Jun 23.

28.

(+)-SJ733, a clinical candidate for malaria that acts through ATP4 to induce rapid host-mediated clearance of Plasmodium.

Jiménez-Díaz MB, Ebert D, Salinas Y, Pradhan A, Lehane AM, Myrand-Lapierre ME, O'Loughlin KG, Shackleford DM, Justino de Almeida M, Carrillo AK, Clark JA, Dennis AS, Diep J, Deng X, Duffy S, Endsley AN, Fedewa G, Guiguemde WA, Gómez MG, Holbrook G, Horst J, Kim CC, Liu J, Lee MC, Matheny A, Martínez MS, Miller G, Rodríguez-Alejandre A, Sanz L, Sigal M, Spillman NJ, Stein PD, Wang Z, Zhu F, Waterson D, Knapp S, Shelat A, Avery VM, Fidock DA, Gamo FJ, Charman SA, Mirsalis JC, Ma H, Ferrer S, Kirk K, Angulo-Barturen I, Kyle DE, DeRisi JL, Floyd DM, Guy RK.

Proc Natl Acad Sci U S A. 2014 Dec 16;111(50):E5455-62. doi: 10.1073/pnas.1414221111. Epub 2014 Dec 1. Erratum in: Proc Natl Acad Sci U S A. 2015 Oct 20;112(42):E5764.

29.

Pyrazoleamide compounds are potent antimalarials that target Na+ homeostasis in intraerythrocytic Plasmodium falciparum.

Vaidya AB, Morrisey JM, Zhang Z, Das S, Daly TM, Otto TD, Spillman NJ, Wyvratt M, Siegl P, Marfurt J, Wirjanata G, Sebayang BF, Price RN, Chatterjee A, Nagle A, Stasiak M, Charman SA, Angulo-Barturen I, Ferrer S, Belén Jiménez-Díaz M, Martínez MS, Gamo FJ, Avery VM, Ruecker A, Delves M, Kirk K, Berriman M, Kortagere S, Burrows J, Fan E, Bergman LW.

Nat Commun. 2014 Nov 25;5:5521. doi: 10.1038/ncomms6521.

30.

Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans.

Malmquist NA, Sundriyal S, Caron J, Chen P, Witkowski B, Menard D, Suwanarusk R, Renia L, Nosten F, Jiménez-Díaz MB, Angulo-Barturen I, Santos Martínez M, Ferrer S, Sanz LM, Gamo FJ, Wittlin S, Duffy S, Avery VM, Ruecker A, Delves MJ, Sinden RE, Fuchter MJ, Scherf A.

Antimicrob Agents Chemother. 2015 Feb;59(2):950-9. doi: 10.1128/AAC.04419-14. Epub 2014 Nov 24.

31.

N-aryl-2-aminobenzimidazoles: novel, efficacious, antimalarial lead compounds.

Ramachandran S, Hameed P S, Srivastava A, Shanbhag G, Morayya S, Rautela N, Awasthy D, Kavanagh S, Bharath S, Reddy J, Panduga V, Prabhakar KR, Saralaya R, Nanduri R, Raichurkar A, Menasinakai S, Achar V, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Waterson D, Lee MC, Coburn-Flynn O, Fidock DA, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK.

J Med Chem. 2014 Aug 14;57(15):6642-52. doi: 10.1021/jm500715u. Epub 2014 Jul 21.

PMID:
25007124
32.

Case Study of Small Molecules As Antimalarials: 2-Amino-1-phenylethanol (APE) Derivatives.

Chaparro MJ, Vidal J, Angulo-Barturen I, Bueno JM, Burrows J, Cammack N, Castañeda P, Colmenarejo G, Coterón JM, de Las Heras L, Fernández E, Ferrer S, Gabarró R, Gamo FJ, García M, Jiménez-Díaz MB, Lafuente MJ, León ML, Martínez MS, Minick D, Prats S, Puente M, Rueda L, Sandoval E, Santos-Villarejo A, Witty M, Calderón F.

ACS Med Chem Lett. 2014 Mar 26;5(6):657-61. doi: 10.1021/ml500015r. eCollection 2014 Jun 12.

33.

Aminoazabenzimidazoles, a novel class of orally active antimalarial agents.

Hameed P S, Chinnapattu M, Shanbag G, Manjrekar P, Koushik K, Raichurkar A, Patil V, Jatheendranath S, Rudrapatna SS, Barde SP, Rautela N, Awasthy D, Morayya S, Narayan C, Kavanagh S, Saralaya R, Bharath S, Viswanath P, Mukherjee K, Bandodkar B, Srivastava A, Panduga V, Reddy J, Prabhakar KR, Sinha A, Jiménez-Díaz MB, Martínez MS, Angulo-Barturen I, Ferrer S, Sanz LM, Gamo FJ, Duffy S, Avery VM, Magistrado PA, Lukens AK, Wirth DF, Waterson D, Balasubramanian V, Iyer PS, Narayanan S, Hosagrahara V, Sambandamurthy VK, Ramachandran S.

J Med Chem. 2014 Jul 10;57(13):5702-13. doi: 10.1021/jm500535j. Epub 2014 Jun 24.

PMID:
24914738
34.

Antimalarial drug resistance: new treatments options for Plasmodium.

Gamo FJ.

Drug Discov Today Technol. 2014 Mar;11:81-88. doi: 10.1016/j.ddtec.2014.03.002. Review.

PMID:
24847657
35.

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.

36.

A new in vivo screening paradigm to accelerate antimalarial drug discovery.

Jiménez-Díaz MB, Viera S, Ibáñez J, Mulet T, Magán-Marchal N, Garuti H, Gómez V, Cortés-Gil L, Martínez A, Ferrer S, Fraile MT, Calderón F, Fernández E, Shultz LD, Leroy D, Wilson DM, García-Bustos JF, Gamo FJ, Angulo-Barturen I.

PLoS One. 2013 Jun 25;8(6):e66967. doi: 10.1371/journal.pone.0066967. Print 2013.

37.

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
38.

Quinolone-3-diarylethers: a new class of antimalarial drug.

Nilsen A, LaCrue AN, White KL, Forquer IP, Cross RM, Marfurt J, Mather MW, Delves MJ, Shackleford DM, Saenz FE, Morrisey JM, Steuten J, Mutka T, Li Y, Wirjanata G, Ryan E, Duffy S, Kelly JX, Sebayang BF, Zeeman AM, Noviyanti R, Sinden RE, Kocken CHM, Price RN, Avery VM, Angulo-Barturen I, Jiménez-Díaz MB, Ferrer S, Herreros E, Sanz LM, Gamo FJ, Bathurst I, Burrows JN, Siegl P, Guy RK, Winter RW, Vaidya AB, Charman SA, Kyle DE, Manetsch R, Riscoe MK.

Sci Transl Med. 2013 Mar 20;5(177):177ra37. doi: 10.1126/scitranslmed.3005029.

39.

Antimalarial drug discovery: recent progress and future directions.

Calderón F, Wilson DM, Gamo FJ.

Prog Med Chem. 2013;52:97-151. doi: 10.1016/B978-0-444-62652-3.00003-X. Review. No abstract available.

PMID:
23384667
40.

Exploration of 4(1H)-pyridones as a novel family of potent antimalarial inhibitors of the plasmodial cytochrome bc1.

Bueno JM, Herreros E, Angulo-Barturen I, Ferrer S, Fiandor JM, Gamo FJ, Gargallo-Viola D, Derimanov G.

Future Med Chem. 2012 Dec;4(18):2311-23. doi: 10.4155/fmc.12.177. Review.

PMID:
23234553
41.

Antimalarial drug resistance and early drug discovery.

Garcia-Bustos JF, Gamo FJ.

Curr Pharm Des. 2013;19(2):270-81. Review.

PMID:
22973885
42.

Discovery and biochemical characterization of Plasmodium thioredoxin reductase inhibitors from an antimalarial set.

Theobald AJ, Caballero I, Coma I, Colmenarejo G, Cid C, Gamo FJ, Hibbs MJ, Bass AL, Thomas DA.

Biochemistry. 2012 Jun 12;51(23):4764-71. doi: 10.1021/bi3005076. Epub 2012 Jun 1.

PMID:
22612231
43.

A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold.

Calderón F, Vidal-Mas J, Burrows J, de la Rosa JC, Jiménez-Díaz MB, Mulet T, Prats S, Solana J, Witty M, Gamo FJ, Fernández E.

ACS Med Chem Lett. 2012 Feb 9;3(5):373-7. doi: 10.1021/ml300008j. eCollection 2012 May 10.

44.

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.

45.

P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action.

Sanz LM, Crespo B, De-Cózar C, Ding XC, Llergo JL, Burrows JN, García-Bustos JF, Gamo FJ.

PLoS One. 2012;7(2):e30949. doi: 10.1371/journal.pone.0030949. Epub 2012 Feb 23.

46.

Global phenotypic screening for antimalarials.

Guiguemde WA, Shelat AA, Garcia-Bustos JF, Diagana TT, Gamo FJ, Guy RK.

Chem Biol. 2012 Jan 27;19(1):116-29. doi: 10.1016/j.chembiol.2012.01.004. Review.

47.

Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.

Zhang YK, Plattner JJ, Freund YR, Easom EE, Zhou Y, Ye L, Zhou H, Waterson D, Gamo FJ, Sanz LM, Ge M, Li Z, Li L, Wang H, Cui H.

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1299-307. doi: 10.1016/j.bmcl.2011.12.096. Epub 2011 Dec 28.

PMID:
22243961
48.

Identification and validation of tetracyclic benzothiazepines as Plasmodium falciparum cytochrome bc1 inhibitors.

Dong CK, Urgaonkar S, Cortese JF, Gamo FJ, Garcia-Bustos JF, Lafuente MJ, Patel V, Ross L, Coleman BI, Derbyshire ER, Clish CB, Serrano AE, Cromwell M, Barker RH Jr, Dvorin JD, Duraisingh MT, Wirth DF, Clardy J, Mazitschek R.

Chem Biol. 2011 Dec 23;18(12):1602-10. doi: 10.1016/j.chembiol.2011.09.016.

49.

Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS).

Rueda L, Castellote I, Castro-Pichel J, Chaparro MJ, de la Rosa JC, Garcia-Perez A, Gordo M, Jimenez-Diaz MB, Kessler A, Macdonald SJ, Martinez MS, Sanz LM, Gamo FJ, Fernandez E.

ACS Med Chem Lett. 2011 Aug 29;2(11):840-4. doi: 10.1021/ml2001517. eCollection 2011 Nov 10.

50.

An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS.

Calderón F, Barros D, Bueno JM, Coterón JM, Fernández E, Gamo FJ, Lavandera JL, León ML, Macdonald SJ, Mallo A, Manzano P, Porras E, Fiandor JM, Castro J.

ACS Med Chem Lett. 2011 Aug 3;2(10):741-6. doi: 10.1021/ml200135p. eCollection 2011 Oct 13.

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