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514 results

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Page 1
Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance.
Kirkman LA, Zhan W, Visone J, Dziedziech A, Singh PK, Fan H, Tong X, Bruzual I, Hara R, Kawasaki M, Imaeda T, Okamoto R, Sato K, Michino M, Alvaro EF, Guiang LF, Sanz L, Mota DJ, Govindasamy K, Wang R, Ling Y, Tumwebaze PK, Sukenick G, Shi L, Vendome J, Bhanot P, Rosenthal PJ, Aso K, Foley MA, Cooper RA, Kafsack B, Doggett JS, Nathan CF, Lin G. Kirkman LA, et al. Among authors: sanz l. Proc Natl Acad Sci U S A. 2018 Jul 17;115(29):E6863-E6870. doi: 10.1073/pnas.1806109115. Epub 2018 Jul 2. Proc Natl Acad Sci U S A. 2018. PMID: 29967165 Free PMC article.
Thousands of chemical starting points for antimalarial lead identification.
Gamo FJ, Sanz LM, Vidal J, de Cozar C, Alvarez E, Lavandera JL, Vanderwall DE, Green DV, Kumar V, Hasan S, Brown JR, Peishoff CE, Cardon LR, Garcia-Bustos JF. Gamo FJ, et al. Nature. 2010 May 20;465(7296):305-10. doi: 10.1038/nature09107. Nature. 2010. PMID: 20485427
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. Zhang YK, et al. Among authors: sanz lm. J Med Chem. 2015 Jul 9;58(13):5344-54. doi: 10.1021/acs.jmedchem.5b00678. Epub 2015 Jun 23. J Med Chem. 2015. PMID: 26067904 Free PMC article.
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. Sonoiki E, et al. Among authors: sanz lm. Nat Commun. 2017 Mar 6;8:14574. doi: 10.1038/ncomms14574. Nat Commun. 2017. PMID: 28262680 Free PMC article.
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. O'Neill PM, et al. Among authors: sanz l. Nat Commun. 2017 May 24;8:15159. doi: 10.1038/ncomms15159. Nat Commun. 2017. PMID: 28537265 Free PMC article.
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. Zhang YK, et al. Among authors: sanz lm. J Med Chem. 2017 Jul 13;60(13):5889-5908. doi: 10.1021/acs.jmedchem.7b00621. Epub 2017 Jun 29. J Med Chem. 2017. PMID: 28635296
Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis.
Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C, Norcross NR, Vinayak S, Anderson M, Brooks CF, Cooper CA, Damerow S, Delves M, Dowers K, Duffy J, Edwards TE, Hallyburton I, Horst BG, Hulverson MA, Ferguson L, Jiménez-Díaz MB, Jumani RS, Lorimer DD, Love MS, Maher S, Matthews H, McNamara CW, Miller P, O'Neill S, Ojo KK, Osuna-Cabello M, Pinto E, Post J, Riley J, Rottmann M, Sanz LM, Scullion P, Sharma A, Shepherd SM, Shishikura Y, Simeons FRC, Stebbins EE, Stojanovski L, Straschil U, Tamaki FK, Tamjar J, Torrie LS, Vantaux A, Witkowski B, Wittlin S, Yogavel M, Zuccotto F, Angulo-Barturen I, Sinden R, Baum J, Gamo FJ, Mäser P, Kyle DE, Winzeler EA, Myler PJ, Wyatt PG, Floyd D, Matthews D, Sharma A, Striepen B, Huston CD, Gray DW, Fairlamb AH, Pisliakov AV, Walpole C, Read KD, Van Voorhis WC, Gilbert IH. Baragaña B, et al. Among authors: sanz lm. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. doi: 10.1073/pnas.1814685116. Epub 2019 Mar 20. Proc Natl Acad Sci U S A. 2019. PMID: 30894487 Free PMC article.
The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance.
Murithi JM, Pascal C, Bath J, Boulenc X, Gnädig NF, Pasaje CFA, Rubiano K, Yeo T, Mok S, Klieber S, Desert P, Jiménez-Díaz MB, Marfurt J, Rouillier M, Cherkaoui-Rbati MH, Gobeau N, Wittlin S, Uhlemann AC, Price RN, Wirjanata G, Noviyanti R, Tumwebaze P, Cooper RA, Rosenthal PJ, Sanz LM, Gamo FJ, Joseph J, Singh S, Bashyam S, Augereau JM, Giraud E, Bozec T, Vermat T, Tuffal G, Guillon JM, Menegotto J, Sallé L, Louit G, Cabanis MJ, Nicolas MF, Doubovetzky M, Merino R, Bessila N, Angulo-Barturen I, Baud D, Bebrevska L, Escudié F, Niles JC, Blasco B, Campbell S, Courtemanche G, Fraisse L, Pellet A, Fidock DA, Leroy D. Murithi JM, et al. Among authors: sanz lm. Sci Transl Med. 2021 Jul 21;13(603):eabg6013. doi: 10.1126/scitranslmed.abg6013. Sci Transl Med. 2021. PMID: 34290058 Free PMC article.
Preclinical characterization and target validation of the antimalarial pantothenamide MMV693183.
de Vries LE, Jansen PAM, Barcelo C, Munro J, Verhoef JMJ, Pasaje CFA, Rubiano K, Striepen J, Abla N, Berning L, Bolscher JM, Demarta-Gatsi C, Henderson RWM, Huijs T, Koolen KMJ, Tumwebaze PK, Yeo T, Aguiar ACC, Angulo-Barturen I, Churchyard A, Baum J, Fernández BC, Fuchs A, Gamo FJ, Guido RVC, Jiménez-Diaz MB, Pereira DB, Rochford R, Roesch C, Sanz LM, Trevitt G, Witkowski B, Wittlin S, Cooper RA, Rosenthal PJ, Sauerwein RW, Schalkwijk J, Hermkens PHH, Bonnert RV, Campo B, Fidock DA, Llinás M, Niles JC, Kooij TWA, Dechering KJ. de Vries LE, et al. Among authors: sanz lm. Nat Commun. 2022 Apr 20;13(1):2158. doi: 10.1038/s41467-022-29688-5. Nat Commun. 2022. PMID: 35444200 Free PMC article.
Cyclopropyl carboxamides, a chemically novel class of antimalarial agents identified in a phenotypic screen.
Sanz LM, Jiménez-Díaz MB, Crespo B, De-Cozar C, Almela MJ, Angulo-Barturen I, Castañeda P, Ibañez J, Fernández EP, Ferrer S, Herreros E, Lozano S, Martínez MS, Rueda L, Burrows JN, García-Bustos JF, Gamo FJ. Sanz LM, et al. Antimicrob Agents Chemother. 2011 Dec;55(12):5740-5. doi: 10.1128/AAC.05188-11. Epub 2011 Oct 3. Antimicrob Agents Chemother. 2011. PMID: 21968362 Free PMC article.
514 results