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Page 1
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. Baker DA, et al. Nat Commun. 2017 Sep 5;8(1):430. doi: 10.1038/s41467-017-00572-x. Nat Commun. 2017. PMID: 28874661 Free PMC article.
Chemical genetics of Plasmodium falciparum.
Guiguemde WA, Shelat AA, Bouck D, Duffy S, Crowther GJ, Davis PH, Smithson DC, Connelly M, Clark J, Zhu F, Jiménez-Díaz MB, Martinez MS, Wilson EB, Tripathi AK, Gut J, Sharlow ER, Bathurst I, El Mazouni F, Fowble JW, Forquer I, McGinley PL, Castro S, Angulo-Barturen I, Ferrer S, Rosenthal PJ, Derisi JL, Sullivan DJ, Lazo JS, Roos DS, Riscoe MK, Phillips MA, Rathod PK, Van Voorhis WC, Avery VM, Guy RK. Guiguemde WA, et al. Nature. 2010 May 20;465(7296):311-5. doi: 10.1038/nature09099. Nature. 2010. PMID: 20485428 Free PMC article.
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. Chaparro MJ, et al. ACS Med Chem Lett. 2014 Mar 26;5(6):657-61. doi: 10.1021/ml500015r. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944739 Free PMC article.
Optimized Pyridazinone Nutrient Channel Inhibitors Are Potent and Specific Antimalarial Leads.
Butler MM, Waidyarachchi SL, Shao J, Nguyen ST, Ding X, Cardinale SC, Morin LR, Kwasny SM, Ito M, Gezelle J, Jiménez-Díaz MB, Angulo-Barturen I, Jacobs RT, Burrows JN, Aron ZD, Bowlin TL, Desai SA. Butler MM, et al. Among authors: jimenez diaz mb. Mol Pharmacol. 2022 Sep;102(3):172-182. doi: 10.1124/molpharm.122.000549. Epub 2022 Jul 7. Mol Pharmacol. 2022. PMID: 35798366 Free PMC article.
Structure-Based Discovery and Development of Highly Potent Dihydroorotate Dehydrogenase Inhibitors for Malaria Chemoprevention.
Nie Z, Bonnert R, Tsien J, Deng X, Higgs C, El Mazouni F, Zhang X, Li R, Ho N, Feher V, Paulsen J, Shackleford DM, Katneni K, Chen G, Ng ACF, McInerney M, Wang W, Saunders J, Collins D, Yan D, Li P, Campbell M, Patil R, Ghoshal A, Mondal P, Kundu A, Chittimalla R, Mahadeva M, Kokkonda S, White J, Das R, Mukherjee P, Angulo-Barturen I, Jiménez-Díaz MB, Malmstrom R, Lawrenz M, Rodriguez-Granillo A, Rathod PK, Tomchick DR, Palmer MJ, Laleu B, Qin T, Charman SA, Phillips MA. Nie Z, et al. Among authors: jimenez diaz mb. J Med Chem. 2025 Jan 9;68(1):590-637. doi: 10.1021/acs.jmedchem.4c02394. Epub 2024 Dec 22. J Med Chem. 2025. PMID: 39710971 Free PMC article.
Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria.
Lawong A, Gahalawat S, Ray S, Ho N, Han Y, Ward KE, Deng X, Chen Z, Kumar A, Xing C, Hosangadi V, Fairhurst KJ, Tashiro K, Liszczak G, Shackleford DM, Katneni K, Chen G, Saunders J, Crighton E, Casas A, Robinson JJ, Imlay LS, Zhang X, Lemoff A, Zhao Z, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Campbell SF, Fidock DA, Laleu B, Charman SA, Ready JM, Phillips MA. Lawong A, et al. Among authors: jimenez diaz mb. Cell Chem Biol. 2024 Aug 15;31(8):1503-1517.e19. doi: 10.1016/j.chembiol.2024.07.001. Epub 2024 Jul 30. Cell Chem Biol. 2024. PMID: 39084225
Macrocyclic Peptidomimetic Plasmepsin X Inhibitors with Potent In Vitro and In Vivo Antimalarial Activity.
Kovada V, Withers-Martinez C, Bobrovs R, Ce Rule HN, Liepins E, Grinberga S, Hackett F, Collins CR, Kreicberga A, Jiménez-Díaz MB, Angulo-Barturen I, Rasina D, Suna E, Jaudzems K, Blackman MJ, Jirgensons A. Kovada V, et al. Among authors: jimenez diaz mb. J Med Chem. 2023 Aug 10;66(15):10658-10680. doi: 10.1021/acs.jmedchem.3c00812. Epub 2023 Jul 28. J Med Chem. 2023. PMID: 37505188 Free PMC article.
Predicting Optimal Antimalarial Drug Combinations from a Standardized Plasmodium falciparum Humanized Mouse Model.
Demarta-Gatsi C, Andenmatten N, Jiménez-Díaz MB, Gobeau N, Cherkaoui-Rabti MH, Fuchs A, Díaz P, Berja S, Sánchez R, Gómez H, Ruiz E, Sainz P, Salazar E, Gil-Merino R, Mendoza LM, Eguizabal C, Leroy D, Moehrle JJ, Tornesi B, Angulo-Barturen I. Demarta-Gatsi C, et al. Among authors: jimenez diaz mb. Antimicrob Agents Chemother. 2023 Jun 15;67(6):e0157422. doi: 10.1128/aac.01574-22. Epub 2023 May 3. Antimicrob Agents Chemother. 2023. PMID: 37133382 Free PMC article.
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362.
Lowe MA, Cardenas A, Valentin JP, Zhu Z, Abendroth J, Castro JL, Class R, Delaunois A, Fleurance R, Gerets H, Gryshkova V, King L, Lorimer DD, MacCoss M, Rowley JH, Rosseels ML, Royer L, Taylor RD, Wong M, Zaccheo O, Chavan VP, Ghule GA, Tapkir BK, Burrows JN, Duffey M, Rottmann M, Wittlin S, Angulo-Barturen I, Jiménez-Díaz MB, Striepen J, Fairhurst KJ, Yeo T, Fidock DA, Cowman AF, Favuzza P, Crespo-Fernandez B, Gamo FJ, Goldberg DE, Soldati-Favre D, Laleu B, de Haro T. Lowe MA, et al. Among authors: jimenez diaz mb. J Med Chem. 2022 Oct 27;65(20):14121-14143. doi: 10.1021/acs.jmedchem.2c01336. Epub 2022 Oct 10. J Med Chem. 2022. PMID: 36216349 Free PMC article.
60 results