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Page 1
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: angulo barturen i. J Med Chem. 2024 Dec 22. doi: 10.1021/acs.jmedchem.4c02394. Online ahead of print. J Med Chem. 2024. PMID: 39710971
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: angulo barturen i. 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: angulo barturen i. 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: angulo barturen i. 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.
Determination of the Pharmacokinetics and Pharmacodynamics of Isoniazid, Rifampicin, Pyrazinamide and Ethambutol in a Cross-Over Cynomolgus Macaque Model of Mycobacterium tuberculosis Infection.
Sibley L, White AD, Sarfas C, Gullick J, Gleeson F, Lanni F, Clark S, Rayner E, Ferrer-Bazaga S, Ortega-Muro F, Alameda L, Rullas J, Sousa V, Martinez M, Angulo-Barturen I, Garcia A, Vaquero JJ, Pertinez HE, Davies G, Dennis M, Williams A, Sharpe S. Sibley L, et al. Among authors: angulo barturen i. Pharmaceutics. 2022 Nov 30;14(12):2666. doi: 10.3390/pharmaceutics14122666. Pharmaceutics. 2022. PMID: 36559163 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: angulo barturen i. 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.
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: angulo barturen i. 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.
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: angulo barturen i. Nat Commun. 2022 Apr 20;13(1):2158. doi: 10.1038/s41467-022-29688-5. Nat Commun. 2022. PMID: 35444200 Free PMC article.
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Taft BR, Yokokawa F, Kirrane T, Mata AC, Huang R, Blaquiere N, Waldron G, Zou B, Simon O, Vankadara S, Chan WL, Ding M, Sim S, Straimer J, Guiguemde A, Lakshminarayana SB, Jain JP, Bodenreider C, Thompson C, Lanshoeft C, Shu W, Fang E, Qumber J, Chan K, Pei L, Chen YL, Schulz H, Lim J, Abas SN, Ang X, Liu Y, Angulo-Barturen I, Jiménez-Díaz MB, Gamo FJ, Crespo-Fernandez B, Rosenthal PJ, Cooper RA, Tumwebaze P, Aguiar ACC, Campo B, Campbell S, Wagner J, Diagana TT, Sarko C. Taft BR, et al. Among authors: angulo barturen i. J Med Chem. 2022 Mar 10;65(5):3798-3813. doi: 10.1021/acs.jmedchem.1c01995. Epub 2022 Mar 1. J Med Chem. 2022. PMID: 35229610 Free PMC article.
84 results