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Page 1
Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome.
Xie SC, Metcalfe RD, Mizutani H, Puhalovich T, Hanssen E, Morton CJ, Du Y, Dogovski C, Huang SC, Ciavarri J, Hales P, Griffin RJ, Cohen LH, Chuang BC, Wittlin S, Deni I, Yeo T, Ward KE, Barry DC, Liu B, Gillett DL, Crespo-Fernandez BF, Ottilie S, Mittal N, Churchyard A, Ferguson D, Aguiar ACC, Guido RVC, Baum J, Hanson KK, Winzeler EA, Gamo FJ, Fidock DA, Baud D, Parker MW, Brand S, Dick LR, Griffin MDW, Gould AE, Tilley L. Xie SC, et al. Among authors: mittal n. Proc Natl Acad Sci U S A. 2021 Sep 28;118(39):e2107213118. doi: 10.1073/pnas.2107213118. Proc Natl Acad Sci U S A. 2021. PMID: 34548400 Free PMC article.
Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity.
Vanaerschot M, Murithi JM, Pasaje CFA, Ghidelli-Disse S, Dwomoh L, Bird M, Spottiswoode N, Mittal N, Arendse LB, Owen ES, Wicht KJ, Siciliano G, Bösche M, Yeo T, Kumar TRS, Mok S, Carpenter EF, Giddins MJ, Sanz O, Ottilie S, Alano P, Chibale K, Llinás M, Uhlemann AC, Delves M, Tobin AB, Doerig C, Winzeler EA, Lee MCS, Niles JC, Fidock DA. Vanaerschot M, et al. Among authors: mittal n. Cell Chem Biol. 2020 Jul 16;27(7):806-816.e8. doi: 10.1016/j.chembiol.2020.04.001. Epub 2020 Apr 30. Cell Chem Biol. 2020. PMID: 32359426 Free PMC article.
Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-b]pyridines.
Eagon S, Hammill JT, Sigal M, Ahn KJ, Tryhorn JE, Koch G, Belanger B, Chaplan CA, Loop L, Kashtanova AS, Yniguez K, Lazaro H, Wilkinson SP, Rice AL, Falade MO, Takahashi R, Kim K, Cheung A, DiBernardo C, Kimball JJ, Winzeler EA, Eribez K, Mittal N, Gamo FJ, Crespo B, Churchyard A, García-Barbazán I, Baum J, Anderson MO, Laleu B, Guy RK. Eagon S, et al. Among authors: mittal n. J Med Chem. 2020 Oct 22;63(20):11902-11919. doi: 10.1021/acs.jmedchem.0c01152. Epub 2020 Oct 1. J Med Chem. 2020. PMID: 32945666
Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box.
Reader J, van der Watt ME, Taylor D, Le Manach C, Mittal N, Ottilie S, Theron A, Moyo P, Erlank E, Nardini L, Venter N, Lauterbach S, Bezuidenhout B, Horatscheck A, van Heerden A, Spillman NJ, Cowell AN, Connacher J, Opperman D, Orchard LM, Llinás M, Istvan ES, Goldberg DE, Boyle GA, Calvo D, Mancama D, Coetzer TL, Winzeler EA, Duffy J, Koekemoer LL, Basarab G, Chibale K, Birkholtz LM. Reader J, et al. Among authors: mittal n. Nat Commun. 2021 Jan 11;12(1):269. doi: 10.1038/s41467-020-20629-8. Nat Commun. 2021. PMID: 33431834 Free PMC article.
Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in Plasmodium falciparum.
Lawong A, Gahalawat S, Okombo J, Striepen J, Yeo T, Mok S, Deni I, Bridgford JL, Niederstrasser H, Zhou A, Posner B, Wittlin S, Gamo FJ, Crespo B, Churchyard A, Baum J, Mittal N, Winzeler E, Laleu B, Palmer MJ, Charman SA, Fidock DA, Ready JM, Phillips MA. Lawong A, et al. Among authors: mittal n. J Med Chem. 2021 Mar 11;64(5):2739-2761. doi: 10.1021/acs.jmedchem.0c02022. Epub 2021 Feb 23. J Med Chem. 2021. PMID: 33620219 Free PMC article.
PfMFR3: A Multidrug-Resistant Modulator in Plasmodium falciparum.
Rocamora F, Gupta P, Istvan ES, Luth MR, Carpenter EF, Kümpornsin K, Sasaki E, Calla J, Mittal N, Carolino K, Owen E, Llinás M, Ottilie S, Goldberg DE, Lee MCS, Winzeler EA. Rocamora F, et al. Among authors: mittal n. ACS Infect Dis. 2021 Apr 9;7(4):811-825. doi: 10.1021/acsinfecdis.0c00676. Epub 2021 Mar 14. ACS Infect Dis. 2021. PMID: 33715347 Free PMC article.
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
Palmer MJ, Deng X, Watts S, Krilov G, Gerasyuto A, Kokkonda S, El Mazouni F, White J, White KL, Striepen J, Bath J, Schindler KA, Yeo T, Shackleford DM, Mok S, Deni I, Lawong A, Huang A, Chen G, Wang W, Jayaseelan J, Katneni K, Patil R, Saunders J, Shahi SP, Chittimalla R, Angulo-Barturen I, Jiménez-Díaz MB, Wittlin S, Tumwebaze PK, Rosenthal PJ, Cooper RA, Aguiar ACC, Guido RVC, Pereira DB, Mittal N, Winzeler EA, Tomchick DR, Laleu B, Burrows JN, Rathod PK, Fidock DA, Charman SA, Phillips MA. Palmer MJ, et al. Among authors: mittal n. J Med Chem. 2021 May 13;64(9):6085-6136. doi: 10.1021/acs.jmedchem.1c00173. Epub 2021 Apr 20. J Med Chem. 2021. PMID: 33876936 Free PMC article.
Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention.
Summers RL, Pasaje CFA, Pisco JP, Striepen J, Luth MR, Kumpornsin K, Carpenter EF, Munro JT, Lin D, Plater A, Punekar AS, Shepherd AM, Shepherd SM, Vanaerschot M, Murithi JM, Rubiano K, Akidil A, Ottilie S, Mittal N, Dilmore AH, Won M, Mandt REK, McGowen K, Owen E, Walpole C, Llinás M, Lee MCS, Winzeler EA, Fidock DA, Gilbert IH, Wirth DF, Niles JC, Baragaña B, Lukens AK. Summers RL, et al. Among authors: mittal n. Cell Chem Biol. 2022 Feb 17;29(2):191-201.e8. doi: 10.1016/j.chembiol.2021.07.010. Epub 2021 Aug 3. Cell Chem Biol. 2022. PMID: 34348113 Free PMC article.
Semi-Synthetic Analogues of Cryptolepine as a Potential Source of Sustainable Drugs for the Treatment of Malaria, Human African Trypanosomiasis, and Cancer.
Abacha YZ, Forkuo AD, Gbedema SY, Mittal N, Ottilie S, Rocamora F, Winzeler EA, van Schalkwyk DA, Kelly JM, Taylor MC, Reader J, Birkholtz LM, Lisgarten DR, Cockcroft JK, Lisgarten JN, Palmer RA, Talbert RC, Shnyder SD, Wright CW. Abacha YZ, et al. Among authors: mittal n. Front Pharmacol. 2022 Apr 26;13:875647. doi: 10.3389/fphar.2022.875647. eCollection 2022. Front Pharmacol. 2022. PMID: 35600849 Free PMC article.
The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages.
Arendse LB, Murithi JM, Qahash T, Pasaje CFA, Godoy LC, Dey S, Gibhard L, Ghidelli-Disse S, Drewes G, Bantscheff M, Lafuente-Monasterio MJ, Fienberg S, Wambua L, Gachuhi S, Coertzen D, van der Watt M, Reader J, Aswat AS, Erlank E, Venter N, Mittal N, Luth MR, Ottilie S, Winzeler EA, Koekemoer LL, Birkholtz LM, Niles JC, Llinás M, Fidock DA, Chibale K. Arendse LB, et al. Among authors: mittal n. Sci Transl Med. 2022 Oct 19;14(667):eabo7219. doi: 10.1126/scitranslmed.abo7219. Epub 2022 Oct 19. Sci Transl Med. 2022. PMID: 36260689 Free PMC article.
625 results