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2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy.
Dziwornu GA, Seanego D, Fienberg S, Clements M, Ferreira J, Sypu VS, Samanta S, Bhana AD, Korkor CM, Garnie LF, Teixeira N, Wicht KJ, Taylor D, Olckers R, Njoroge M, Gibhard L, Salomane N, Wittlin S, Mahato R, Chakraborty A, Sevilleno N, Coyle R, Lee MCS, Godoy LC, Pasaje CF, Niles JC, Reader J, van der Watt M, Birkholtz LM, Bolscher JM, de Bruijni MHC, Coulson LB, Basarab GS, Ghorpade SR, Chibale K. Dziwornu GA, et al. Among authors: niles jc. J Med Chem. 2024 Jul 11;67(13):11401-11420. doi: 10.1021/acs.jmedchem.4c01154. Epub 2024 Jun 25. J Med Chem. 2024. PMID: 38918002 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: niles jc. 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.
Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35.
Atack TC, Raymond DD, Blomquist CA, Pasaje CF, McCarren PR, Moroco J, Befekadu HB, Robinson FP, Pal D, Esherick LY, Ianari A, Niles JC, Sellers WR. Atack TC, et al. Among authors: niles jc. ACS Med Chem Lett. 2020 Sep 1;11(11):2131-2138. doi: 10.1021/acsmedchemlett.0c00272. eCollection 2020 Nov 12. ACS Med Chem Lett. 2020. PMID: 33209191 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: niles jc. 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.
Reaction hijacking inhibition of Plasmodium falciparum asparagine tRNA synthetase.
Xie SC, Wang Y, Morton CJ, Metcalfe RD, Dogovski C, Pasaje CFA, Dunn E, Luth MR, Kumpornsin K, Istvan ES, Park JS, Fairhurst KJ, Ketprasit N, Yeo T, Yildirim O, Bhebhe MN, Klug DM, Rutledge PJ, Godoy LC, Dey S, De Souza ML, Siqueira-Neto JL, Du Y, Puhalovich T, Amini M, Shami G, Loesbanluechai D, Nie S, Williamson N, Jana GP, Maity BC, Thomson P, Foley T, Tan DS, Niles JC, Han BW, Goldberg DE, Burrows J, Fidock DA, Lee MCS, Winzeler EA, Griffin MDW, Todd MH, Tilley L. Xie SC, et al. Among authors: niles jc. Res Sq [Preprint]. 2023 Jul 27:rs.3.rs-3198291. doi: 10.21203/rs.3.rs-3198291/v1. Res Sq. 2023. Update in: Nat Commun. 2024 Jan 31;15(1):937. doi: 10.1038/s41467-024-45224-z PMID: 37546892 Free PMC article. Updated. Preprint.
Reaction hijacking inhibition of Plasmodium falciparum asparagine tRNA synthetase.
Xie SC, Wang Y, Morton CJ, Metcalfe RD, Dogovski C, Pasaje CFA, Dunn E, Luth MR, Kumpornsin K, Istvan ES, Park JS, Fairhurst KJ, Ketprasit N, Yeo T, Yildirim O, Bhebhe MN, Klug DM, Rutledge PJ, Godoy LC, Dey S, De Souza ML, Siqueira-Neto JL, Du Y, Puhalovich T, Amini M, Shami G, Loesbanluechai D, Nie S, Williamson N, Jana GP, Maity BC, Thomson P, Foley T, Tan DS, Niles JC, Han BW, Goldberg DE, Burrows J, Fidock DA, Lee MCS, Winzeler EA, Griffin MDW, Todd MH, Tilley L. Xie SC, et al. Among authors: niles jc. Nat Commun. 2024 Jan 31;15(1):937. doi: 10.1038/s41467-024-45224-z. Nat Commun. 2024. PMID: 38297033 Free PMC article.
The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance.
Murithi JM, Deni I, Pasaje CFA, Okombo J, Bridgford JL, Gnädig NF, Edwards RL, Yeo T, Mok S, Burkhard AY, Coburn-Flynn O, Istvan ES, Sakata-Kato T, Gomez-Lorenzo MG, Cowell AN, Wicht KJ, Le Manach C, Kalantarov GF, Dey S, Duffey M, Laleu B, Lukens AK, Ottilie S, Vanaerschot M, Trakht IN, Gamo FJ, Wirth DF, Goldberg DE, Odom John AR, Chibale K, Winzeler EA, Niles JC, Fidock DA. Murithi JM, et al. Among authors: niles jc. Cell Chem Biol. 2022 May 19;29(5):824-839.e6. doi: 10.1016/j.chembiol.2021.06.006. Epub 2021 Jul 6. Cell Chem Biol. 2022. PMID: 34233174 Free PMC article.
MalDA, Accelerating Malaria Drug Discovery.
Yang T, Ottilie S, Istvan ES, Godinez-Macias KP, Lukens AK, Baragaña B, Campo B, Walpole C, Niles JC, Chibale K, Dechering KJ, Llinás M, Lee MCS, Kato N, Wyllie S, McNamara CW, Gamo FJ, Burrows J, Fidock DA, Goldberg DE, Gilbert IH, Wirth DF, Winzeler EA; Malaria Drug Accelerator Consortium. Yang T, et al. Among authors: niles jc. Trends Parasitol. 2021 Jun;37(6):493-507. doi: 10.1016/j.pt.2021.01.009. Epub 2021 Feb 26. Trends Parasitol. 2021. PMID: 33648890 Free PMC article. Review.
69 results