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Torin 2 Derivative, NCATS-SM3710, Has Potent Multistage Antimalarial Activity through Inhibition of P. falciparum Phosphatidylinositol 4-Kinase (Pf PI4KIIIβ).
Krishnan K, Ziniel P, Li H, Huang X, Hupalo D, Gombakomba N, Guerrero SM, Dotrang T, Lu X, Caridha D, Sternberg AR, Hughes E, Sun W, Bargieri DY, Roepe PD, Sciotti RJ, Wilkerson MD, Dalgard CL, Tawa GJ, Wang AQ, Xu X, Zheng W, Sanderson PE, Huang W, Williamson KC. Krishnan K, et al. Among authors: roepe pd. ACS Pharmacol Transl Sci. 2020 Sep 11;3(5):948-964. doi: 10.1021/acsptsci.0c00078. eCollection 2020 Oct 9. ACS Pharmacol Transl Sci. 2020. PMID: 33073193 Free PMC article.
High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations.
Mott BT, Eastman RT, Guha R, Sherlach KS, Siriwardana A, Shinn P, McKnight C, Michael S, Lacerda-Queiroz N, Patel PR, Khine P, Sun H, Kasbekar M, Aghdam N, Fontaine SD, Liu D, Mierzwa T, Mathews-Griner LA, Ferrer M, Renslo AR, Inglese J, Yuan J, Roepe PD, Su XZ, Thomas CJ. Mott BT, et al. Among authors: roepe pd. Sci Rep. 2015 Sep 25;5:13891. doi: 10.1038/srep13891. Sci Rep. 2015. PMID: 26403635 Free PMC article.
Additional PfCRT mutations driven by selective pressure for improved fitness can result in the loss of piperaquine resistance and altered Plasmodium falciparum physiology.
Hagenah LM, Dhingra SK, Small-Saunders JL, Qahash T, Willems A, Schindler KA, Rangel GW, Gil-Iturbe E, Kim J, Akhundova E, Yeo T, Okombo J, Mancia F, Quick M, Roepe PD, Llinás M, Fidock DA. Hagenah LM, et al. Among authors: roepe pd. mBio. 2024 Jan 16;15(1):e0183223. doi: 10.1128/mbio.01832-23. Epub 2023 Dec 7. mBio. 2024. PMID: 38059639 Free PMC article.
130 results