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Chemoprotective antimalarials identified through quantitative high-throughput screening of Plasmodium blood and liver stage parasites.
Dorjsuren D, Eastman RT, Wicht KJ, Jansen D, Talley DC, Sigmon BA, Zakharov AV, Roncal N, Girvin AT, Antonova-Koch Y, Will PM, Shah P, Sun H, Klumpp-Thomas C, Mok S, Yeo T, Meister S, Marugan JJ, Ross LS, Xu X, Maloney DJ, Jadhav A, Mott BT, Sciotti RJ, Winzeler EA, Waters NC, Campbell RF, Huang W, Simeonov A, Fidock DA. Dorjsuren D, et al. Among authors: jansen d. Sci Rep. 2021 Jan 22;11(1):2121. doi: 10.1038/s41598-021-81486-z. Sci Rep. 2021. PMID: 33483532 Free PMC article.
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: jansen dj. J Med Chem. 2018 Apr 12;61(7):3193-3208. doi: 10.1021/acs.jmedchem.8b00261. Epub 2018 Mar 23. J Med Chem. 2018. PMID: 29537847 Free PMC article.
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Cheng X. Horton JR, et al. Among authors: jansen dj. J Med Chem. 2018 Dec 13;61(23):10588-10601. doi: 10.1021/acs.jmedchem.8b01219. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30392349 Free PMC article.
Small Molecule Inhibitors of Activation-Induced Deaminase Decrease Class Switch Recombination in B Cells.
Alvarez-Gonzalez J, Yasgar A, Maul RW, Rieffer AE, Crawford DJ, Salamango DJ, Dorjsuren D, Zakharov AV, Jansen DJ, Rai G, Marugan J, Simeonov A, Harris RS, Kohli RM, Gearhart PJ. Alvarez-Gonzalez J, et al. Among authors: jansen dj. ACS Pharmacol Transl Sci. 2021 May 7;4(3):1214-1226. doi: 10.1021/acsptsci.1c00064. eCollection 2021 Jun 11. ACS Pharmacol Transl Sci. 2021. PMID: 34151211 Free PMC article.
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds.
Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JSK, Kales SC, Mott BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: jansen dj. Cell Chem Biol. 2016 Jul 21;23(7):769-781. doi: 10.1016/j.chembiol.2016.06.006. Epub 2016 Jul 14. Cell Chem Biol. 2016. PMID: 27427228 Free PMC article.
KDM5 histone demethylases repress immune response via suppression of STING.
Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT, Pohida K, Rai G, Kales SC, Henderson MJ, Hu X, Jadhav A, Maloney DJ, Simeonov A, Zhu S, Iwasaki A, Hall MD, Cheng X, Shadel GS, Yan Q. Wu L, et al. Among authors: jansen dj. PLoS Biol. 2018 Aug 6;16(8):e2006134. doi: 10.1371/journal.pbio.2006134. eCollection 2018 Aug. PLoS Biol. 2018. PMID: 30080846 Free PMC article.
Discovery of a functionally selective ghrelin receptor (GHSR1a) ligand for modulating brain dopamine.
Gross JD, Kim DW, Zhou Y, Jansen D, Slosky LM, Clark NB, Ray CR, Hu X, Southall N, Wang A, Xu X, Barnaeva E, Wetsel WC, Ferrer M, Marugan JJ, Caron MG, Barak LS, Toth K. Gross JD, et al. Among authors: jansen d. Proc Natl Acad Sci U S A. 2022 Mar 8;119(10):e2112397119. doi: 10.1073/pnas.2112397119. Epub 2022 Mar 3. Proc Natl Acad Sci U S A. 2022. PMID: 35239443 Free PMC article.
KDM5B Promotes Drug Resistance by Regulating Melanoma-Propagating Cell Subpopulations.
Liu X, Zhang SM, McGeary MK, Krykbaeva I, Lai L, Jansen DJ, Kales SC, Simeonov A, Hall MD, Kelly DP, Bosenberg MW, Yan Q. Liu X, et al. Among authors: jansen dj. Mol Cancer Ther. 2019 Mar;18(3):706-717. doi: 10.1158/1535-7163.MCT-18-0395. Epub 2018 Dec 6. Mol Cancer Ther. 2019. PMID: 30523048 Free PMC article.
426 results