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Optimization and Characterization of N-Acetamide Indoles as Antimalarials That Target PfATP4. J Med Chem. 2025 Apr 24; 68(8):8933-8966.
Awalt JK, Ooi ZK, Ashton TD, Mansouri M, Calic PPS, Zhou Q, Vasanthan S, Lee S, Loi K, Jarman KE, Penington JS, Qiu D, Zhang X, Lehane AM, Mao EY, Gancheva MR, Wilson DW, Giannangelo C, MacRaild CA, Creek DJ, Yeo T, Sheth T, Fidock DA, Churchyard A, Baum J, Famodimu MT, Delves MJ, Kristan M, Stewart L, Sutherland CJ, Coyle R, Jagoe H, Lee MCS, Chowdury M, de Koning-Ward TF, Baud D, Brand S, Jackson PF, Cowman AF, Dans MG, Sleebs BE. PMID: 40228810; PMCID: PMC12035806.
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HumansAnimals
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Lactam Truncation Yields a Dihydroquinazolinone Scaffold with Potent Antimalarial Activity that Targets PfATP4. ChemMedChem. 2024 Dec 16; 19(24):e202400549.
Ashton TD, Calic PPS, Dans MG, Kang Ooi Z, Zhou Q, Loi K, Jarman KE, Palandri J, Qiu D, Lehane AM, Maity B, De N, Famodimu MT, Delves MJ, Mao EY, Gancheva MR, Wilson DW, Chowdury M, de Koning-Ward TF, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE. PMID: 39210733; PMCID: PMC11648822.
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HumansAnimalsCells
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Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b. Eur J Med Chem. 2024 Dec 15; 280:116921.
Awalt JK, Su W, Nguyen W, Loi K, Jarman KE, Penington JS, Ramesh S, Fairhurst KJ, Yeo T, Park H, Uhlemann AC, Chandra Maity B, De N, Mukherjee P, Chakraborty A, Churchyard A, Famodimu MT, Delves MJ, Baum J, Mittal N, Winzeler EA, Papenfuss AT, Chowdury M, de Koning-Ward TF, Maier AG, van Dooren GG, Baud D, Brand S, Fidock DA, Jackson PF, Cowman AF, Dans MG, Sleebs BE. PMID: 39388903; PMCID: PMC11609934.
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Property and Activity Refinement of Dihydroquinazolinone-3-carboxamides as Orally Efficacious Antimalarials that Target PfATP4. J Med Chem. 2024 08 22; 67(16):14493-14523.
Ashton TD, Calic PPS, Dans MG, Ooi ZK, Zhou Q, Palandri J, Loi K, Jarman KE, Qiu D, Lehane AM, Maity BC, De N, Giannangelo C, MacRaild CA, Creek DJ, Mao EY, Gancheva MR, Wilson DW, Chowdury M, de Koning-Ward TF, Famodimu MT, Delves MJ, Pollard H, Sutherland CJ, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE. PMID: 39134060; PMCID: PMC11345840.
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Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3. Eur J Med Chem. 2024 Oct 05; 276:116677.
Calic PPS, Ashton TD, Mansouri M, Loi K, Jarman KE, Qiu D, Lehane AM, Roy S, Rao GP, Maity B, Wittlin S, Crespo B, Gamo FJ, Deni I, Fidock DA, Chowdury M, de Koning-Ward TF, Cowman AF, Jackson PF, Baud D, Brand S, Laleu B, Sleebs BE. PMID: 39024967.
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3 Fields:
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Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein. Eur J Med Chem. 2024 Apr 15; 270:116354.
Nguyen W, Boulet C, Dans MG, Loi K, Jarman KE, Watson GM, Tham WH, Fairhurst KJ, Yeo T, Fidock DA, Wittlin S, Chowdury M, de Koning-Ward TF, Chen G, Yan D, Charman SA, Baud D, Brand S, Jackson PF, Cowman AF, Gilson PR, Sleebs BE. PMID: 38554474.
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6 Fields:
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High-throughput phenotypic screen identifies a new family of potent anti-amoebic compounds. PLoS One. 2023; 18(5):e0280232.
Sauvey C, Meewan I, Ehrenkaufer G, Blevitt J, Jackson P, Abagyan R. PMID: 37159460; PMCID: PMC10168566.
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7-N-Substituted-3-oxadiazole Quinolones with Potent Antimalarial Activity Target the Cytochrome bc1 Complex. ACS Infect Dis. 2023 03 10; 9(3):668-691.
Nguyen W, Dans MG, Currie I, Awalt JK, Bailey BL, Lumb C, Ngo A, Favuzza P, Palandri J, Ramesh S, Penington J, Jarman KE, Mukherjee P, Chakraborty A, Maier AG, van Dooren GG, Papenfuss T, Wittlin S, Churchyard A, Baum J, Winzeler EA, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE. PMID: 36853190; PMCID: PMC10012268.
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Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4. J Med Chem. 2023 03 09; 66(5):3540-3565.
Ashton TD, Dans MG, Favuzza P, Ngo A, Lehane AM, Zhang X, Qiu D, Chandra Maity B, De N, Schindler KA, Yeo T, Park H, Uhlemann AC, Churchyard A, Baum J, Fidock DA, Jarman KE, Lowes KN, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE. PMID: 36812492; PMCID: PMC10009754.
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8 Fields:
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Optimisation of 2-(N-phenyl carboxamide) triazolopyrimidine antimalarials with moderate to slow acting erythrocytic stage activity. Bioorg Chem. 2021 10; 115:105244.
Bailey BL, Nguyen W, Ngo A, Goodman CD, Gancheva MR, Favuzza P, Sanz LM, Gamo FJ, Lowes KN, McFadden GI, Wilson DW, Laleu B, Brand S, Jackson PF, Cowman AF, Sleebs BE. PMID: 34452759.
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10 Fields:
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Guided Imagery Improves Mood, Fatigue, and Quality of Life in Individuals With Multiple Sclerosis: An Exploratory Efficacy Trial of Healing Light Guided Imagery. J Evid Based Integr Med. 2018 Jan-Dec; 23:2515690X17748744.
Case LK, Jackson P, Kinkel R, Mills PJ. PMID: 29405761; PMCID: PMC5871039.
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11 Fields:
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Structural Basis of Small-Molecule Aggregate Induced Inhibition of a Protein-Protein Interaction. J Med Chem. 2017 04 27; 60(8):3511-3517.
Blevitt JM, Hack MD, Herman KL, Jackson PF, Krawczuk PJ, Lebsack AD, Liu AX, Mirzadegan T, Nelen MI, Patrick AN, Steinbacher S, Milla ME, Lumb KJ. PMID: 28300404.
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27 Fields:
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Still NAAG'ing After All These Years: The Continuing Pursuit of GCPII Inhibitors. Adv Pharmacol. 2016; 76:215-55.
Vornov JJ, Hollinger KR, Jackson PF, Wozniak KM, Farah MH, Majer P, Rais R, Slusher BS. PMID: 27288079.
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34 Fields:
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JNJ-40255293, a novel adenosine A2A/A1 antagonist with efficacy in preclinical models of Parkinson's disease. ACS Chem Neurosci. 2014 Oct 15; 5(10):1005-19.
Atack JR, Shook BC, Rassnick S, Jackson PF, Rhodes K, Drinkenburg WH, Ahnaou A, Te Riele P, Langlois X, Hrupka B, De Haes P, Hendrickx H, Aerts N, Hens K, Wellens A, Vermeire J, Megens AA. PMID: 25203719.
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Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists. Bioorg Med Chem Lett. 2013 May 01; 23(9):2688-91.
Shook BC, Chakravarty D, Barbay JK, Wang A, Leonard K, Alford V, Powell MT, Rassnick S, Scannevin RH, Carroll K, Wallace N, Crooke J, Ault M, Lampron L, Westover L, Rhodes K, Jackson PF. PMID: 23522563.
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3 Fields:
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Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease. J Med Chem. 2012 Feb 09; 55(3):1402-17.
Shook BC, Rassnick S, Wallace N, Crooke J, Ault M, Chakravarty D, Barbay JK, Wang A, Powell MT, Leonard K, Alford V, Scannevin RH, Carroll K, Lampron L, Westover L, Lim HK, Russell R, Branum S, Wells KM, Damon S, Youells S, Li X, Beauchamp DA, Rhodes K, Jackson PF. PMID: 22239465.
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11 Fields:
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Animals