Search Results - "Frearson, Julie A"

Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay by DE RYCKER, Manu, HALLYBURTON, Irene, FAIRLAMB, Alan H, GRAY, David W, THOMAS, John, CAMPBELL, Lorna, WYLLIE, Susan, JOSHI, Dhananjay, CAMERON, Scott, GILBERT, Ian H, WYATT, Paul G, FREARSON, Julie A

“…OA  Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Finding new hits in neglected disease projects: target or phenotypic based screening? by Gilbert, Ian H, Leroy, Didier, Frearson, Julie A

“…In this article, we discuss the merits of both target-based and phenotypic screening strategies to find starting points for drug discovery projects in…”
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One Scaffold, Three Binding Modes: Novel and Selective Pteridine Reductase 1 Inhibitors Derived from Fragment Hits Discovered by Virtual Screening by Mpamhanga, Chidochangu P, Spinks, Daniel, Tulloch, Lindsay B, Shanks, Emma J, Robinson, David A, Collie, Iain T, Fairlamb, Alan H, Wyatt, Paul G, Frearson, Julie A, Hunter, William N, Gilbert, Ian H, Brenk, Ruth

“…The enzyme pteridine reductase 1 (PTR1) is a potential target for new compounds to treat human African trypanosomiasis. A virtual screening campaign for…”
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Screening a protein kinase inhibitor library against Plasmodium falciparum by Hallyburton, Irene, Grimaldi, Raffaella, Woodland, Andrew, Baragaña, Beatriz, Luksch, Torsten, Spinks, Daniel, James, Daniel, Leroy, Didier, Waterson, David, Fairlamb, Alan H, Wyatt, Paul G, Gilbert, Ian H, Frearson, Julie A

“…Protein kinases have been shown to be key drug targets, especially in the area of oncology. It is of interest to explore the possibilities of protein kinases…”
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IspE inhibitors identified by a combination of in silico and in vitro high-throughput screening by Tidten-Luksch, Naomi, Grimaldi, Raffaella, Torrie, Leah S, Frearson, Julie A, Hunter, William N, Brenk, Ruth

“…CDP-ME kinase (IspE) contributes to the non-mevalonate or deoxy-xylulose phosphate (DOXP) pathway for isoprenoid precursor biosynthesis found in many species…”
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Acetazolamide-based fungal chitinase inhibitors by Schüttelkopf, Alexander W., Gros, Ludovic, Blair, David E., Frearson, Julie A., van Aalten, Daan M.F., Gilbert, Ian H.

“…Chitin is an essential structural component of the fungal cell wall. Chitinases are thought to be important for fungal cell wall remodelling, and inhibition of…”
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High-content screening of feeder-free human embryonic stem cells to identify pro-survival small molecules by Andrews, Paul D, Becroft, Melissa, Aspegren, Anders, Gilmour, Jane, James, Martyn J, McRae, Scott, Kime, Robert, Allcock, Robert W, Abraham, Achamma, Jiang, Zhong, Strehl, Raimund, Mountford, Joanne C, Milligan, Graeme, Houslay, Miles D, Adams, David R, Frearson, Julie A

“…The propensity of human embryonic stem cells to die upon enzymatic disaggregation or low-density plating is an obstacle to their isolation and routine use in…”
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Investigation of Trypanothione Reductase as a Drug Target in Trypanosoma brucei by Spinks, Daniel, Shanks, Emma J., Cleghorn, Laura A. T., McElroy, Stuart, Jones, Deuan, James, Daniel, Fairlamb, Alan H., Frearson, Julie A., Wyatt, Paul G., Gilbert, Ian H.

“…There is an urgent need for new drugs for the treatment of tropical parasitic diseases such as human African trypanosomiasis, which is caused by Trypanosoma…”
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Synthesis and Evaluation of 1-(1-(Benzo[b]thiophen-2-yl)cyclohexyl)piperidine (BTCP) Analogues as Inhibitors of Trypanothione Reductase by Patterson, Stephen, Jones, Deuan C., Shanks, Emma J., Frearson, Julie A., Gilbert, Ian H., Wyatt, Paul G., Fairlamb, Alan H.

“…Thirty two analogues of phencyclidine were synthesised and tested as inhibitors of trypanothione reductase (TryR), a potential drug target in trypanosome and…”
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A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N‑Myristoyltransferase Inhibitors by Harrison, Justin R, Brand, Stephen, Smith, Victoria, Robinson, David A, Thompson, Stephen, Smith, Alasdair, Davies, Kenneth, Mok, Ngai, Torrie, Leah S, Collie, Iain, Hallyburton, Irene, Norval, Suzanne, Simeons, Frederick R. C, Stojanovski, Laste, Frearson, Julie A, Brenk, Ruth, Wyatt, Paul G, Gilbert, Ian H, Read, Kevin D

“…Crystallography has guided the hybridization of two series of Trypanosoma brucei N-myristoyltransferase (NMT) inhibitors, leading to a novel highly selective…”
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The Design and Synthesis of Potent and Selective Inhibitors of Trypanosoma brucei Glycogen Synthase Kinase 3 for the Treatment of Human African Trypanosomiasis by Urich, Robert, Grimaldi, Raffaella, Luksch, Torsten, Frearson, Julie A, Brenk, Ruth, Wyatt, Paul G

“…Glycogen synthase kinase 3 (GSK3) is a genetically validated drug target for human African trypanosomiasis (HAT), also called African sleeping sickness. We…”
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HTS and hit finding in academia – from chemical genomics to drug discovery by Frearson, Julie A., Collie, Iain T.

“…The liaison between academia and the pharmaceutical industry was originally served primarily through the scientific literature and limited, specific…”
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Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein Crystallography by Patterson, Stephen, Alphey, Magnus S, Jones, Deuan C, Shanks, Emma J, Street, Ian P, Frearson, Julie A, Wyatt, Paul G, Gilbert, Ian H, Fairlamb, Alan H

“…Trypanothione reductase (TryR) is a genetically validated drug target in the parasite Trypanosoma brucei, the causative agent of human African trypanosomiasis…”
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Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy by Baragaña, Beatriz, Norcross, Neil R, Wilson, Caroline, Porzelle, Achim, Hallyburton, Irene, Grimaldi, Raffaella, Osuna-Cabello, Maria, Norval, Suzanne, Riley, Jennifer, Stojanovski, Laste, Simeons, Frederick R. C, Wyatt, Paul G, Delves, Michael J, Meister, Stephan, Duffy, Sandra, Avery, Vicky M, Winzeler, Elizabeth A, Sinden, Robert E, Wittlin, Sergio, Frearson, Julie A, Gray, David W, Fairlamb, Alan H, Waterson, David, Campbell, Simon F, Willis, Paul, Read, Kevin D, Gilbert, Ian H

“…The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic…”
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Development of a 2,4-Diaminothiazole Series for the Treatment of Human African Trypanosomiasis Highlights the Importance of Static–Cidal Screening of Analogues by Cleghorn, Laura A. T., Wall, Richard J., Albrecht, Sébastien, MacGowan, Stuart A., Norval, Suzanne, De Rycker, Manu, Woodland, Andrew, Spinks, Daniel, Thompson, Stephen, Patterson, Stephen, Corpas Lopez, Victoriano, Dey, Gourav, Collie, Iain T., Hallyburton, Irene, Kime, Robert, Simeons, Frederick R. C., Stojanovski, Laste, Frearson, Julie A., Wyatt, Paul G., Read, Kevin D., Gilbert, Ian H., Wyllie, Susan

“…While treatment options for human African trypanosomiasis (HAT) have improved significantly, there is still a need for new drugs with eradication now a…”
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N -myristoyltransferase inhibitors as new leads to treat sleeping sickness by Cleghorn, Laura A. T, Torrie, Leah S, Frearson, Julie A, Guther, M. Lucia S, Smid, Ondrej, Smith, Deborah F, Stojanovski, Laste, Wilkinson, Anthony J, Wyatt, Paul G, Brannigan, James A, Hui, Raymond, Brand, Stephen, Raimi, Olawale G, Brenk, Ruth, Robinson, David A, Hodgkinson, Michael, Ferguson, Michael A. J, Hallyburton, Irene, Mpamhanga, Chidochangu P, Gilbert, Ian H, McElroy, Stuart P, van Aalten, Daan M. F, Qiu, Wei, Read, Kevin D, Price, Helen P, Fairlamb, Alan H

“…African sleeping sickness or human African trypanosomiasis, caused by Trypanosoma brucei spp., is responsible for ∼30,000 deaths each year. Available…”
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Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis by Jones, Deuan C., Hallyburton, Irene, Stojanovski, Laste, Read, Kevin D., Frearson, Julie A., Fairlamb, Alan H.

“…Phenotypic screening of the LOPAC library identified several potent and selective inhibitors of African trypanosomes. The κ-opioid agonist (+)-U50,488…”
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Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma brucei N‑Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis by Brand, Stephen, Norcross, Neil R, Thompson, Stephen, Harrison, Justin R, Smith, Victoria C, Robinson, David A, Torrie, Leah S, McElroy, Stuart P, Hallyburton, Irene, Norval, Suzanne, Scullion, Paul, Stojanovski, Laste, Simeons, Frederick R. C, van Aalten, Daan, Frearson, Julie A, Brenk, Ruth, Fairlamb, Alan H, Ferguson, Michael A. J, Wyatt, Paul G, Gilbert, Ian H, Read, Kevin D

“…Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatment of human African trypanosomiasis (HAT). From previous…”
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Design and Synthesis of Brain Penetrant Trypanocidal N‑Myristoyltransferase Inhibitors by Bayliss, Tracy, Robinson, David A., Smith, Victoria C., Brand, Stephen, McElroy, Stuart P., Torrie, Leah S., Mpamhanga, Chido, Norval, Suzanne, Stojanovski, Laste, Brenk, Ruth, Frearson, Julie A., Read, Kevin D., Gilbert, Ian H., Wyatt, Paul G.

“…N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human…”
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Target assessment for antiparasitic drug discovery by Frearson, Julie A, Wyatt, Paul G, Gilbert, Ian H, Fairlamb, Alan H

“…Drug discovery is a high-risk, expensive and lengthy process taking at least 12 years and costing upwards of US$500 million per drug to reach the clinic. For…”
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