Browsing by Author "LLOYD, DAVID G"
Now showing items 1-7 of 7
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Comprehensive characterization of cytochrome P450 isozyme selectivity across chemical libraries.
LLOYD, DAVID G (Nature Publishing Group, 2009)The cytochrome P450 (CYP) gene family catalyzes drug metabolism and bioactivation and is therefore relevant to drug development. We determined potency values for 17,143 compounds against five recombinant CYP isozymes (1A2, ... -
Identification of Plasmepsin Inhibitors as Selective Antimalarial Agents using Ligand Based Drug Design
DEMPSEY, ENDA; LLOYD, DAVID G; CARTA, GIORGIO; FAYNE, DARREN; BELL, ANGUS (Elsevier, 2011)We describe the application of Ligand Based Virtual Screening technologies towards the discovery of novel Plasmepsin (PM) inhibitors, a family of malarial parasitic aspartyl proteases. Pharmacophore queries were used to ... -
Lead identification of beta-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90
MEEGAN, MARY JANE; ZISTERER, DANIELA MARIA; WILLIAMS, DAVID CLIVE; KNOX, ANDREW; LLOYD, DAVID G; O'BOYLE, NIAMH (Elsevier, 2011)Heat shock protein 90 is an emerging target for oncology therapeutics. Inhibitors of this molecular chaperone, which is responsible for the maintenance of a number of oncogenic proteins, have shown promise in clinical ... -
Lead identification of conformationally restricted ?-lactam type combretastatin analogues: synthesis, antiproliferative activity and tubulin targeting effects
GREENE, LISA; ZISTERER, DANIELA MARIA; MEEGAN, MARY JANE; LLOYD, DAVID G (Elsevier, 2010)The synthesis and study of the structure-activity relationships of a series of rigid analogues of combretastatin A-4 are described which contain the 1,4-diaryl-2-azetidinone (?-lactam) ring system in place of the usual ... -
Murine model of autosomal dominant retinitis pigmentosa generated by targeted deletion at codon 307 of the rds-peripherin gene
FARRAR, JANE; HUMPHRIES, MARIAN; HUMPHRIES, PETER; LLOYD, DAVID G (Oxford University Press, 2002)We introduced a targeted single base deletion at codon 307 of the rds-peripherin gene in mice, similar mutations being known to cause autosomal dominant retinitis pigmentosa (RP) in man. Histopathological and electroretinographic ... -
Rational ligand based drug design and structure-activity relationship studies in the ligand-binding domain of the glucocorticoid receptor ?
FAYNE, DARREN; LLOYD, DAVID G (Future Science, 2009) -
Synthesis, Biochemical and Molecular Modelling Studies of Antiproliferative Azetidinones causing Microtubule Disruption and Mitotic Catastrophe
MEEGAN, MARY JANE; ZISTERER, DANIELA MARIA; KEELY, NIALL O.; MC CABE, THOMAS; GREENE, LISA; KNOX, ANDREW; LLOYD, DAVID G; O'BOYLE, NIAMH (Elsevier, 2011)The structure-activity relationships of antiproliferative ?-lactams, focusing on modifications at the 4-position of the ?-lactam ring, is described. Synthesis of this series of compounds was achieved utilizing the Staudinger ...