|A Crystallographic-Based Fragment Screen Against Human BRD4 Bromodomain 1|
Hubbard P, Ritchie A, Hughes S, Lipkin M, Blackaby W & MacLeod A
Fragment-based drug discovery has now become firmly established as an important method in the lead discovery process, and is an integral component of drug discovery at BioFocus. Using a selection of compounds from our fragment collection, we have performed a crystallographic-based screen against human BRD4 bromodomain 1.
|Application of the SoftFocus® Design Strategy to Epigenetics Targets|
Sheppard D, Macritchie J, Allen V & Hughes S
Epigenetics describes the regulation of gene expression that occurs through DNA methylation and post translational modification of histones. The pharmaceutical industry has shown an explosion of interest in this field with new targets emerging.
|Fragmentor: A New Technique to Facilitate Scaffold Design for Library Generation|
Sheppard D, Macritchie J & Allen V
The requirement for novel starting points to ignite drug discovery projects is always high for emerging targets. Over the past 12 years BioFocus has built an impressive track record for the successful and original design of high quality libraries.
|Novel Antimalarial Drug Candidates Generated In Silico by Analysis of Public HTS Data|
Robert Fraczkiewicz, Michael S. Lawless, Robert D. Clark, and Walter S. Woltosz
This research aims to provide proof-in-principle that in silico tools could be applied to public data so as to efficiently identify active chemistry with good ADMET properties.
|Development of an Automated Platform for HT Cloning and Expression|
Stefano Bonacci; Sara Iozzi; Scilla Buccato; Manuele Martinelli; John Telford; Domenico Maione; Roberto Petracca
Biomolecular protocols covering the whole cloning process were implemented in liquid handler robots. When compared to the manual approach, it was found that automation significantly speeds up HT cloning.
|Metal Polymers, A Glue to Immobilise Proteins Onto Synthetic Surfaces|
Abernethy N, Chung E, Fontanelle BT, Gao Y, Jennins D, Koudijs MM, Lim D, Yang L, Ling T, Vukovic P, Wong A, Maeji, NJ
The main objective of this work was to develop a surface chemistry which maintains protein function and orientation per unit surface area, regardless of the surface used.
|UPLC-MS/MS for the Screening, Confirmation and Quantification of 32 Drugs Illegally Added to Herbal/Dietary Supplements for the Enhancement of Male Sexual Performance|
Salman Azimi, Nayan Mistry and Michelle Wood
This poster outlines development of a novel screening method that is suitable for both the detection of known and unknown ED drugs and analogues. Comprehensive spectral data is collected and automatically compared to a prepared library if known drugs.
|Effect of Liquid Handling Quality Control on Biological Assay Performance|
Nathaniel Hentz, Ph.D and Tanya Knaide
High quality assays are required in order to take forward potential drugs, post screening. Therefore the liquid handling must be accurate and precise, as demonstrated in this experiment.
|Nanoliter Volume Pin Tool Transfers as Measured by a Dual-Dye Absorbance Method|
Duong T. Chau; Patrick H. Cleveland, Ph.D.; John Thomas Bradshaw, Ph.D.
Increasing costs of chemical compounds and commonly used solvents has pushed high throughput screening labs towards lower working volumes, specifically in the nanoliter range. The ability to controllably dispense “known” nanoliter aliquots of samples is desired, which can readily be achieved using Pin Tools.