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Keywords: drug discovery
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Articles
Biochem Soc Trans (2021) 49 (4): 1723–1734.
Published: 25 August 2021
... 2021 28 7 2021 30 7 2021 © 2021 The Author(s). Published by Portland Press Limited on behalf of the Biochemical Society 2021 chemical biology drug discovery protein tyrosine phosphatase Post-translational phosphorylation of tyrosine residues regulates a wide variety...
Articles
Biochem Soc Trans (2021) 49 (4): 1881–1890.
Published: 16 August 2021
... and scope of implementing OoCs across the drug discovery process are also discussed. Correspondence: Augustin Amour ( augustin.j.amour@gsk.com ) 21 6 2021 20 7 2021 26 7 2021 © 2021 The Author(s) 2021 This is an open access article published by Portland Press Limited...
Articles
Biochem Soc Trans (2019) 47 (1): 281–293.
Published: 15 January 2019
...Tom Ceska; Chun-Wa Chung; Rob Cooke; Chris Phillips; Pamela A. Williams The impact of structural biology on drug discovery is well documented, and the workhorse technique for the past 30 years or so has been X-ray crystallography. With the advent of several technological improvements, including...
Articles
Biochem Soc Trans (2019) 47 (1): 63–76.
Published: 21 December 2018
... considerable resources for follow-up activities in a drug discovery project. To simplify this validation process, a graphical scheme — the validation cross — can be used. This simple graphic is a powerful tool for identifying blind spots of a binding hypothesis, for selecting the most informative combination...
Articles
Biochem Soc Trans (2019) 47 (1): 47–61.
Published: 17 December 2018
...–function relationships. Today, this information is vital to drug discovery and medicine. In the last two decades, many have been the technical advances and breakthroughs in the field of MP structural biology that have contributed to an exponential growth in the number of unique MP structures in the Protein...
Articles
Biochem Soc Trans (2016) 44 (2): 555–561.
Published: 11 April 2016
...Richard Carr, III; Jeffrey L. Benovic For over a decade, pepducins have been utilized to develop unique pharmacological profiles that have been particularly challenging for traditional drug discovery methods. It is becoming increasingly clear that these cell-penetrating lipopeptides can access...
Articles
Biochem Soc Trans (2015) 43 (4): 674–679.
Published: 03 August 2015
...-associated protein 1 (Keap1) drug discovery nuclear factor erytheroid-2-related factor 2 (Nrf2) protein–protein interactions Small molecule inducers of the transcription factor nuclear factor erythroid-2-related factor 2 (Nrf2) have been proposed as potential therapeutic agents in a wide range...
Articles
Biochem Soc Trans (2013) 41 (4): 1037–1041.
Published: 18 July 2013
... and of phosphorylation. Knowledge of kinase-specific mechanisms of activation can be exploited in drug discovery. In the case of Aurora-A, the flexibility of the activation loop shown in the unphosphorylated kinase has been exploited in the design of kinase inhibitors that bind an inactive conformation in which...
Articles
Biochem Soc Trans (2012) 40 (3): 573–579.
Published: 22 May 2012
.... In the present paper, we review recent genomic and biochemical evidence implicating Mycobacterium tuberculosis CYP (cytochrome P450) enzymes as exciting potential targets for new classes of anti-tuberculars. We also discuss HTS (high-throughput screening) and fragment-based drug-discovery campaigns...
Articles
Biochem Soc Trans (2012) 40 (1): 31–36.
Published: 19 January 2012
... 2012 autotaxin cancer drug discovery lysophosphatidic acid (LPA) 4-pentadecylbenzylphosphonic acid (4-PBA) therapy ATX (autotaxin) is a member of the NPP (nucleotide pyrophosphatase/phosphodiesterase) enzyme family and is also known as NPP2 [ 1 , 2 ]. ATX was originally identified...
Articles
Biochem Soc Trans (2011) 39 (5): 1365–1370.
Published: 21 September 2011
... relationship) data, which can be used to support chemical biology, lead discovery and target selection in drug discovery. The database contains the abstracted structures, properties and biological activities for over 700000 distinct compounds and in excess of more than 3 million bioactivity records abstracted...
Articles
Biochem Soc Trans (2010) 38 (4): 1033–1036.
Published: 26 July 2010
...Claire N. Medine; Sebastian Greenhough; David C. Hay Accurate prediction of human drug toxicity is a vital part of the drug discovery process. However, the safety evaluation process is hindered by the availability and quality of primary human liver models with which to study drug toxicity...
Articles
Biochem Soc Trans (2010) 38 (4): 1046–1050.
Published: 26 July 2010
... chemical category affect cell phenotype in a similar way and that it was possible to streamline assignment of a compound to a chemical category on the basis of measured cellular features. Modern drug discovery is limited by the lack of suitable models for primary screens. The paradigm of using...
Articles
Biochem Soc Trans (2010) 38 (4): 1072–1075.
Published: 26 July 2010
...Daniel J. Maltman; Stefan A. Przyborski Drug discovery programmes require accurate in vitro systems for drug screening and testing. Traditional cell culture makes use of 2D (two-dimensional) surfaces for ex vivo cell growth. In such environments, cells are forced to adopt unnatural characteristics...
Articles
Biochem Soc Trans (2007) 35 (5): 985–990.
Published: 25 October 2007
...D.A. Middleton Structure-based design has gained credibility as a valuable component of the modern drug discovery process. The technique of SSNMR (solid-state NMR) promises to be a useful counterpart to the conventional experimental techniques of X-ray crystallography and solution-state NMR...
Articles
Biochem Soc Trans (2006) 34 (2): 313–316.
Published: 20 March 2006
...G.P. Belfield; S.J. Delaney The discipline of molecular biology has become increasingly important in recent times for the process of drug discovery. We describe the impact of molecular biology across the whole process of drug discovery and development, including (i) the identification...
Articles
Biochem Soc Trans (2006) 34 (2): 238–242.
Published: 20 March 2006
...J.G. McCormack Scientists and science in the pharmaceutical industry rely heavily on the more academically orientated basic research carried out at Universities, for first of all training, but also as a source of new ideas and approaches to drug discovery. Progress in the discovery and development...
Articles
Biochem Soc Trans (2005) 33 (4): 553–558.
Published: 01 August 2005
... © 2005 The Biochemical Society 2005 Alzheimer's disease amyloid drug discovery immunization protease secretase AD (Alzheimer's disease) is a progressive, degenerative brain disorder resulting in cognitive and behavioural decline and is the leading cause of dementia in the Western...
Articles
Biochem Soc Trans (2005) 33 (1): 306–310.
Published: 01 February 2005
...’. The case of GK research illustrates how basic science may culminate in therapeutic advances of human medicine. drug discovery genetics glucose glucokinase glucose homeostasis therapeutics The tenets of the GK glucose sensor concept received their proof from the biochemical genetic...
Articles
Biochem Soc Trans (2004) 32 (5): 873–877.
Published: 26 October 2004
... interaction drug discovery G-protein-coupled receptor kinetics ternary complex model The GPCRs (G-protein-coupled receptors) are the largest receptor superfamily and are extremely tractable drug targets. Traditional approaches to drug discovery at GPCRs focus on mimicking or inhibiting the actions...
Articles
Biochem Soc Trans (2003) 31 (3): 631–633.
Published: 01 June 2003
...B.A. Wallace; Robert W. Janes CD spectroscopy is an established and valuable technique for examining protein structure, dynamics and folding. Because of its ability to sensitively detect conformational changes, it has important potential for drug discovery, enabling screening for ligand and drug...