... is not amenable to high-throughput screening of large chemical libraries limiting its utility in drug discovery ( Figure 1 ). Figure 1. Summary of methods currently utilized for telomerase-based drug discovery. Protein structures are from the Protein Data Bank as follows: Tribolium castaneum TERT [ 47...

... in complexity and unable to self-assemble or regenerate, and thus aren't as advanced as organoids. This terminology has led to some confusion in the field, and here we review both lung spheroids and lung organoids as they are both useful as 3D models. airway modeling drug discovery lung disease modeling...

... for anti-Tb drug development. Correspondence: Zhong-Yin Zhang ( [email protected] ) 3 6 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...

... and scope of implementing OoCs across the drug discovery process are also discussed. Correspondence: Augustin Amour ( [email protected] ) 21 6 2021 20 7 2021 26 7 2021 The use of primary cells, where possible, is an important consideration when replicating in vivo...

...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...

... 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...

...–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...

...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...

... involved in phase II metabolism promotes the formation of conjugated and detoxified products of primary metabolism that contribute to the cytoprotective effects of Nrf2 induction. Kelch-like ECH-associated protein 1 (Keap1) drug discovery nuclear factor erytheroid-2-related factor 2 (Nrf2...

... should be addressed (email [email protected] ). 26 4 2013 © The Authors Journal compilation © 2013 Biochemical Society 2013 activation mechanism Aurora-A drug discovery Nek7 protein kinase structural biology On the basis of measurements of kinase activity and analysis...

.... 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...

... is a logical extension of the juxtacrine signalling concept because one inhibits both targets that are spatially and functionally linked in the cancer cell microenvironment. © The Authors Journal compilation © 2012 Biochemical Society 2012 autotaxin cancer drug discovery lysophosphatidic acid...

... 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...

...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...

... erythroleukaemia cells respectively [ 16 , 17 ]. drug discovery embryonic stem cell high-content screening high-throughput screening induced pluripotent stem cell ES (embryonic stem) cells, obtained from a blastocyst stage embryo [ 1 ], and iPS (induced pluripotent stem) cells, derived by somatic...

...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...

...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...

...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...

...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...

... therapies for the treatment of AD. In this review, we will review a variety of approaches and mechanisms capable of modulating levels of Aβ. 22 3 2005 © 2005 The Biochemical Society 2005 Alzheimer's disease amyloid drug discovery immunization protease secretase AD (Alzheimer's...

...’. The case of GK research illustrates how basic science may culminate in therapeutic advances of human medicine. © 2005 The Biochemical Society 2005 drug discovery genetics glucose glucokinase glucose homeostasis therapeutics 1 To whom correspondence should be addressed (email...

... of the modulators is lacking. allosteric interaction drug discovery G-protein-coupled receptor kinetics ternary complex model 1 To whom correspondence should be addressed, at Department of Pharmacology, University of Melbourne (email [email protected] ). The GPCRs (G-protein-coupled...

...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...