Advances in targeting 'undruggable'transcription factors with small molecules

MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …

[HTML][HTML] PROteolysis TArgeting Chimeras (PROTACs)—past, present and future

M Pettersson, CM Crews - Drug Discovery Today: Technologies, 2019 - Elsevier
The majority of currently used therapeutics are small molecule-based and utilize occupancy-
driven pharmacology as the mode of action (MOA), in which the protein function is …

Impact of a five-dimensional framework on R&D productivity at AstraZeneca

P Morgan, DG Brown, S Lennard… - Nature reviews Drug …, 2018 - nature.com
In 2011, AstraZeneca embarked on a major revision of its research and development (R&D)
strategy with the aim of improving R&D productivity, which was below industry averages in …

The development of ruthenium (II) polypyridyl complexes and conjugates for in vitro cellular and in vivo applications

FE Poynton, SA Bright, S Blasco, DC Williams… - Chemical Society …, 2017 - pubs.rsc.org
Ruthenium (II)[Ru (II)] polypyridyl complexes have been the focus of intense investigations
since work began exploring their supramolecular interactions with DNA. In recent years …

[HTML][HTML] Advanced MALDI mass spectrometry imaging in pharmaceutical research and drug development

S Schulz, M Becker, MR Groseclose, S Schadt… - Current opinion in …, 2019 - Elsevier
Highlights•Ideal mass spectrometer for MALDI MSI would satisfy the '4S-criteria for
performance'(speed, specificity, spatial resolution and sensitivity).•Quantification MALDI MSI …

Feeling nature's PAINS: natural products, natural product drugs, and pan assay interference compounds (PAINS)

JB Baell - Journal of natural products, 2016 - ACS Publications
We have previously reported on classes of compounds that can interfere with bioassays via
a number of different mechanisms and termed such compounds Pan Assay INterference …

Improving target assessment in biomedical research: the GOT-IT recommendations

CH Emmerich, LM Gamboa, MCJ Hofmann… - Nature reviews Drug …, 2021 - nature.com
Academic research plays a key role in identifying new drug targets, including understanding
target biology and links between targets and disease states. To lead to new drugs, however …

Discovery of roblitinib (FGF401) as a reversible-covalent inhibitor of the kinase activity of fibroblast growth factor receptor 4

RA Fairhurst, T Knoepfel, N Buschmann… - Journal of medicinal …, 2020 - ACS Publications
FGF19 signaling through the FGFR4/β-klotho receptor complex has been shown to be a key
driver of growth and survival in a subset of hepatocellular carcinomas, making selective …

Virtual screening techniques in drug discovery: review and recent applications

SFL da Silva Rocha, CG Olanda… - Current topics in …, 2019 - ingentaconnect.com
The discovery of bioactive molecules is an expensive and time-consuming process and new
strategies are continuously searched for in order to optimize this process. Virtual Screening …

Concise review: stem cell trials using companion animal disease models

AM Hoffman, SW Dow - Stem cells, 2016 - academic.oup.com
Studies to evaluate the therapeutic potential of stem cells in humans would benefit from
more realistic animal models. In veterinary medicine, companion animals naturally develop …