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 …

Small-molecule inhibitors of protein-protein interactions: progressing toward the reality

MR Arkin, Y Tang, JA Wells - Chemistry & biology, 2014 - cell.com
The past 20 years have seen many advances in our understanding of protein-protein
interactions (PPIs) and how to target them with small-molecule therapeutics. In 2004, we …

[HTML][HTML] Visualizing and trapping transient oligomers in amyloid assembly pathways

EE Cawood, TK Karamanos, AJ Wilson… - Biophysical chemistry, 2021 - Elsevier
Oligomers which form during amyloid fibril assembly are considered to be key contributors
towards amyloid disease. However, understanding how such intermediates form, their …

Real-time monitoring of endogenous cysteine levels in vivo by near-infrared turn-on fluorescent probe with large stokes shift

Y Qi, Y Huang, B Li, F Zeng, S Wu - Analytical chemistry, 2018 - ACS Publications
Cysteine (Cys), as an important biothiol, plays a major role in many physiological processes
like protein synthesis, detoxification and metabolism, and also is closely associated with a …

Reversible dual-covalent molecular locking of the 14-3-3/ERRγ protein–protein interaction as a molecular glue drug discovery approach

BA Somsen, RJC Schellekens… - Journal of the …, 2023 - ACS Publications
Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool
compounds for biophysics and (structural) biology, and as starting points for molecular glue …

Minimum information guidelines for experiments structurally characterizing intrinsically disordered protein regions

B Mészáros, A Hatos, N Palopoli, F Quaglia… - Nature …, 2023 - nature.com
An unambiguous description of an experiment, and the subsequent biological observation,
is vital for accurate data interpretation. Minimum information guidelines define the …

19 F NMR viewed through two different lenses: ligand-observed and protein-observed 19 F NMR applications for fragment-based drug discovery

CR Buchholz, WCK Pomerantz - RSC chemical biology, 2021 - pubs.rsc.org
19F NMR has emerged as a powerful tool in drug discovery, particularly in fragment-based
screens. The favorable magnetic resonance properties of the fluorine-19 nucleus, the …

Mitochondria-Anchored Colorimetric and Ratiometric Fluorescent Chemosensor for Visualizing Cysteine/Homocysteine in Living Cells and Daphnia magna Model

M Yang, J Fan, W Sun, J Du, X Peng - Analytical chemistry, 2019 - ACS Publications
Cysteine (Cys) and homocysteine (Hcy) are essential for maintaining the cellular redox
homeostasis and play critical roles in pathological and physiological processes. The …

Motif mediated protein-protein interactions as drug targets

C Corbi-Verge, PM Kim - Cell Communication and Signaling, 2016 - Springer
Protein-protein interactions (PPI) are involved in virtually every cellular process and thus
represent an attractive target for therapeutic interventions. A significant number of protein …

Molecular recognition by the KIX domain and its role in gene regulation

JK Thakur, A Yadav, G Yadav - Nucleic acids research, 2014 - academic.oup.com
The kinase-inducible domain interacting (KIX) domain is a highly conserved independently
folding three-helix bundle that serves as a docking site for transcription factors, whereupon …