Molecular Biophysics and Biochemistry group in SGC/TDI Oxford specialises on chemical probe discovery projects, especially in the field of Epigenetics. Main target areas are currently acetyl-lysine reader domains and histone demethylases. The group supports the wide variety of screening assays developed for most of the targets. The in-depth characterization of chemical probe candidates relies on a series of biophysical techniques established for accurate measurements of thermodynamics of and kinetic parameters of binding. The group also supports and extend the focused libraries of small molecular weight ligands for proteins of interest.
Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1
Ni X. et al, (2019), ACS Medicinal Chemistry Letters, 10, 1661 - 1666
A chemical toolbox for the study of bromodomains and epigenetic signaling
Wu Q. et al, (2019), Nature Communications, 10
A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function
Fagan V. et al, (2019), Journal of Medicinal Chemistry
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays.
Le Bihan Y-V. et al, (2019), European journal of medicinal chemistry, 177, 316 - 337
Discovery of a potent and selective fragment-like inhibitor of SPIN1
Yan X. et al, (2019), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 258