Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3.
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Raux B. et al, (2024), Bioorganic & medicinal chemistry letters, 98
Target deconvolution with matrix-augmented pooling strategy reveals cell-specific drug-protein interactions.
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Open resources for chemical probes and their implications for future drug discovery
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Discovery of a chemical probe to study implications of BPTF bromodomain inhibition in cellular and in vivo experiments.
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Cyclic peptides target the aromatic cage of a PHD-finger reader domain to modulate epigenetic protein function
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Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
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Londregan AT. et al, (2023), Journal of medicinal chemistry, 66, 460 - 472
Global Assessment of Drug Target Engagement and Selectivity of Covalent Cysteine-Reactive Inhibitors Using Alkyne-Functionalized Probes.
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DNA double-strand break-derived RNA drives TIRR/53BP1 complex dissociation.
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Ketley RF. et al, (2022), Cell reports, 41
Covalent fragment-based ligand screening approaches for identification of novel ubiquitin proteasome system modulators
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Chemoproteomic Profiling of Covalent XPO1 Inhibitors to Assess Target Engagement and Selectivity
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Fragment Screening Reveals Starting Points for Rational Design of Galactokinase 1 Inhibitors to Treat Classic Galactosemia
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Mackinnon SR. et al, (2021), ACS Chemical Biology, 16, 586 - 595
TP-MAP - an Integrated Software Package for the Analysis of 1D and 2D Thermal Profiling Data
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Feyertag F. and Huber KVM., (2021)
Deletion of the deISGylating enzyme USP18 enhances tumour cell antigenicity and radiosensitivity
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Pinto-Fernandez A. et al, (2021), British Journal of Cancer, 124, 817 - 830
Deliberately Losing Control of C-H Activation Processes in the Design of Small-Molecule-Fragment Arrays Targeting Peroxisomal Metabolism.
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Discovery of novel immunopharmacological ligands targeting the IL-17 inflammatory pathway.
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Álvarez-Coiradas E. et al, (2020), International immunopharmacology, 89
Quantifying CDK inhibitor selectivity in live cells.
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Wells CI. et al, (2020), Nature communications, 11
Demonstration of the utility of DOS-derived fragment libraries for rapid hit derivatisation in a multidirectional fashion.
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Kidd SL. et al, (2020), Chemical science, 11, 10792 - 10801
Re-Evaluating the Mechanism of Action of α,β-Unsaturated Carbonyl DUB Inhibitors b-AP15 and VLX1570: A Paradigmatic Example of Unspecific Protein Cross-linking with Michael Acceptor Motif-Containing Drugs
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Ward JA. et al, (2020), Journal of Medicinal Chemistry, 63, 3756 - 3762
Quantifying Target Occupancy of Small Molecules Within Living Cells.
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Robers MB. et al, (2020), Annual review of biochemistry
Importance of Quantifying Drug-Target Engagement in Cells
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Stefaniak J. and Huber KVM., (2020), ACS Medicinal Chemistry Letters