Contact information
ChemBioHub - Huber Lab Website
https://orcid.org/0000-0002-1103-5300
NDM Research Building
Websites
- Huber Lab TDI Website
- Huber Lab CMD Website
- Podcast: Targeting Drug Discovery
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WIRED Feature
Learn more about our approach to open access drug discovery and scientific crowdsourcing
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Discovering Druggable Targets
Interview with Technology Networks
Kilian Huber
Principal Investigator
Chemical Biology - Drug Discovery - Proteomics - Systems Pharmacology - Medicinal Chemistry
Probing Biology with Small Molecules for Drug Target Discovery
The development of new medicines to treat diseases like cancer or inflammatory disorders is dependent on the identification of novel drug targets. Target selection requires an understanding of the functional relevance of a given protein in both physiological and pathophysiological conditions.
Chemical Biology combines chemistry and biology to generate small molecule tools, so-called “chemical probes”, that enable the functional exploration of cellular proteins with regard to their relevance for drug discovery. Candidate targets may originate from genetic studies linking the expression or mutation of a selected gene to a particular disease, in vitro genetic screens such as RNA-interference or genome-editing (e.g. CRISPR), compounds identified in phenotypic assays or drugs already in use.
To identify, explore and validate targets the Huber laboratory uses a variety of different discovery approaches such as small molecule screens, biochemical assays, protein X-ray crystallography, chemical and protein-protein interaction proteomics, medicinal chemistry, RNAi, genome-editing alongside classical molecular and cellular biology techniques aiming at the development of chemical probes that may provide leads for drug discovery.
Recent publications
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Discovery of a chemical probe to study implications of BPTF bromodomain inhibition in cellular and in vivo experiments.
Journal article
Martinelli P. et al, (2023), ChemMedChem
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Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4.
Journal article
Londregan AT. et al, (2022), J Med Chem
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Covalent fragment-based ligand screening approaches for identification of novel ubiquitin proteasome system modulators
Journal article
Rothweiler EM. et al, (2022), Biological Chemistry, 403, 391 - 402
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A chemical biology toolbox to investigate in-cell target engagement and specificity of PRMT5-inhibitors
Preprint
Rothweiler EM. et al, (2022)
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Chemoproteomic Profiling of Covalent XPO1 Inhibitors to Assess Target Engagement and Selectivity
Journal article
Martin JG. et al, (2021), ChemBioChem, 22, 2116 - 2123