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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Open resources for chemical probes and their implications for future drug discovery.
Journal article
Balıkçı E. et al, (2023), Expert Opin Drug Discov, 18, 505 - 513
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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, (2023), J Med Chem, 66, 460 - 472
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Cyclic peptides target the aromatic cage of a PHD-finger reader domain to modulate epigenetic protein function
Journal article
Coleman OD. et al, (2023), Chemical Science
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Global Assessment of Drug Target Engagement and Selectivity of Covalent Cysteine-Reactive Inhibitors Using Alkyne-Functionalized Probes.
Journal article
Rothweiler EM. and Huber KVM., (2023), Methods Mol Biol, 2706, 191 - 200