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 potent SARS-CoV-2 nsp3 macrodomain inhibitors uncovers lack of translation to cellular antiviral response.
Preprint
Lee AA. et al, (2024)
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Paralogue-Selective Degradation of the Lysine Acetyltransferase EP300
Journal article
Chen X. et al, (2024), JACS Au
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Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist
Journal article
Balıkçı E. et al, (2024), Journal of Medicinal Chemistry, 67, 7245 - 7259
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Advancing drug discovery through assay development: a survey of tool compounds within the human solute carrier superfamily.
Journal article
Digles D. et al, (2024), Frontiers in pharmacology, 15
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Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3.
Journal article
Raux B. et al, (2024), Bioorganic & medicinal chemistry letters, 98