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.
A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function
Fagan V. et al, (2019), Journal of Medicinal Chemistry
Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.
Böttcher J. et al, (2019), Nat Chem Biol, 15, 822 - 829
Regulation of influenza A virus mRNA splicing by CLK1.
Artarini A. et al, (2019), Antiviral Res, 168, 187 - 196
Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening
Resnick E. et al, (2019), Journal of the American Chemical Society, 141, 8951 - 8968
Target identification studies of a utrophin modulator for treatment of Duchenne muscular dystrophy
Wilkinson I. et al, (2019), ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 257