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Markus Schirle: "Affinity proteomics and target identification for small molecule drug candidates"

Wann 19.04.2012
von 13:15 bis 14:00
Wo FRIAS Seminar Room, Albertstr. 19, 79104 Freiburg
Name Jörn Dengjel
Kontakttelefon +49-(0)761-203-97208
Teilnehmer Open to University employees
Termin übernehmen vCal

Markus Schirle
Novartis Institutes for BioMedical Research, Cambridge, USA


Affinity proteomics and target identification for small molecule drug candidates

Affinity proteomics has become a valuable tool in preclinical small molecule drug discovery, in particular in the context of target identification and elucidation of the mechanism of action for drug candidates from phenotypic and pathway-centric approaches to drug discovery. Quantitative chemoproteomics, employing variations of a competition-based approach to small molecule affinity chromatography and mass spectrometry-based protein identification and quantitation, identifies cellular protein interactors and thus potential targets of drug candidates under conditions approximating the disease-relevant in vivo situation. Several examples will be presented and discussed in the context of orthogonal approaches to the generation of target hypotheses. On the other hand, the identification of protein-protein interactions using e.g. an affinity-tagged bait protein is often a crucial step towards functional characterization of hits from unbiased chemoproteomic experiments. By allowing the description of the molecular environment of poorly annotated proteins and e.g. the characterization of enzyme-substrate relationships, this approach can provide insights into the cellular mechanisms affected by the drug candidate.