Co-Mentor: Cara Brocklehurst, PhD
Global Discovery Chemistry
Good chemical starting points are key for the success of drug discovery projects. The Hit Generation Sciences (HGS) group of NIBR is searching for novel, trackable chemical matter that allows not only investigating new disease treatment pathways, but ideally also enabling further optimization towards the potential drug substance. To identify such new chemical matter, the long-standing archive of proprietary substances is constantly being enriched with new compounds evolving from the latest research findings and regularly utilized in multiple screening efforts. Furthermore, new technologies, such as DNA encoded and RNA template encoded ribosomal cyclic peptide libraries, are these days key approaches we use for the discovery of novel chemical matter that modulates a specific protein.
In addition, our group is enhancing the novel chemical matter to enable the study and validation of the new concepts for disease treatments. To accelerate not only the identification but also optimization of such compounds, we are also looking into further developments of organic synthesis.
Cyclic Carbo-Isosteric Depsipeptides and Peptides as a Novel Class of Peptidomimetics.
Gueret SM, Meier P, Roth HJ.
Org Lett. 2014 Mar 7;16(5):1502-5
Detecting S-adenosyl-L-methionine-induced conformational change of a histone methyltransferase using a homogeneous time-resolved fluorescence-based binding assay.
Lin Y, Fan H, Frederiksen M, Zhao K, Jiang L, Wang Z, Zhou S, Guo W, Gao J, Li S, Harrington E, Meier P, Scheufler C, Xu YC, Atadja P, Lu C, Li E, Gu XJ.
Anal Biochem. 2012 Apr 1;423(1):171-7
Key Aspects of the Novartis Compound Collection Enhancement Project for the Compilation of a Comprehensive Chemogenomics Drug Discovery Screening Collection.
Jacoby E, Schuffenhauer A, Popov M, Azzaoui K, Havill B, Schopfer U, Engeloch C, Stanek J, Acklin P, Rigollier P, Stoll P, Koch G, Meier P, Orain D, Giger R, Hinrichs J, Malagu K, Zimmermann J, Roth HJ.
Curr Top Med Chem. 2005;5(4):397-411
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