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Title [sv]
Paramagnetisk märkning av ligander, ett nytt molekylärt verktyg i läkemedelsutveckling
Title [en]
Paramagnetic ligand tagging, a new tool in drug development
Abstract [en]
Access to 3D-structural information on the protein complexes of pharmaceutical screening hits is crucial for their development into lead molecules, i.e. starting points for new drugs. Due to inefficiency – and often inability – of currently used spectroscopic and crystallization methods to provide detailed structural information of low affinity hit-target complexes, this step is a major bottleneck of current drug development.Our aim is to show proof of concept of a novel concept for determination of the binding site and binding mode of bioactive substances to their target proteins. We will synthesize a paramagnetic tag that can be attached to virtually any types of substances, and that will provide detailed structural information with at least hundred times higher sensitivity than conventional techniques.To demonstrate the scope and usability of this technique, we will replace the DNA-tag of real life pharmaceutical hits, identified by AstraZeneca using DNA-encoded library technology, with our tag and collect information on their protein binding site. This will facilitate the structure-guided development into drugs.We will then generate a paramagnetic toolbox, i.e. a set of tags with a variety of attachment points and with different magnetic susceptibilities, and make these tags commercially available.The new technique introduced here will increase the efficiency of drug development, by making it cheaper and faster, and enable development of hits otherwise discarded.
Principal InvestigatorErdelyi, Mate
Coordinating organisation
Uppsala University
Funder
Period
2016-01-01 － 2016-12-31
National Category
Medicinal Chemistry
Identifiers
DiVA, id: project:5978Project, id: 2016-05978_VR

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