Fragment-Based Drug Discovery (FBDD) for Finding Novel Chemical Probes

DRA symposium

Fragment-based drug discovery (FBDD) has in recent years grown into a powerful approach for identifying potent and druglike small-molecule protein inhibitors and has provided several clinical candidates and 3 marketed drugs. The principle of FBDD is to start from small substructures (fragments) of druglike compounds with molecular weight of 100-300 Daltons and few functional groups. This comes with several advantages, but also challenges. In this symposium we will see examples of how FBDD is conducted in leading FBDD labs – academic and industrial – from Copenhagen as well as Oxford.

(download programme and abstracts)

15:15 – 15:35

Targeting Protein-Protein Interactions Involved in Oxidative Stress using FBDD
Assoc. Prof. Anders Bach, University of Copenhagen (Dept. of Drug Design and Pharmacology)

15:35 – 16:05

Chemical Probes in Target Discovery
Prof. Paul Brennan, University of Oxford (Target Discovery Institute) & Structural Genomics Consortium

16:05 – 16:15

Coffee break

16:15 – 16:45

The 3F Library: Fluorinated Fsp3-rich Fragments for Expeditious 19F-NMR-based Screening
PhD student Nikolaj Sten Troelsen, Technical University of Denmark (Dept. of Chemistry; Group of Prof. Mads H. Clausen)

16:45 – 17:15

Fragment-Based Discovery of JAK1 Inhibitors with Excellent Subtype Selectivity
Andreas Ritzén, LEO Pharma A/S (MedChem II)

The following day PhD student Jakob Staun Pallesen will defend his thesis entitled:
‘Development of Novel Keap1−Nrf2 Protein-Protein Interaction Inhibitors by Fragment-Based Drug Discovery’
Tuesday 8th October 2019, 14:00 – 17:00, Auditorium 3

The symposium is organized on behalf of the graduate programme in pharmaceutical sciences, Drug Research Academy, by Assoc. Prof. Anders Bach, Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen.

The symposium is free of charge and open for attendance by all interested parties. It is not necessary to pre-register.