Neuroscience in Denmark


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General information

Name (center, department, group or other)
Bach Group, Dept. Drug Design and Pharmacology, University of Copenhagen
Contact name
Anders Bach
Contact email
anders#dot#bach#at#sund#dot#ku#dot#dk
Contact title
Assistant Professor
Date
25. January 2016
(Last edited: 25. January 2016)

Brief description of research activities

In our group we focus on medicinal chemistry and brain proteins. Our goal is to develop biological active small-molecule inhibitors against CNS proteins involved in excitotoxicity and oxidative stress. We evaluate the druggability of selected targets and aim at developing new high-quality chemical probes useful for pharmacological studies and for identifying new therapeutic principles against ischemic stroke and related diseases.

Fragment-based drug discovery (FBDD) is a core theme of our research. We screen our library of >2500 fragments (i.e. small substructures of druglike molecules) using very sensitive biophysical methods (SPR and ligand-based NMR) and biochemical assays. Promising hits are optimized into lead molecules by medicinal chemistry, biostructural studies and pharmacology.


Keywords

Medicinal Chemistry, Fragment-based drug discovery, Small molecules, Multi-target inhibitors, Surface Plasmon Resonance (SPR), Ligand-based NMR, Ischemic Stroke, Keap1, NADPH oxidase, PSD-95

Research tools and techniques

Medicinal Chemistry, Fragment-based drug discovery, Fragment Screening, Protein expression, Surface Plasmon Resonance (SPR)

Scientific Personnel

No of Associate Professors/Postdocs: 3
No of PhD students: 1
Other: 1

Key references from within the last 5 years

Bach, A.*; Pedersen, T. B.; Strømgaard, K. Design and synthesis of triazole-based peptidomimetics of a PSD-95 PDZ domain inhibitor. Med. Chem. Comm. 2016, in press. (*Corresponding).

Bach, A.*; Pizzirani, D.*; Realini, N.; Vozella, V.; Russo, D.; Penna, I.; Melzig, L.; Scarpelli, R.; Piomelli, D. Benzoxazolone carboxamides as potent acid ceramidase inhibitors: Synthesis and structure-activity relationship (SAR) studies. J. Med. Chem. 2015, 58, 9258–9272. (*Shared 1st)

Bach, A.*; Pedersen, S. W.; Dorr, L. A.; Vallon, G.; Ripoche, I.; Ducki, S.; Lian, L.-Y*. Biochemical investigations of the mechanism of action of small molecules ZL006 and IC87201 as potential inhibitors of the nNOS-PDZ/PSD-95-PDZ interactions. Sci. Rep. 2015, 5, 12157. (*Corresponding).

Pizzirani, D.*; Bach, A.*; Realini, N.; Armirotti, A.; Mengatto, L.; Bauer, I.; Girotto, S.; Pagliuca, C.; De Vivo, M.; Summa, M.; Ribeiro, A.; Piomelli, D. Benzoxazolone Carboxamides: Potent and systemically active inhibitors of intracellular acid ceramidase. Angew. Chem. Int. Ed. 2015, 54, 485–489. (*Shared 1st)

Bach, A.*; Clausen, B. H.; Møller, M.; Vestergaard, B.; Chi, C. N.; Round, A.; Sørensen, P. L.; Nissen, K. B.; Kastrup, J. S.; Gajhede, M.; Jemth, P.; Kristensen, A. S.; Lundström, P.; Lambertsen, K. L.; Strømgaard, K.*. A high-affinity, dimeric inhibitor of PSD-95 bivalently interacts with PDZ1-2 and protects against ischemic brain damage. Proc. Natl. Acad. Sci. U. S. A. 2012, 109, 3317-3322. (*Corresponding).
Scherfigsvej 7
2100 Copenhagen Ø
Denmark
Tel. +45 39 12 80 00
CVR-nr. 11 81 49 13
info@thebrainprize.org
www.thebrainprize.org
Nils Axelsen Ralf Hemmingsen Lauritz Holm-Nielsen Ralf Hemmingsen Jens Oddershede Jens Frederik Rehfeld Anders Bjørklund