Beactica, the leading Swedish fragment-based drug discovery company, today announced the publication of two key papers based on in-house research in the field-leading Journal of Medicinal Chemistry*. The papers present methodological advances in SPR biosensor-based drug discovery targeting structurally dynamic proteins, a significant challenge for the pharmaceutical industry, that have been implemented in Beactica’s Sprint™ platform.
The first paper describes the identification of novel chemical scaffolds for inhibition of wild-type and drug-resistant HIV-1 reverse transcriptase by SPR-based fragment screening. The study demonstrates that an efficient experimental design can enable the identification of molecular fragments with desired characteristics and a defined mode of action – also for challenging targets. The second paper outlines concepts for an improved understanding of the druggability of target proteins during fragment-based lead generation. The Sprint™ methodology developed on the basis of the findings enables an improved evaluation and prioritization of screening hits.
The research is a result of an international collaboration between Beactica, IOTA Pharmaceuticals Ltd, Cambridge, UK, and scientists at Uppsala University, Sweden.
For additional information please contact Dr Per Källblad, Beactica CEO, +46 18 560880.
* Publication references
Geitmann et al., Identification of a novel scaffold for allosteric inhibition of wild type and drug resistant HIV-1 reverse transcriptase by fragment library screening. Journal of Medicinal Chemistry, 2011, 54:699–708 (DOI: 10.1021/jm1010513).
Brandt et al., Deconstruction of non-nucleoside reverse transcriptase inhibitors of human immunodeficiency virus type 1 for exploration of the optimization landscape of fragments. Journal of Medicinal Chemistry, 2011, 54:709–18 (DOI: 10.1021/jm101052g).
Beactica AB is a specialist drug discovery company, utilising its proprietary methodologies to evaluate the biophysical interaction of molecules in order to generate novel therapeutics. The Company offers expertise and services in the area of surface plasmon resonance (SPR) biosensor-based small molecule interaction analysis and partnerships for fragment-based lead generation using its proprietary Sprint™ platform. Founded in 2006 based on research carried out at Uppsala University and first-hand experience from the drug discovery industry, Beactica has established a robust reputation as the leader in SPR-based small molecule drug discovery. As well as providing services and building collaborations with external companies, Beactica is progressing its own drug discovery programmes. The company has its headquarter in Uppsala, Sweden. For more information, please visit www.beactica.com.