Beactica scientists describe strategies for fragment-based drug discovery in two publications in Journal of Medicinal Chemistry.
Uppsala, Sweden, 4 February 2011
Beactica, the leading Swedish fragment-based drug discovery company, 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.
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 interaction of molecules in order to generate novel therapeutics. The Company offers expertise and services in the area of 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. For more information, please visit www.beactica.com.
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Beactica increases its capacity to address complex research challenges with a Biacore 4000
Uppsala, Sweden, 2 November 2010
Beactica, the Swedish fragment-based drug discovery company, today announced an important move to address the need for increased data quality and higher capacity in understanding molecular interactions. Growing customer demand for solutions to ever more complex research challenges has led Beactica to invest in the world’s most sophisticated SPR biosensor to date, the Biacore 4000. The instrument will enable Beactica to offer more advanced experimental designs and a deeper interpretation of interaction analysis data so that stronger therapeutic candidates can be developed.
For additional information please contact Dr Per Källblad, Beactica CEO, +46 18 560 880.