DYRK family of protein kinases plays crucial role in numerous neurodegenerative diseases (from Alzheimer to Down syndrome). The action of existing kinase modulators is predominantly based on the competitive binding mechanism, for which the knowledge about hinge binding motif is important. Determined hinge binding motif of DYRK1A/B differs them advantageously from the range of other kinases. Considering this, we have summarized the data of modulators’ activity and selectivity known from the literature.1,2,3
The docking based on hot-spot approach was performed and compounds, which form undesirable hydrogen bonds, were removed to increase selectivity.
Physicochemical profiles of UORSY DYRK1A/B modulator library:
250<MW<540; 2<HbA<8; 0<HbD<3; -0.5<logP<6; RotBonds≤8; TPSA<140.
UORSY DYRK1A/B modulator library is available as powders, dry films or DMSO solutions. All compounds have a minimum purity of 90% assessed by 1H NMR; analytical data is provided.
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1 Cuny G. et al., Bioorg. Med. Chem. Lett. 2012 22 2015-2019
2 Anderson K. et al., Bioorg. Med. Chem. Lett. 2013 23 6610-6615
3 Falke H. et al., J. Med. Chem. 2015, 58, 3131-3143
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