26 research outputs found
Isolation and structural elucidation of thermal degradation products of theFusarium mycotoxin nivalenol
On the development of a finite element model to analyze the behavior of hybrid composites considering the manufacturing history
Flexible Frequency-Band Reallocation Networks Using Variable Oversampled Complex-Modulated Filter Banks
Structure–activity relationship study of beta-carboline derivatives as haspin kinase inhibitors
Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: Development of chemical probe ML315
Substituted pyrimidine inhibitors of the Clk and Dyrk kinases have been developed, exploring structure-activity relationships around four different chemotypes. The most potent compounds have low-nanomolar inhibitory activity against Clk1, Clk2, Clk4, Dyrk1A and Dyrk1B. Kinome scans with 442 kinases using agents representing three of the chemotypes show these inhibitors to be highly selective for the Clk and Dyrk families. Further off-target pharmacological evaluation with ML315, the most selective agent, supports this conclusion