33 research outputs found
Effect of waterfowl (Anas platyrhynchos) on indicator bacteria populations in a recreational lake Madison, Wisconsin
No full textMechanistic Studies on the Reaction of Fischer Carbene Complex with Alkynes: Does the Alkyne Insertion Intermediate Form Irreversibly?
No full textConformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity
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Simple Analysis of Primary and Secondary Bile Salt Hydrolysis in Mouse and Human Gut Microbiome Samples by Using Fluorogenic Substrates
No full textConformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity
No full textIn the kinase field, there are many
widely held tenets about conformation-selective
inhibitors that have yet to be validated using controlled experiments.
We have designed, synthesized, and characterized a series of kinase
inhibitor analogues of dasatinib, an FDA-approved kinase inhibitor
that binds the active conformation. This inhibitor series includes
two Type II inhibitors that bind the DFG-out inactive conformation
and two inhibitors that bind the αC-helix-out inactive conformation.
Using this series of compounds, we analyze the impact that conformation-selective
inhibitors have on target binding and kinome-wide selectivity
On the Return-Volatility Relationship in the Bitcoin Market around the Price Crash of 2013
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