AI Article Synopsis
- Solubilizing groups are added to kinase inhibitor drugs to improve their solubility for development, often at sites that don't affect their effectiveness.
- In this study, researchers incorporated these solubilizing groups into Rho kinase (ROCK) inhibitors.
- The addition not only increased solubility but also boosted the inhibitors' potency and selectivity against a similar kinase, PKA.
Article Abstract
Solubilizing groups have been frequently appended to kinase inhibitor drug molecules when solubility is insufficient for pharmaceutical development. Such groups are usually located at substitution sites that have minimal impact on target activity. In this report we describe the incorporation of solubilizing groups in a class of Rho kinase (ROCK) inhibitors that not only confer improved solubility, but also enhance target potency and selectivity against a closely related kinase, PKA.
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| http://dx.doi.org/10.1016/j.bmcl.2018.06.043 | DOI Listing |
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