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Medicine & Law Weekly

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Abbott Laboratories



Potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) discovered



June 2nd, 2006

A potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) was discovered.

According to recent research published in the journal Bioorganic & Medicinal Chemistry Letters, "Structure-based design and synthesis of the 3,4'-bispyridinylethylene series led to the discovery of 3-isoquinolinylpyridine 13a as a potent PKB/Akt inhibitor with an IC50 of 1.3 nM against Akt1. Compound 13a shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor to marginal selectivity against closely related kinases in the AGC and CMGC families."

"Moreover, 13a demonstrates potent...


Source: Medicine & Law Weekly (2006-06-02)

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