Bruton’s Tyrosine Kinase Inhibitors: Approaches to Potent and Selective Inhibition, Preclinical and Clinical Evaluation for Inflammatory Diseases and B Cell Malignancies

Journal of Medicinal Chemistry
2012.0

Abstract

This article will review BTK structural biology with a focus on design features for selective BTK inhibitors. We first summarize the publically available structural information on the BTK kinase domain. Then we will provide a brief summary and analysis with key SAR information for the most potent inhibitors reported for the chemical classes that have been disclosed in patents and publications. When available, preclinical and clinical data for advanced compounds will be summarized.

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