A Small Molecule Compound Binds to a Target Protein 2

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André Richters, Brice H. Curtin, Angela N. Koehler

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Dysfunctional proteins drive the onset and progression of cancer. The protein CDK9 is a major player in cell cycle regulation. It modulates and alters the half-life of various downstream proteins such as the Androgen Receptor (AR) which regulates gene expression. A truncated and therefore dysfunctional version of AR represents the prime molecular target that drives castration-resistant prostate cancer (CRPC). This truncated version is considered “undruggable”. This image provides a first insight into the molecular details of a drug-like small molecule selectively binding to CDK9 and thereby provides the foundation for further drug development approaches.