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Biased agonism in drug discovery: is it too soon to choose a path? (2018)
Journal Article
Michel, M. C., & Charlton, S. J. (2018). Biased agonism in drug discovery: is it too soon to choose a path?. Molecular Pharmacology, 93(4), https://doi.org/10.1124/mol.117.110890

A single receptor can activate multiple signaling pathways that have distinct or even opposite effects on cell function. Biased agonists stabilize receptor conformations preferentially stimulating one of these pathways, and therefore allow a more tar... Read More about Biased agonism in drug discovery: is it too soon to choose a path?.

Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor (2018)
Journal Article
Whittaker, S. R., Barlow, C., Martin, M. P., Mancusi, C., Wagner, S., Self, A., …Workman, P. (in press). Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor. Molecular Oncology, 12(3), https://doi.org/10.1002/1878-0261.12148

Deregulation of the cyclin-dependent kinases (CDKs) has been implicated in the pathogenesis of multiple cancer types. Consequently, CDKs have garnered intense interest as therapeutic targets for the treatment of cancer. We describe herein the molecul... Read More about Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor.