Allen John Lovey

TL;DR: The identification of a stereoisomer of retinoic acid, 9-cis retinol, which directly binds and activates RXRα, which suggests a new role for isomerization in the physiology of natural retinoids.

TL;DR: 9-cis forms of endogenous retinoid can contribute to the pleiotropic effects of retinoids by interacting with both the RARs and RXRs.

TL;DR: RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket ofMDM2, which stabilizes p53 and activates the p 53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts.

TL;DR: Dual MDM2/MDMX antagonists restored p53 apoptotic activity in the presence of high levels of MDMX and may offer a more effective therapeutic modality for MDMX-overexpressing cancers.

TL;DR: The 2,4-diamino-5-ketopyrimidines 6 reported here represent a novel class of potent and ATP-competitive inhibitors that selectively target the cyclin-dependent kinase family, and compound 39 demonstrates significant in vivo efficacy in the HCT116 human colorectal tumor xenograft model in nude mice with up to 95% tumor growth inhibition.