Rosemary Burke

TL;DR: Responses to anticancer agents ex vivo in organoids and PDO-based orthotopic mouse tumor xenograft models with the responses of the patients in clinical trials are compared to suggest that PDOs can recapitulate patient responses in the clinic and could be implemented in personalized medicine programs.

TL;DR: In this article, the effects of HSP90 inhibitors on cells with disruption of the microRNA 21 (MIR21 or miRNA21) gene, cells incubated with MIR21 inhibitors, and stable cell lines with inducible expression of microRNA21 were investigated.

TL;DR: Compound 109 (CCT251921), a potent, selective, and orally bioavailable inhibitor of CDK8 with equipotent affinity for CDK19 is reported, which affords the optimal compromise of in vitro biochemical, pharmacokinetic, and physicochemical properties and is suitable for progression to animal models of cancer.

TL;DR: N-substituted 4-(pyridin- 2-yl)thiazole-2-amine derivatives are discovered and their subsequent optimization is guided by structure-based design to give 8-(1H-pyrazol-3-yl]pyrido[3,4-d]pyrimid in-4(3H)-ones, a series of potent JmjC histone N-methyl lysine demethylase (KDM) inhibitors

TL;DR: This potent and selective chemical tool stabilizes an inactive conformation of MPS1 with the activation loop ordered in a manner incompatible with ATP and substrate-peptide binding, which displays a favorable oral pharmacokinetic profile and is an attractive tool compound to elucidate further the therapeutic potential of Mps1 inhibition.