Paul R. Keller

TL;DR: Results indicate that inhibition of Cdk4/6 alone is sufficient to cause tumor regression and a net reduction in tumor burden in some tumors.

TL;DR: A direct comparison between 6-acrylamido-4-anilinoquinazoline and an equally potent but reversible analog shows that the irreversible inhibitor has far superior in vivo antitumor activity in a human epidermoid carcinoma xenograft model with no overt toxicity at therapeutically active doses.

TL;DR: It is reported that the introduction of a methyl substituent at the C-5 position of the pyrido[2,3-d]pyrimidin-7-one template is sufficient to confer excellent selectivity for Cdk4 vs other Cdks and representative tyrosine kinases.

TL;DR: The tyrosine kinase inhibitors PD 69896, 153717, and 158780 were characterized with respect to enzymology, target specificity, and antiproliferative effects in tumor cells, indicating an anticancer utility in tumors expressing these receptors.

TL;DR: The results demonstrate a novel synthetic inhibitor with nanomolar potency and specificity towards the FGF-1 receptor tyrosine kinase.