Li Sun

TL;DR: The pharmacokinetic/pharmacodynamic relationship established for SU11248 in these preclinical studies has aided in the design, selection, and evaluation of dosing regimens being tested in human trials.

TL;DR: A new class of protein tyrosine kinase inhibitors was identified that is based on an oxindole core (indolinones) and two compounds from this class inhibited the kinase activity of fibroblast growth factor receptor 1 (FGFR1) and showed differential specificity toward other receptor tyrosin kinases.

TL;DR: Findings support that pharmacological inhibition of the enzymatic activity of the vascular endothelial growth factor receptor represents a novel strategy for limiting the growth of a wide variety of tumor types.

TL;DR: The identified and characterized a small-molecule inhibitor, SU6656, which exhibits selectivity for Src and other members of the Src family, and microinjection experiments demonstrated that a Shc molecule carrying mutations of tyrosines 239 and 240, in conjunction with an SH2 domain mutation, interfered with PDGF-stimulated DNA synthesis.

TL;DR: Oral or i.p. administration of SU6668 in athymic mice resulted in significant growth inhibition of a diverse panel of human tumor xenografts of glioma, melanoma, lung, colon, ovarian, and epidermoid origin, and intravital multifluorescence videomicroscopy of C6glioma xenografteds in the dorsal skinfold chamber model revealed thatSU6668 treatment suppressed tumor angiogenesis.