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Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain
TLDR
PD 173074 is a promising candidate for a therapeutic angiogenesis inhibitor to be used in the treatment of cancer and other diseases whose progression is dependent upon new blood vessel formation.
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Subclasses of angiotensin II binding sites and their functional significance.
TLDR
The results suggest the existence of two subclasses of angiotensin II binding sites, which differ in their tissue distribution and affinity for the nonpeptide ligands Dup 763, Exp 6803, and PD 123319.
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In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase.
TLDR
Results highlight the discovery of PD 166866, a new nanomolar potent and selective small molecule inhibitor of the FGFR-1 tyrosine kinase with potential use as antiproliferative/antiangiogenic agent for such therapeutic targets as tumor growth and neovascularization of atherosclerotic plaques.
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In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor.
  • R. Panek, G. Lu, J. Keiser
  • Biology, Chemistry
    The Journal of pharmacology and experimental…
  • 1 December 1997
TLDR
The potential therapeutic utility of this broadly acting inhibitor as an antiproliferative and antimigratory agent could extend to such diseases as cancer, atherosclerosis and restenosis, in which redundancies in protein kinase signaling pathways are known to exist.
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2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.
TLDR
In in vivo studies against a panel of seven xenograft tumor models with known and/or inferred dependence on the EGFr, PDGFr, and c-Src TKs, compound 63 produced a tumor growth delay of 10.6 days against the relatively refractory SK-OV-3 ovarian Xenograft and also displayed activity against the HT-29 tumor.
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Inhibition of Sphingomyelin Synthesis Reduces Atherogenesis in Apolipoprotein E–Knockout Mice
TLDR
Inhibition of de novo SM biosynthesis in apoE-KO mice lowers plasma cholesterol and triglyceride levels, raises HDL cholesterol, and prevents development of atherosclerotic lesions.
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Endothelin and structurally related analogs distinguish between endothelin receptor subtypes.
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Modulation of lipoprotein metabolism by inhibition of sphingomyelin synthesis in ApoE knockout mice.
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PDGF receptor protein tyrosine kinase expression in the balloon-injured rat carotid artery.
TLDR
It is shown that balloon injury to rat carotid arteries results in temporally related changes in the expression of PDGF receptors and their state of tyrosine phosphorylation, which resulted in the association of PI-3 kinase.
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A Contrasting effect of the diabetic state upon the contractile responses of aortic preparations from the rat and rabbit
TLDR
While both rats and rabbits exhibited a similar degree of hyperglycemia after treatment with a diabetogenic agent, aortic preparations from the rabbit are not affected in the same way as the aorta from the diabetic rat when exposed to NA, 5‐HT and KCl, suggesting that the diabetic state may affect processes responsible for contraction beyond the level of receptor activation.
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