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Vascular endothelial growth factor upregulates the expression of matrix metalloproteinases in vascular smooth muscle cells: role of flt-1.
These data are the first to show a direct effect of VEGF on SMCs, and suggest SMC-derived MMPs may be an additional source of proteases to digest vascular basement membrane, which is a crucial step in the initial stage of angiogenesis. Expand
In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor.
  • R. Panek, G. Lu, +6 authors J. Keiser
  • Biology, Medicine
  • The Journal of pharmacology and experimental…
  • 1 December 1997
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. Expand
Torcetrapib induces aldosterone and cortisol production by an intracellular calcium-mediated mechanism independently of cholesteryl ester transfer protein inhibition.
The results indicate that the pressor and adrenal effects observed with torcetrapib and related molecules are independent of CETP inhibition. Expand
Pharmacological characterization of PD 156707, an orally active ETA receptor antagonist.
PD 156707 administered orally to rats blocked subsequent ETAR-mediated pressor responses in vivo but had no effect on ETBR-mediated dilator responses, which will be useful in defining the physiological and pathological roles of ETAR. Expand
PDGF receptor protein tyrosine kinase expression in the balloon-injured rat carotid artery.
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. Expand
Mechanistic studies of blood pressure in rats treated with a series of cholesteryl ester transfer protein inhibitors
ILLUMINATE, the Phase 3 clinical trial of morbidity and mortality (M&M) with the cholesteryl ester transfer protein inhibitor (CETPi), torcetrapib (CP‐529,414), was terminated in December 2006 due toExpand
Role for endothelin-1 in angiotensin II-mediated hypertension.
Some of the vascular effects of Ang II thought to be unique to this hormone are likely mediated by endothelin-1, and blockade of ET(A) receptor during Ang II-mediated hypertension was associated with marked elevations of plasma endothelins-1 levels. Expand
Renal hemodynamic and excretory responses to PD 123319 and losartan, nonpeptide AT1 and AT2 subtype-specific angiotensin II ligands.
Compared the renal response to treatment with the nonpeptides, DuP 753 and PD 123319, and the peptide antagonist, saralasin, in anesthetized mongrel dogs, and suggests that the angiotensin type 2 receptor may be related to water handling by the kidney. Expand
Effects of quinapril, a new angiotensin converting enzyme inhibitor, on left ventricular failure and survival in the cardiomyopathic hamster. Hemodynamic, morphological, and biochemical correlates.
It is concluded that chronic quinapril therapy exerts a significant cardioprotective effect and also increases survival in CM hamsters. Expand
Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors.
Screening of a compound library for inhibitors of the fibroblast growth factor and platelet-derived growth factor receptor tyrosine kinases led to the development of a novel series of ATP competitive pyrido[2,3-d]pyrimidine tyrosinesine kinase inhibitors, resulting in new analogs with improved potency, solubility, and bioavailability relative to the initial lead. Expand