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A novel endothelial-derived lipase that modulates HDL metabolism
TLDR
The cloning and in vivo functional analysis of a new member of the TG lipase family that is synthesized by endothelial cells in vitro and thus has been termed endothelial lipase (encoded by the LIPG gene) suggests that it may have a role in lipoprotein metabolism and vascular biology. Expand
Bisphosphonates used for the treatment of bone disorders inhibit squalene synthase and cholesterol biosynthesis.
TLDR
Structural modifications on YM 175 to enhance cell permeability may result in a new class of cholesterol-lowering agents. Expand
1-Hydroxy-3-(methylpentylamino)-propylidene-1,1-bisphosphonic acid as a potent inhibitor of squalene synthase.
TLDR
It was discovered that BM 21.0955 inhibited rat liver microsomal squalene synthase, and structural modifications on this molecule to make it more lipophilic may result in a new class of cholesterol-lowering agents. Expand
Inhibition of the effects of thrombin on guinea pig platelets by the diacylglycerol lipase inhibitor RHC 80267.
TLDR
It is proposed that PLC-DGL is an important enzymatic pathway for the release of AA in guinea pig platelets. Expand
Restenosis following angioplasty in the swine coronary artery is inhibited by an orally active PDGF-receptor tyrosine kinase inhibitor, RPR101511A.
TLDR
RPR101511A, which acts by inhibition of the PDGFr-TK, completely prevented angiographic loss of gain following PTCA and significantly reduced histological intimal hyperplasia. Expand
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.
RPR127963 demonstrates an excellent pharmacokinetic profile in several species and was found to be efficacious in the prevention of restenosis in a Yucatan mini-pig model upon oral administration ofExpand
RPR 107393, a potent squalene synthase inhibitor and orally effective cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase.
TLDR
RPR 107393 is an orally effective hypocholesterolemic agent in rats and marmosets that has greater efficacy than lovastatin or pravastatin in the marmoset and in vitro data demonstrate that these compounds are inhibitors of squalene synthase. Expand
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent.
  • M. Myers, W. He, +8 authors A. Spada
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
  • 15 September 2003
TLDR
Replacement of an anilino-substituent with substituted cyclohexylamino- or norbornylamino substituents led to significant improvements in the pharmacokinetic profile of these analogues. Expand
RG 12561 (dalvastatin): a novel synthetic inhibitor of HMG-CoA reductase and cholesterol-lowering agent.
TLDR
In WHHL rabbits and cholestyramine-fed hamsters, RG 12561 and lovastatin reduced serum cholesterol by 17 and 16%, respectively, and these results demonstrate thatRG 12561 is a potent cholesterol-lowering agent. Expand
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