Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
- M. Coghlan, A. Culbert, J. Holder
- Biology, ChemistryChemistry and Biology
- 1 October 2000
The key role of apolipoprotein E in atherosclerosis
- K. Greenow, N. Pearce, D. Ramji
- BiologyJournal of molecular medicine
- 13 April 2005
Evidence is presented for the potent anti-atherogenic action of apolipoprotein E and the current understanding of its multiple functions and regulation by factors implicated in the pathogenesis of cardiovascular disease is described.
Development of glucose intolerance in male transgenic mice overexpressing human glycogen synthase kinase-3beta on a muscle-specific promoter.
- N. Pearce, J. R. Arch, J. Holder
- BiologyMetabolism: Clinical and Experimental
- 1 October 2004
Synthetic LXR agonists increase LDL in CETP species Published, JLR Papers in Press, July 16, 2005. DOI 10.1194/jlr.M500116-JLR200
Results in hamsters and cynomolgus monkeys reveal additional problems associated with current synthetic LXR agonists and emphasize the importance of profiling compounds in preclinical species with a more human-like LXR response and lipoprotein metabolism.
The role of ATP citrate-lyase in the metabolic regulation of plasma lipids. Hypolipidaemic effects of SB-204990, a lactone prodrug of the potent ATP citrate-lyase inhibitor SB-201076.
Overall these results are consistent with the concept that ATP citrate-lyase is an important enzyme in controlling substrate supply for lipid synthesis de novo and a potential enzyme target for hypolipidaemic intervention.
A thyromimetic that decreases plasma cholesterol levels without increasing cardiac activity
- A. Underwood, J. C. Emmett, V. P. Shah
- Medicine, BiologyNature
- 4 December 1986
A number of agents that mimic the ability of the thryoid hormone, T3, to decrease plasma cholesterol levels are described; one is as effective as T3 at reducing cholesterol levels and stimulating…
The effect of (-)-hydroxycitrate on the activity of the low-density-lipoprotein receptor and 3-hydroxy-3-methylglutaryl-CoA reductase levels in the human hepatoma cell line Hep G2.
- T. Berkhout, L. Havekes, N. Pearce, P. Groot
- Biology, ChemistryBiochemical Journal
- 15 November 1990
The results suggest that the increases in HMG-CoA reductase and the LDL receptor are initiated by the decreased flux of carbon units in the cholesterol-synthetic pathway, owing to inhibition of ATP citratelyase.
Effects of cholestyramine on lipoprotein levels and metabolism in Syrian hamsters.
- P. Groot, N. Pearce, K. Suckling, S. Eisenberg
- BiologyBiochimica et Biophysica Acta
- 3 January 1992
Apolipoprotein E*3-Leiden transgenic mice as a test model for hypolipidaemic drugs.
- B. V. van Vlijmen, N. Pearce, P. Groot
- BiologyArzneimittel-Forschung
- 1 April 1998
The responsiveness to hypolipidaemic therapy combined with a clear relationship between aortic lesion size and plasma cholesterol exposure, as demonstrated previously, makes this mouse an attractive model for the testing of anti-atherosclerotic properties of hypolIPidaemic drugs.
ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme.
- A. Gribble, R. Dolle, J. Yates
- Biology, ChemistryJournal of Medicinal Chemistry
- 30 August 1996
A lead structural class of compound has been identified with the potential for modification into potent, cell-penetrant, and efficacious inhibitors of ATP-citrate lyase, which were able to inhibit cholesterol and/or fatty acid synthesis in HepG2 cells.
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