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Farnesyltransferase inhibitors versus Ras inhibitors

Current Opinion in Chemical Biology, 1997
Over the past few years, the idea that farnesyl-protein transferase (FPTase) inhibitors might be effective antiproliferative/antitumor agents has been realized in studies of cultured cells and in rodent models of cancer. Most of the studies with FPTase inhibitors have focused on inhibiting the growth of ras-transformed cells in vitro or the growth of ...
J B, Gibbs   +6 more
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Sirtuin inhibitors

Expert Opinion on Therapeutic Patents, 2009
The sirtuin family of deacetylase enzymes comprises seven proteins (SIRT1-7) that are dependent on NAD(+) for their activity. Three proteins are located in the nucleus, three in the mitochondria and only one is predominantly cytoplasmic. Caloric restriction and oxidative stress generally up-regulate their expression. SIRT1, the orthologue of yeast Sir2,
Francisco J, Alcaín, José M, Villalba
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Renin Inhibitors

Pharmaceutical Research, 1987
Since the early 1980s, an intensive effort has been focused on the development of orally effective and long-acting inhibitors of renin. During this time, in vitro potency has increased greatly, with several transition-state inhibitor designs yielding inhibitors with subnanomolar IC50 values.
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PCSK9 inhibitors

Current Opinion in Lipidology, 2013
To summarize the therapeutic strategies to inhibit PCSK9 and to describe the main results obtained in phase I and II trials with monoclonal antibodies targeting PCSK9.Among the various approaches for PCSK9 inhibition, human data are only available for inhibition of PCSK9 binding to LDL receptor by monoclonal antibodies.
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SGLT2 inhibitors

Biochemical Pharmacology, 2016
Diabetes mellitus is a serious health issue and an economic burden, rising in epidemic proportions over the last few decades worldwide. Although several treatment options are available, only half of the global diabetic population achieves the recommended or individualized glycemic targets.
I, Dardi, T, Kouvatsos, S A, Jabbour
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