منابع مشابه
Dual dehydrosqualene/squalene synthase inhibitors: leads for innate immune system-based therapeutics.
With the rapid rise in bacterial drug resistance, there is great interest in developing innovative approaches to anti-infective therapy. For example, in the United States, more people die from Staphylococcus aureus infections than die from human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS). Alternative approaches are thus of interest, and as discussed in a recent Natio...
متن کاملSqualene synthase inhibitors suppress triglyceride biosynthesis through the farnesol pathway in rat hepatocytes.
We recently demonstrated that squalene synthase (SQS) inhibitors reduce plasma triglyceride through an LDL receptor-independent mechanism in Watanabe heritable hyperlipidemic rabbits (Hiyoshi et al. 2001. Eur. J. Pharmacol. 431: 345-352). The present study deals with the mechanism of the inhibition of triglyceride biosynthesis by the SQS inhibitors ER-27856 and RPR-107393 in rat primary culture...
متن کاملThe squalestatins, novel inhibitors of squalene synthase produced by a species of Phoma. III. Biosynthesis.
The biosynthetic origin of the carbon and oxygen atoms of the novel fungal secondary metabolite 1 was studied. Incorporation studies with single and multiple labelled 13C precursors indicated that the major portion of the molecule was derived from two polyketide chains made up of acetate units. One of the chains had benzoic acid (which can be derived from phenylalanine) as a starter unit. The r...
متن کاملBiphenylquinuclidines as inhibitors of squalene synthase and growth of parasitic protozoa.
In this paper we describe the preparation of some biphenylquinuclidine derivatives and their evaluation as inhibitors of squalene synthase in order to explore their potential in the treatment of the parasitic diseases leishmaniasis and Chagas disease. The compounds were screened against recombinant Leishmania major squalene synthase and against Leishmania mexicana promastigotes, Leishmania dono...
متن کاملAccumulation of Squalene in a Microalga Chlamydomonas reinhardtii by Genetic Modification of Squalene Synthase and Squalene Epoxidase Genes
Several microalgae accumulate high levels of squalene, and as such provide a potentially valuable source of this useful compound. However, the molecular mechanism of squalene biosynthesis in microalgae is still largely unknown. We obtained the sequences of two enzymes involved in squalene synthesis and metabolism, squalene synthase (CrSQS) and squalene epoxidase (CrSQE), from the model green al...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2003
ISSN: 0007-1188
DOI: 10.1038/sj.bjp.0705331