Topic
Lanosterol
About: Lanosterol is a research topic. Over the lifetime, 1239 publications have been published within this topic receiving 36737 citations. The topic is also known as: (3β)-lanosta-8,24-dien-3-ol & (3β,20R)-lanosta-8,24-dien-3-ol.
Papers published on a yearly basis
Papers
More filters
TL;DR: A cDNA encoding human lanosterol synthase, the enzyme responsible for the backbone formation step in sterol biosynthesis, was cloned by extensive application of PCRs and full nucleotide sequence of c DNA was obtained by a "rapid amplification of cDNA ends" (RACE) method.
Abstract: A cDNA encoding human lanosterol synthase, the enzyme responsible for the backbone formation step in sterol biosynthesis, was cloned by extensive application of PCRs. Five degenerate oligonucleotide primers (139S, 440S, 528A, 575A and 712A) corresponding to the homologous amino acid sequences among the known 2,3-oxidosqualene cyclase(OSC) were designed. PCR with one pair(440S and 528A) of five primers yielded a 285-bp fragment. PCRs with the primers based on the obtained fragment and the degenerate primers (139S and 712A) gave longer fragments. Finally, full nucleotide sequence of cDNA was obtained by a "rapid amplification of cDNA ends" (RACE) method.
37 citations
37 citations
TL;DR: The results demonstrate that the renal cortex is the primary site of mevalonic acid metabolism within the kidney and that the glomerulus is responsible for 95% of the mevalonate metabolized by the renal cerebral cortex.
37 citations
TL;DR: Saperconazole‐induced inhibition of ergosterol synthesis coincides with an accumulation of 14‐methylated sterols, which indicates that saperconazoles interferes with the cytochrome P‐450 (P‐450)‐dependent 14α‐demethylation of lanosterol and/or 24‐methylenedihydrolanosterol.
Abstract: The N-1-substituted triazole antifungal, saperconazole, is a potent inhibitor of ergosterol synthesis in Candida albicans, Aspergillus fumigatus and Trichophyton mentagrophytes. Fifty % inhibition is already achieved at nanomolar concentrations. The saperconazole-induced inhibition of ergosterol synthesis coincides with an accumulation of 14-methylated sterols, such as 24-methylenedihydrolanosterol, lanosterol, obtusifoliol, 14 alpha-methylfecosterol, 14 alpha-methylergosta-8,24(28)-dien-3 beta-6 alpha-diol and 14 alpha-methylergosta-5,7,22,24(28)-tetraenol. This indicates that saperconazole interferes with the cytochrome P-450 (P-450)-dependent 14 alpha-demethylation of lanosterol and/or 24-methylenedihydrolanosterol. Saperconazole forms stable drug-P-450-complexes by binding via its free triazole nitrogen to the heme iron and via its N-1 substituent to the apoprotein moiety. The triazole derivative is a highly selective inhibitor of the 14 alpha-demethylase in fungal cells. It is a poor inhibitor of the 14 alpha-demethylation of lanosterol in rat and human liver cells. Saperconazole is, at concentrations as high as 10 microM, devoid of effects on the P-450-dependent cholesterol side-chain cleavage and 11 beta-hydroxylase, 17,20-lyase,21-hydroxylase and aromatase. Saperconazole does not interfere with the 2 alpha, 6 alpha-, 6 beta- and 7 alpha-hydroxylations of testosterone in microsomes from male rat liver. At high concentrations (greater than 5 microM) an inhibition of the 16 beta-hydroxylations is seen.
36 citations
TL;DR: The Trypanosoma cruzi lanosterol synthase has now been cloned and the sequence shares with the T. brucei lanosterl synthase a tyrosine substitution for the catalytically important active-site threonine found in animal and fungal lanosterols synthases.
36 citations