Zobrazeno 1 - 10
of 37
pro vyhledávání: '"J R, Halpert"'
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 29(9)
4-Vinyl-1-cyclohexene (VCH) is ovotoxic in B6C3F(1) mice but not in Fischer-344 rats, which can be partially attributed to greater formation of toxic epoxides from VCH in mice compared with rats. Since repeated exposure to VCH is necessary to cause o
Autor:
R, Eiselt, T L, Domanski, A, Zibat, R, Mueller, E, Presecan-Siedel, E, Hustert, U M, Zanger, J, Brockmoller, H P, Klenk, U A, Meyer, K K, Khan, Y A, He, J R, Halpert, L, Wojnowski
Publikováno v:
Pharmacogenetics. 11(5)
The genetic component of the inter-individual variability in CYP3A4 activity has been estimated to be between 60% and 90%, but the underlying genetic factors remain largely unknown. A study of 213 Middle and Western European DNA samples resulted in t
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 293(2)
The structural basis of cooperativity of progesterone hydroxylation catalyzed by human cytochrome P450 3A4 has been investigated. A recent study suggested that substitution of larger side chains at positions Leu-211 and Asp-214 partially mimics the a
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 290(3)
The structural basis for functional differences between human cytochrome P-450 2B6 and rat 2B1 was investigated. An amino acid sequence alignment predicted the location of 2B6 substrate recognition site (SRS) residues. Ten residues within these SRSs
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 290(2)
RPR 106541 (20R-16alpha,17alpha-[butylidenebis(oxy)]-6al pha, 9alpha-difluoro-11beta-hydroxy-17beta-(methylthio)androst a-4-en-3-one) is an airway-selective steroid developed for the treatment of asthma. Two metabolites produced by human liver micros
Autor:
S M, Strobel, G D, Szklarz, Y, He, M, Foroozesh, W L, Alworth, E S, Roberts, P F, Hollenberg, J R, Halpert
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 290(1)
Rabbit cytochromes P-450 (P-450) 2B4 and 2B5 differ by only 12 amino acid residues yet they exhibit unique steroid hydroxylation profiles. Previous studies have led to the identification of active site residues that are determinants of these specific
Autor:
J K, Doerr-Stevens, J, Liu, G J, Stevens, J C, Kraner, S M, Fontaine, J R, Halpert, I G, Sipes
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 27(2)
4-Vinylcyclohexene (VCH), an ovarian toxicant in mice, is known to irreversibly deplete ovarian follicles as a consequence of VCH diepoxide formation. Because ovotoxicity requires repeated dosing of VCH, the effect of consecutive daily doses of VCH (
Autor:
J R, Halpert, T L, Domanski, O, Adali, C P, Biagini, J, Cosme, E A, Dierks, E F, Johnson, J P, Jones, P, Ortiz de Montellano, R M, Philpot, O, Sibbesen, W K, Wyatt, Z, Zheng
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 26(12)
This article is a report on a symposium held at Experimental Biology '98 in San Francisco, California. Recent developments in site-directed mutagenesis, computer-modeling, and mechanistic analysis of cytochromes P450 and flavin-containing monooxygena
Autor:
J R, Halpert
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 26(12)
Autor:
G D, Szklarz, J R, Halpert
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 26(12)
Three-dimensional homology models of cytochromes P450 (P450) 2B1 and P450 3A4 have been utilized along with site-directed mutagenesis to elucidate the molecular determinants of substrate specificity. Most of the key residues identified in 2B enzymes