Cytochrome P450 1A1 opens up to new substrates
نویسندگان
چکیده
منابع مشابه
Mechanism-based inhibition of human cytochrome P450 1A1 by rhapontigenin.
Recently we reported that resveratrol (trans-3,4',5-trihydroxystilbene) showed selective inhibition of recombinant human cytochrome P450 (P450) 1A1 in a concentration-dependent manner. The inhibition of recombinant human P450 1A1, 1A2, or 1B1 by various hydroxystilbene compounds having a similar structure to resveratrol was investigated using bacterial membranes from a human P450/NADPH-P450 red...
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The flavone backbone is a well-known pharmacophore present in a number of substrates and inhibitors of various P450 enzymes. In order to find highly potent and novel P450 family I enzyme inhibitors, an acetylene group was incorporated into six different positions of flavone. The introduction of an acetylene group at certain locations of the flavone backbone lead to time-dependent inhibitors of ...
متن کاملMethoxyestrogens exert feedback inhibition on cytochrome P450 1A1 and 1B1.
Cytochrome P450 1A1 (CYP1A1) and 1B1 (CYP1B1) catalyze the oxidative metabolism of 17 beta-estradiol (E2) to catechol estrogens (2-OHE2 and 4-OHE2) and estrogen quinones, which may lead to DNA damage. Catechol-O-methyltransferase catalyzes the methylation of catechol estrogens to methoxyestrogens (2-MeOE2, 2-OH-3-MeOE2, and 4-MeOE2), which simultaneously lowers the potential for DNA damage and ...
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OBJECTIVES Cytochrome P450 (CYP) 1A1 located in the membrane of endoplasmic reticulum is the most important enzyme in both activation and detoxification of carcinogenic benzo[a]pyrene (BaP), in combination with microsomal epoxide hydrolase (mEH). However, it is still not clearly explained how the electron transfer is mediated by NADPH:CYP oxidoreductase (POR), another component of the microsoma...
متن کاملStudy of Cytochrome P450 1A1 (T3801C) Single Nucleotide Polymorphism in Patients with Breast Cancer in Mazandaran Province-Northern Iran
Background: Breast cancer is the first leading cause of cancer-related death in women. Pesticides which are excessively used in northern Iran are one of the most important risk factors for breast cancer incidence. The cytochrome P450 1A1 (cyp1A1) is a key enzyme in xenobiotics metabolism and SNPs of its coding gene has been verified to be important in cancer susceptibility. The aim of thi...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2018
ISSN: 0021-9258
DOI: 10.1074/jbc.h118.006715