Results 11 to 20 of about 174,785 (211)

Ethynylflavones, highly potent, and selective inhibitors of cytochrome P450 1A1. [PDF]

Chem Res Toxicol, 2014
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.
Goyal N, Liu J, Lovings L, Dupart P, Taylor S, Bellow S, Mensah L, McClain E, Dotson B, Sridhar J, Zhang X, Zhao M, Foroozesh M.   +12 more
europepmc   +5 more sources

Cytochrome P450 Family 1 Inhibitors and Structure-Activity Relationships [PDF]

Molecules, 2013
With the widespread use of O-alkoxyresorufin dealkylation assays since the 1990s, thousands of inhibitors of cytochrome P450 family 1 enzymes (P450s 1A1, 1A2, and 1B1) have been identified and studied.
Jiawang Liu, Jayalakshmi Sridhar, Maryam Foroozesh   +2 more
doaj   +3 more sources

NADH:Cytochrome b5 Reductase and Cytochrome b5 Can Act as Sole Electron Donors to Human Cytochrome P450 1A1-Mediated Oxidation and DNA Adduct Formation by Benzo[a]pyrene. [PDF]

Chem Res Toxicol, 2016
Benzo[a]pyrene (BaP) is a human carcinogen that covalently binds to DNA after activation by cytochrome P450 (P450). Here, we investigated whether NADH:cytochrome b5 reductase (CBR) in the presence of cytochrome b5 can act as sole electron donor to human ...
Stiborová M, Indra R, Moserová M, Frei E, Schmeiser HH, Kopka K, Phillips DH, Arlt VM.   +7 more
europepmc   +3 more sources

Cytochrome P450 1A1 opens up to new substrates. [PDF]

J Biol Chem, 2018
The cytochromes P450 (CYPs) oxidatively transform a huge number of substrates in both prokaryotic and eukaryotic organisms, but the mechanisms by which they accommodate these diverse molecules remain unclear. A new study by Bart and Scott reports two co-crystal structures of CYP1A1 that reveal structural rearrangements and flexible interaction networks
Munro AW.
europepmc   +5 more sources

Melatonin Activation by Human Cytochrome P450 Enzymes: A Comparison between Different Isozymes

Molecules, 2023
Cytochrome P450 enzymes in the human body play a pivotal role in both the biosynthesis and the degradation of the hormone melatonin. Melatonin plays a key role in circadian rhythms in the body, but its concentration is also linked to mood fluctuations as
Thirakorn Mokkawes, Tamar De Visser, Yuanxin Cao, Sam P. De Visser   +3 more
doaj   +1 more source

Combinatorial targeting of G‐protein‐coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in drug‐induced liver injury

Hepatology, EarlyView., 2022
CHIN117 is a dual cysteinyl leukotriene receptor 1 (CYSLTR1) antagonist and G‐protein‐coupled bile acid receptor 1 (GPBAR1) agonist. In the liver, GPBAR1 and CYSLTR1 are coexpressed by liver sinusoidal endothelial cells (LSECs), HSCs, circulating monocytes/macrophages, and liver resident macrophages (Kupffer cells).
Michele Biagioli, Silvia Marchianò, Cristina di Giorgio, Rosalinda Roselli, Martina Bordoni, Rachele Bellini, Bianca Fiorillo, Valentina Sepe, Bruno Catalanotti, Chiara Cassiano, Maria Chiara Monti, Eleonora Distrutti, Angela Zampella, Stefano Fiorucci   +13 more
wiley   +1 more source

Generation of reactive oxygen species by polyenylpyrroles derivatives causes DNA damage leading to G2/M arrest and apoptosis in human oral squamous cell carcinoma cells. [PDF]

PLoS ONE, 2013
Oral squamous cell carcinoma (OSCC) accounts for 5.8% of all malignancies in Taiwan and the incidence of OSCC is on the rise. OSCC is also a common malignancy worldwide and the five-year survival rate remains poor. Therefore, new and effective treatments
Kuo-Feng Hua, Pei-Chun Liao, Zhanxiong Fang, Feng-Ling Yang, Yu-Liang Yang, Yi-Lin Chen, Yi-Chich Chiu, May-Lan Liu, Yulin Lam, Shih-Hsiung Wu   +9 more
doaj   +1 more source

LPS inhibits arginase-1 expression in macrophages by up-regulating activity of cytochrome P450 1A1 epoxidase

陆军军医大学学报, 2023
Objective To explore the regulative effect and mechanism of cytochrome P450 1A1 (CYP1A1) on regulating lipopolysaccharide (LPS)-induced arginase-1 (Arg-1) expression in macrophages. Methods After mouse macrophage-like cell line RAW264.7 (RAW) was treated
TIAN Lixing, ZHU Junyu, WAN Linghui, LIANG Huaping   +3 more
doaj   +1 more source

Heteroactivation of cytochrome P450 1A1 by teas and tea polyphenols [PDF]

British Journal of Pharmacology, 2005
We studied 7‐ethoxyresorufin deethylase as an index of cytochrome P4501A1 (CYP1A1) activity in liver microsomes from rats pretreated with 3‐methylcholanthrene. The enzyme had complex kinetics compatible with a multisite model. At 1 μM substrate, brewed black, green and white teas had complex effects on enzyme activity consisting of activation at low ...
Dana L, Anger, Maria-Alexandra, Petre, Denis J, Crankshaw   +2 more
openaire   +2 more sources

Inhibitory and inductive effects of 4- or 5-methyl-2-mercaptobenzimidazole, thyrotoxic and hepatotoxic rubber antioxidants, on several forms of cytochrome P450 in primary cultured rat and human hepatocytes

Toxicology Reports, 2020
Effects of 4-methyl-2-mercaptobenzimidazole (4-MeMBI) and 5-methyl-2- mercaptobenzimidazole (5-MeMBI) on cytochrome P450 (CYP) activity were examined in primary cultured rat hepatocytes.
Atsuko Miyajima, Yukie Kuroda, Kazue Sakemi-Hoshikawa, Makoto Usami, Katsuyoshi Mitsunaga, Tomohiko Irie, Yasuo Ohno, Momoko Sunouchi   +7 more
doaj   +1 more source