Results 31 to 40 of about 5,044 (130)
ABSTRACT Background The phosphoinositide 3‐kinase (PI3K)/protein kinase B (PKB or AKT)/mammalian target of rapamycin (mTOR) signaling pathway (PAM pathway) plays a critical role in breast cancer pathogenesis and progression, and is closely linked with resistance to endocrine therapy in advanced breast cancer.
The Breast Cancer Expert Committee of the National Quality Control Center for Cancer +3 more
wiley +1 more source
Regulation of human CYP2C9 expression by electrophilic stress involves AP-1 activation and DNA looping [PDF]
CYP2C9 and CYP2C19 are important human enzymes that metabolize therapeutic drugs, environmental chemicals and physiologically important endogenous compounds.
Goldstein, J. A. +4 more
core +1 more source
The downregulation of ADH4 expression induces hepatocyte apoptosis, thereby contributing to liver fibrosis and the initiation of hepatocellular carcinoma (HCC). Moreover, sustained suppression of ADH4 in HCC cells disrupts retinoic acid synthesis, leading to reduced expression of the Wnt/β‐catenin signaling inhibitor WIF‐1 via RARs/RXRs‐mediated ...
Jiaying Li +10 more
wiley +1 more source
Genetic Variation in the CYP2C Monooxygenase Enzyme Subfamily Shows No Association With Longevity in a German Population [PDF]
Cytochrome P450 enzymes, especially the CYP2C subfamily, are involved in the generation of reactive oxygen species and are regarded as susceptibility factors for age-related diseases.
Flachsbart, Friederike +5 more
core
Marked increase in etravirine and saquinavir plasma concentrations during atovaquone/proguanil prophylaxis [PDF]
The case of a 32-year-old Caucasian female with multi-drug resistant HIV-1 subtype B infection treated with a salvage regimen including maraviroc, raltegravir, etravirine and unboosted saquinavir who started atovaquone/proguanil prophylaxis, is reported.
Chiara Tommasi +8 more
core +2 more sources
ABSTRACT Background Etrasimod is an oral, once‐daily (q.d.), selective sphingosine 1‐phosphate (S1P)1,4,5 receptor modulator for the treatment of moderately to severely active ulcerative colitis (UC). Unlike the S1P receptor modulator ozanimod, etrasimod does not have a molecular structure to inhibit monoamine oxidase (MAO).
Anita Afzali +12 more
wiley +1 more source
Endogenous and xenobiotic metabolic stability of primary human hepatocytes in long-term 3D spheroid cultures revealed by a combination of targeted and untargeted metabolomics [PDF]
Adverse reactions or lack of response to medications are important concerns for drug development programs. However, faithful predictions of drug metabolism and toxicity are difficult because animal models show only limited translatability to humans ...
Beck, Olof +7 more
core +1 more source
Abstract Fezolinetant is an oral, nonhormonal, neurokinin 3 receptor antagonist treatment option for moderate to severe vasomotor symptoms associated with menopause. An in vitro study using human recombinant cytochrome P450 (CYP) enzymes and human liver microsomes showed that fezolinetant is metabolized to its major but inactive metabolite, ES259564 ...
Megumi Iwai +8 more
wiley +1 more source
Cytochrome P450 inhibition potential of new psychoactive substances of the tryptamine class [PDF]
New psychoactive substances (NPS) are not tested for their cytochrome P450 (CYP) inhibition potential before consumption. Therefore, this potential was explored for tryptamine-derived NPS (TDNPS) including alpha-methyl tryptamines (AMTs), dimethyl ...
Brandt, SD +4 more
core +1 more source
This study showcases a novel artificial intelligence (AI)‐driven design strategy for constructing highly specific and orally‐active fluorogenic substrates for imaging CYP3A4 in complex biological systems, while NFa emerged as a practical and reliable tool for sensing and imaging of CYP3A4 activity thus facilitating CYP3A4‐associated fundamental ...
Feng Zhang +13 more
wiley +1 more source

