Results 91 to 100 of about 6,868,569 (338)

A mismatch in enzyme-redox partnerships underlies divergent cytochrome P450 activities between human hepatocytes and microsomes

Communications Biology
NADPH-P450 oxidoreductase (POR) is the accepted redox-partner for drug-metabolising cytochrome P450s (CYPs) over NADH-cytochrome b 5 reductase (Cytb 5 R).
Tashinga E. Bapiro, Scott Martin, Thomas S. Blacker, Stephen D. Wilkinson, Alexandra L. Orton, Niresh Hariparsad, Rhys D. O. Jones, Michael R. Duchen, Stephanie Harlfinger   +8 more
doaj   +1 more source

Metabolic regulation of regulatory T cell development and function [PDF]

, 2014
It is now well established that the effector T cell (Teff) response is regulated by a series of metabolic switches. Quiescent T cells predominantly require ATP-generating processes, whereas proliferating Teff require high metabolic flux through growth ...
Alves, Barbi, Battaglia, Bental, Borsellino, Carr, Cipolletta, Cobbold, Coloff, Cunningham, Curti, Cybulski, Dang, Deiuliis, Delgoffe, Delgoffe, Feuerer, Fisson, Fox, Frauwirth, GabryÅ¡ová, Greiner, Guertin, Guertin, Gulen, Hardie, Hardie, Howie, Hörig, Jacobs, Jones, Jordan, Kane, Lee, Lord, Makki, Matarese, Matteoli, Mellor, Metz, Michalek, Munder, Munder, Oh, Olefsky, Ouchi, Peter, Powell, Powell, Powell, Powell, Procaccini, Procaccini, Sakaguchi, Sarbassov, Shevach, Shi, Sitkovsky, Smith, Thornton, Vanasek, Vander Heiden, Vukmanovic-Stejic, Waickman, Wieman, Winer, Yang, Zeng, Zheng   +68 more
core   +2 more sources

Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system

FEBS Letters, EarlyView.
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley   +1 more source

Simultaneously Predicting the Pharmacokinetics of CES1-Metabolized Drugs and Their Metabolites Using Physiologically Based Pharmacokinetic Model in Cirrhosis Subjects

Pharmaceutics
Hepatic carboxylesterase 1 (CES1) metabolizes numerous prodrugs into active ingredients or direct-acting drugs into inactive metabolites. We aimed to develop a semi-physiologically based pharmacokinetic (semi-PBPK) model to simultaneously predict the ...
Xin Luo, Zexin Zhang, Ruijing Mu, Guangyu Hu, Li Liu, Xiaodong Liu   +5 more
doaj   +1 more source

Modeling hepatic fibrosis in TP53 knockout iPSC‐derived human liver organoids

Molecular Oncology, EarlyView.
This study developed iPSC‐derived human liver organoids with TP53 gene knockout to model human liver fibrosis. These organoids showed elevated myofibroblast activation, early disease markers, and advanced fibrotic hallmarks. The use of profibrotic differentiation medium further amplified the fibrotic signature seen in the organoids.
Mustafa Karabicici, Soheil Akbari, Ceyda Caliskan, Canan Celiker, Ozden Oz, Leman Binokay, Gökhan Karakulah, Serif Senturk, Esra Erdal   +8 more
wiley   +1 more source

DMET™ (Drug Metabolism Enzymes and Transporters): a pharmacogenomic platform for precision medicine

OncoTarget, 2016
In the era of personalized medicine, high-throughput technologies have allowed the investigation of genetic variations underlying the inter-individual variability in drug pharmacokinetics/pharmacodynamics.
M. Arbitrio, M. T. Martino, F. Scionti, Giuseppe Agapito, P. Guzzi, M. Cannataro, P. Tassone, P. Tagliaferri   +7 more
semanticscholar   +1 more source

Clinical application of high throughput molecular screening techniques for pharmacogenomics. [PDF]

, 2011
Genetic analysis is one of the fastest-growing areas of clinical diagnostics. Fortunately, as our knowledge of clinically relevant genetic variants rapidly expands, so does our ability to detect these variants in patient samples.
Schrijver, Iris, Wiita, Arun P
core   +1 more source

A synthetic benzoxazine dimer derivative targets c‐Myc to inhibit colorectal cancer progression

Molecular Oncology, EarlyView.
Benzoxazine dimer derivatives bind to the bHLH‐LZ region of c‐Myc, disrupting c‐Myc/MAX complexes, which are evaluated from SAR analysis. This increases ubiquitination and reduces cellular c‐Myc. Impairing DNA repair mechanisms is shown through proteomic analysis.
Nicharat Sriratanasak, Bodee Nutho, Worawat Wattanathana, Narumon Phaonakrop, Bunnatut Panasawatwong, Katharina Erlenbach‐Wuensch, Sittiruk Roytrakul, Regine Schneider‐Stock, Pithi Chanvorachote   +8 more
wiley   +1 more source

Adipocyte and lipid metabolism in cancer drug resistance.

Journal of Clinical Investigation, 2019
Development of novel and effective therapeutics for treating various cancers is probably the most congested and challenging enterprise of pharmaceutical companies.
Yihai Cao
semanticscholar   +1 more source

Class IIa HDACs forced degradation allows resensitization of oxaliplatin‐resistant FBXW7‐mutated colorectal cancer

Molecular Oncology, EarlyView.
HDAC4 is degraded by the E3 ligase FBXW7. In colorectal cancer, FBXW7 mutations prevent HDAC4 degradation, leading to oxaliplatin resistance. Forced degradation of HDAC4 using a PROTAC compound restores drug sensitivity by resetting the super‐enhancer landscape, reprogramming the epigenetic state of FBXW7‐mutated cells to resemble oxaliplatin ...
Vanessa Tolotto, Nicolò Gualandi, Ylenia Cortolezzis, Raffaella Picco, Monica Colitti, Francesca D'Este, Mariachiara Gani, Wayne W. Hancock, Giovanni Terrosu, Cristina Degrassi, Francesca Agostini, Claudio Brancolini, Luigi E. Xodo, Eros Di Giorgio   +13 more
wiley   +1 more source