Results 61 to 70 of about 361,016 (249)

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

Prediction of Metabolite‐to‐Parent Drug Exposure: Derivation and Application of a Mechanistic Static Model

Clinical and Translational Science, 2020
In the development of new drugs, the prediction of metabolite‐to‐parent plasma exposure ratio in humans prior to administration in a clinical study has emerged as an important need.
Ernesto Callegari, Manthena V.S. Varma, R. Scott Obach   +2 more
doaj   +1 more source

Unraveling the Heterogeneity of Cargo Distribution in the Exogenous Association of Proteins With Extracellular Vesicles

Advanced Healthcare Materials, EarlyView.
We characterized the distribution of cargo proteins associated with extracellular vesicles using various exogenous loading methods. In all cases, single‐particle analysis revealed that the distribution of protein content per EV is heterogeneous, following an exponential decay function.
Karl Normak, Marcell Papp, Carolina Paganini, Andrea Zendrini, Paolo Bergese, Dorothea Pinotsi, Paolo Arosio   +6 more
wiley   +1 more source

Effects of ginkgo leaf tablet on the pharmacokinetics of rosiglitazone in rats and its potential mechanism [PDF]

, 2022
Xueting Xing, Mengzhu Kong, Qiaoyu Hou, Jiaqi Li, Wen Qian, Xijing Chen, Hanhan Li, Chang-qing Yang   +7 more
openalex   +1 more source

Mechanical and Electrical Phenotype of hiPSC‐Cardiomyocytes on Fibronectin‐Based Hydrogels

Advanced Healthcare Materials, EarlyView.
We introduce fibronectin‐based PEG hydrogels with controlled rigidity to enable the culture of iPSC‐derived cardiomyocytes. These substrates offer an alternative to the current culture of these cells on fibronectin‐coated glass, providing enhanced structural and functional behavior. The system provides a more physiologically relevant platform to assess
Ana Da Silva Costa, Lineta Stonkute, Sara Trujillo, Mariana Azevedo Gonzalez Oliva, Francis Burton, Matthew J. Dalby, Oana Dobre, Godfrey Smith, Manuel Salmeron‐Sanchez   +8 more
wiley   +1 more source

Targeted treatment for neuroblastoma using methoxyestradiol (2-ME)-loaded mitochondria-targeting immunoliposomes modified by datuximab (anti-GD2) and (L-cyclohexyl alanine-D-arginine)3 ((Fx,r)3) peptide

Cancer Nanotechnology
The 2-ME therapy encounters significant challenges in practical use. Its low water solubility compromises bioavailability, limiting drug efficacy. In addition, poor stability in the physiological environment hinders sustained therapeutic effects, and ...
Mingyu Wan, Zhili Chen, Yueyi Deng, Robert J. Lee, Chengyun Yan   +4 more
doaj   +1 more source

REV-ERBα integrates colon clock with experimental colitis through regulation of NF-κB/NLRP3 axis

Nature Communications, 2018
REV-ERBα is a nuclear receptor that links the circadian pathways with those of metabolism. Here the authors show REV-ERBα is also involved with linking the circadian system with the inflammatory pathways of an experimental model of colitis through ...
Shuai Wang, Yanke Lin, Xue Yuan, Feng Li, Lianxia Guo, Baojian Wu   +5 more
doaj   +1 more source

Photoactivated Proximity Protein Labeling Reveals Enhanced Tumor Retention of a D‐Peptide‐Ruthenium Prodrug Conjugate

Advanced Healthcare Materials, EarlyView.
Six stereoisomeric ruthenium‐peptide conjugates were synthesized and characterized, which showed high potential in photoactivated chemotherapy (PACT) and proximity protein labeling. Abstract Amino acid chirality is known to influence the biological properties of peptide‐containing prodrugs.
Liyan Zhang, Peiyuan Wang, Hildert Bronkhorst, Yurii Husiev, Ludovic Bretin, Maarten N. van Ginkel, Wen Sun, Sylvestre Bonnet   +7 more
wiley   +1 more source

Kinetic measurements of membrane target level and on-cell binding of biotherapeutic antibodies using flow-cytometry

AAPS Open
Characterization of cell surface target expression is critical for the development of therapeutics that bind membrane proteins or use changes in target abundance as efficacy biomarkers.
Daniel T. Doty, Mahua Roy, Phanidhar Kukutla, Nicholas Lucarelli, Peter E. Struss, Lindsay E. King, Jeffrey R. Chabot, Jatin Narula, Hendrik Neubert, Polina Goihberg   +9 more
doaj   +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