Results 121 to 130 of about 31,417,423 (292)

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

The Natural Product Corramycin Acts as a DNA Gyrase Poison and Overcomes Fluoroquinolone Resistance in Mycobacterium tuberculosis

Advanced Science, EarlyView.
Corramycin, a myxobacterial natural product antibiotic, exhibits potent bactericidal activity against multidrug‐resistant Mycobacterium tuberculosis. The compound hijacks bacterial transporters such as BacA and OppABCD to enter the cell and inhibits DNA synthesis through a previously unrecognized mode of DNA gyrase poisoning, locking the enzyme in an ...
Franziska Fries, Jennifer Herrmann, Michael Dal Molin, Yaëlle Wormser, Timo Risch, Yunsheng Gao, Gareth Prosser, Francesca Gubellini, Ariel Mechaly, Joshua B. Wallach, Anthony Castro, Arka Banerjee, Sari Rasheed, Alexander Horn, Mathias Müsken, Michael Kurz, Lindsay Sonnenkalb, Viola Dreyer, Stefan Niemann, Sönke Andres, Dirk Schnappinger, Uli Kazmaier, Norbert Reiling, Rolf Müller, Jan Rybniker, Stéphanie Petrella   +25 more
wiley   +1 more source

Physiologically Based Pharmacokinetic Modeling of Antibiotics in Children: Perspectives on Model-Informed Precision Dosing

Antibiotics
The appropriate use of antibiotics is crucial and involves selecting an optimal dosing regimen based on pharmacokinetic (PK) and pharmacodynamic (PD) indicators.
Ryota Tanaka, Kei Irie, Tomoyuki Mizuno
doaj   +1 more source

Rocket‐Inspired Sequentially Targeted Nanotherapeutics for Mitochondrial Regulation and Inflammatory Reprogramming in Ischemic Stroke

Advanced Science, EarlyView.
A novel neutrophil‐hitchhiking, rocket‐inspired nanoplatform is developed to cross the blood‐brain barrier for sequential, spatiotemporal drug delivery. By responsive surface transformation in the ischemic penumbra, it precisely targets mitochondria to suppress Drp1‐mediated fission.
He Bai, Zihao Yong, Yang Li, Qingmin Chen, Yong Liu, Xiaomeng Guo, Fukai Li, Shicheng Tang, Zhuo Yang, Yufei Zhang, Ruwei Jie, Xiaohong Lv, Huacheng Wang, Chunming Huang, Liwei Xie, Jianqi Xiao, Qingchun Mu, Longguang Tang   +17 more
wiley   +1 more source

Physiologically‐based pharmacokinetic model of sparsentan to evaluate drug–drug interaction potential

CPT: Pharmacometrics & Systems Pharmacology
Sparsentan is a dual endothelin/angiotensin II receptor antagonist indicated to reduce proteinuria in patients with primary IgA nephropathy at high risk of disease progression. In vitro data indicate that sparsentan is likely to inhibit or induce various
Nikunjkumar K. Patel, Kuan‐Fu Chen, Shang‐Chiung Chen, Kai Liu   +3 more
doaj   +1 more source

A computer-aided framework for development, identification andmanagement of physiologically-based pharmacokinetic models

, 2014
The objective of this work is the development of a generic computer-aided modelling framework to support the development of physiologically-based pharmacokinetic models thereby increasing the efficiency and quality of the modelling process. In particular,
Linninger, Andreas, Sin, Gürkan, Heitzig, Martina, Gani, Rafiqul   +3 more
core   +1 more source

Rhoifolin Alleviates Ulcerative Colitis by Targeting NMNAT1 and Activating SIRT1‐FOXO1 Signaling to Enhance ILC3s Effector Function

Advanced Science, EarlyView.
Rhoifolin directly targets NMNAT1, thereby activating nicotinamide salvage pathway and promoting intracellular NAD+ biosynthesis. Elevated NAD+ levels enhance SIRT1 activity, leading to FOXO1 deacetylation and nuclear translocation. Nuclear FOXO1 subsequently binds to the IL‐22 promoter, upregulating IL‐22 transcription and potentiating ILC3 effector ...
Hongqiong Yang, Yishu Zhang, Sijia Feng, Xiaoqing Ma, Jiayi Feng, Junwei Wang, Jialin Gao, An Pan, Dapeng Wu, Kang Ding, Caijuan Zheng, Qi Lv, Lihong Hu   +12 more
wiley   +1 more source

Comparison of Quantum Dot Biodistribution with a Blood-Flow-Limited Physiologically Based Pharmacokinetic Model

, 2016
A physiologically based pharmacokinetic model with partition coefficients estimated from quantum dot (QD) 705 biodistribution was compared with the biodistribution of other QDs in mice and rats to determine the model’s predictive ability across QD types,
Hyun A. Lee (2393329), Nancy A. Monteiro-Riviere (1747501), Jim E. Riviere (1368789), Teresa L. Leavens (2393335), Sharon E. Mason (2393332)   +4 more
core   +1 more source

Lanthanum Carbonate Nanosheets Based Colloidal Hydrogel for Modulating Innate & Adaptive Tumor Immunotherapy by Augmented Cellular Pyroptosis

Advanced Science, EarlyView.
The Gela/decitabine/La2(CO3)3 colloidal (GDLC) hydrogel developed here could reverse the epigenetic silencing of the GSDME gene by the synergistic interaction between DAC and La3+, while concurrently activating caspase‐3, thus facilitating pyroptosis induction under the tumor microenvironment.
Yang Hong, Haitao Wu, Weitao Wang, Xuan Zhang, Qian Chen, Yaoyu Hu, Zhengbao Zha   +6 more
wiley   +1 more source

Nanoparticle‐Mediated TIPE1 mRNA Delivery Enhances Paclitaxel Sensitivity in Triple‐Negative Breast Cancer by Modulating RAB7A Ubiquitination‐Associated Stability and Autophagy

Advanced Science, EarlyView.
TIPE1m NPs nanoparticles restore TIPE1 expression, promote RAB7A ubiquitination and degradation, suppress autophagic flux, and resensitize paclitaxel‐resistant triple‐negative breast cancer to therapy. ABSTRACT Acquired paclitaxel (PTX) resistance remains a major obstacle in triple‐negative breast cancer (TNBC) treatment.
Wei Hu, Qishuai Chen, Yan Ma, Yang Liu, Xianing Dong, Wenjuan Wei, Jianxin Du, Shusheng Qiu, Maojin Tian, Peiqing Zhao   +9 more
wiley   +1 more source