Results 61 to 70 of about 26,828 (241)

New pyridobenothiazolone derivatives display nanomolar pan‐serotype anti‐DENV activity

ChemMedChem, Accepted Article.
Dengue virus (DENV) serotypes 1–4 are mosquito‐borne flaviviruses that are responsible for significant morbidity and mortality worldwide, particularly in tropical and subtropical regions. Although two vaccines have been approved, their unbalanced efficacy across serotypes poses potential risks for specific populations.
Tommaso Felicetti, Chin Piaw Gwee, Kitti Wing Ki Chan, Giacomo Pepe, Ciro Milite, Pietro Campiglia, Satoru Watanabe, Muhammad Danial Bin Mohd Mazlan, Stefano Sabatini, Serena Massari, Oriana Tabarrini, Gianluca Sbardella, Subhash G. Vasudevan, Giuseppe Manfroni   +13 more
wiley   +1 more source

Multi-Slice Low-Rank Tensor Decomposition Based Multi-Atlas Segmentation: Application to Automatic Pathological Liver CT Segmentation [PDF]

arXiv, 2021
Liver segmentation from abdominal CT images is an essential step for liver cancer computer-aided diagnosis and surgical planning. However, both the accuracy and robustness of existing liver segmentation methods cannot meet the requirements of clinical applications.
arxiv  

Physiologically Based Pharmacokinetic Modeling to Predict Drug–Drug Interactions of Soticlestat as a Victim of CYP Induction and Inhibition, and as a Perpetrator of CYP and P–Glycoprotein Inhibition

Clinical Pharmacology in Drug Development, EarlyView.
Abstract Soticlestat (TAK‐935) is a cholesterol 24‐hydroxylase inhibitor. A physiologically‐based pharmacokinetic model has been developed to predict potential soticlestat drug–drug interactions (DDIs) using the Simcyp v20 Population‐based Simulator and verified with data from single‐/multiple‐rising‐dose and clinical DDI studies.
Hongxia Jia, T. Eric Ballard, Liming Zhang, Lawrence Cohen, Mackenzie C. Bergagnini‐Kolev, Ian E. Templeton, Hannah M. Jones, Wei Yin   +7 more
wiley   +1 more source

In vitro metabolism study of ADB‐P‐5Br‐INACA and ADB‐4en‐P‐5Br‐INACA using human hepatocytes, liver microsomes, and in‐house synthesized references

Drug Testing and Analysis, EarlyView.
Analyzing hepatocytes and liver microsomes samples along with synthesized references. Complete structure elucidation of major metabolites was possible, and biomarkers for both ADB‐P‐5Br‐INACA and ADB‐4en‐P‐5Br‐INACA were suggested. Abstract Synthetic cannabinoids (SCs) remain a major public health concern, as they continuously are linked to severe ...
Tobias Rautio, Robin Obrist, Lucas Krebs, Therése Klingstedt, Johan Dahlén, Xiongyu Wu, Henrik Gréen   +6 more
wiley   +1 more source

Analysis of in vitro and in vivo metabolism of zidovudine and gemfibrozil in trans‐chromosomic mouse line expressing human UGT2 enzymes

Pharmacology Research & Perspectives, 2022
UDP‐glucuronosyltransferases (UGTs) catalyze the conjugation of various substrates with sugars. Since the UGT2 family forms a large cluster spanning 1.5 Mb, transgenic mouse lines carrying the entire human UGT2 family have not been constructed because of
Kaoru Kobayashi, Tsuneo Deguchi, Satoshi Abe, Naoyo Kajitani, Kanako Kazuki, Shoko Takehara, Kazuomi Nakamura, Atsushi Kurihara, Mitsuo Oshimura, Yasuhiro Kazuki   +9 more
doaj   +1 more source

The di-flavoenzyme reductase directly activates oxygen for the metabolism of diverse drug molecules by liver microsomal Cytochrome P450s [PDF]

arXiv, 2006
This submission has been withdrawn by arXiv administration due to complaints of misuse of institutional affiliation.
arxiv  

E$^2$Net: An Edge Enhanced Network for Accurate Liver and Tumor Segmentation on CT Scans [PDF]

arXiv, 2020
Developing an effective liver and liver tumor segmentation model from CT scans is very important for the success of liver cancer diagnosis, surgical planning and cancer treatment. In this work, we propose a two-stage framework for 2D liver and tumor segmentation.
arxiv  

Identification of human metabolites of fast skeletal troponin activators Tirasemtiv and Reldesemtiv for doping control purposes

Drug Testing and Analysis, EarlyView.
The metabolism and urinary elimination of two substances recently classified as prohibited substances in sport was conducted, yielding suitable target analytes for efficient doping controls employing routinely applied chromatographic‐mass spectrometric test methods.
Luisa Euler, Kim Deinert, Felicitas Wagener, Katja Walpurgis, Mario Thevis   +4 more
wiley   +1 more source

Identification and interspecies characterization of UDP-glucuronosyltransferase isoforms catalyzing acacetin glucuronidation using recombinant UGT enzymes and microsomes

Journal of Traditional Chinese Medical Sciences, 2019
Objective: To explore the glucuronic acid metabolism of acacetin in human liver and intestinal microsomes to better characterize human uridine 5′-diphospho (UDP)-glucuronosyltransferase (UGT) isoforms. In addition, interspecies comparisons were performed
Kangle Shi, Shan Li, Qinggang Meng
doaj  

In Vitro Metabolism and In Vivo Pharmacokinetics Profiles of Hydroxy-α-Sanshool

Toxics
Hydroxy-α-sanshool (HAS) is the predominant active compound in Zanthoxylum bungeanum Maxim (ZBM). Our present work was aimed to explore the in vitro metabolism characteristics, and in vivo pharmacokinetic (PK) profile of HAS.
Jie Meng, Die Qian, Ruo-Lan Li, Wei Peng, Li Ai   +4 more
doaj   +1 more source