Exploring the effect of intracellular loop 1 genetic variants in human ABCG2 on transport activity and protein abundance [0.03%]
人ABCG2胞内环1遗传变异体对其转运活性和蛋白丰度的影响研究
Noora Sjöstedt,Ritchie G M Timmermans,Marika Vieraankivi et al.
Noora Sjöstedt et al.
ABCG2 (breast cancer resistance protein, BCRP), can affect drug disposition, and thus, variation in the ABCG2 gene may alter drug exposure. We studied non-synonymous naturally occurring single-nucleotide variants (SNVs) in intracellular loo...
Functional assessment of immortalized human brain microvascular endothelial cells with different passage numbers: A case study for a prospective proposal on variability management of in vitro blood-brain barrier models [0.03%]
不同代次的人脑微血管内皮细胞系的功能评估：针对体外血脑屏障模型变异性管理的前瞻性提议的一个案例研究
Seiya Ohki,Mei Fukuda,Tomoyo Baba et al.
Seiya Ohki et al.
In vitro blood-brain barrier (BBB) models, primarily consisting of brain microvascular endothelial cells (BMEC), are expected to play pivotal roles in evaluating drug permeability into the brain. However, these models often exhibit function...
Population pharmacokinetics of brexpiprazole in Japanese healthy subjects and patients with schizophrenia [0.03%]
日本健康受试者和精神分裂症患者中的布雷哌唑人群药代动力学研究
Koushi Higashi,Tomohiro Sasaki,Kazuo Aoki et al.
Koushi Higashi et al.
Brexpiprazole, widely approved for the treatment of schizophrenia, is an atypical antipsychotic that modulates serotonin-dopamine activity. To better understand the pharmacokinetics (PK) of brexpiprazole in Japanese patients, a population P...
Future direction of animal alternative/microphysiological systems in drug discovery and development [0.03%]
替代动物模型/微生理系统在药物发现和开发中的未来方向
Hiroshi Arakawa,Kazuo Takayama
Hiroshi Arakawa
Advanced in vitro evaluation of drug-induced kidney injury using microphysiological systems in drug discovery and development [0.03%]
利用药物研发中的微生理系统进行先进的体外药物诱导肾损伤评价
Hiroshi Arakawa,Kohei Matsushita,Naoki Ishiguro
Hiroshi Arakawa
Drug-induced kidney injury (DIKI) is a major cause of acute kidney injury (AKI). Given concerns about animal welfare and the need for more accurate prediction of human events, there is an urgent need to develop an in vitro evaluation method...
Comprehensive invitro evaluation of the inhibitory effects of relatively high molecular weight peptides on drug-drug interaction-associated four liver transporters and its association with physicochemical properties [0.03%]
相对较高分子量肽对药物相互作用相关四种肝转运蛋白抑制作用的体外综合评价及其与理化性质的关系
Rika Ishikawa,Takashi Misawa,Yosuke Demizu et al.
Rika Ishikawa et al.
In recent years, advances in peptide synthesis have enabled the construction of relatively high molecular weight (Mw; >1 kDa) peptides using various types of amino acids (AAs), including proteinogenic/natural and nonnatural AAs. This advanc...
Establishment of endogenous canine MUC1 knock-out MDCKII cells using CRISPR-Cas9 and evaluation of drug permeation [0.03%]
使用CRISPR-Cas9建立内源性犬MUC1敲除MDCKII细胞系及药物渗透评价研究
Hisanao Kishimoto,Kaori Miyazaki,Moeko Omori et al.
Hisanao Kishimoto et al.
Most orally administered drugs are absorbed by simple diffusion across the intestinal epithelium. Monolayers of MDCKII cells and parallel artificial membrane permeability assay are widely used to evaluate simple diffusion as an in vitro mod...
Substrate inhibition potential of arachidonic acid on 14,15-epoxidation, a biological drug developmental target, mediated by recombinant human cytochrome P450 2J2 and 2C8 enzymes [0.03%]
花生四烯酸对重组人细胞色素P450 2J2和2C8酶介导的14,15-环氧合酶的底物抑制潜能：生物药物开发靶点
Ayaka Kojima,Masayuki Nadai,Hiroshi Yamazaki et al.
Ayaka Kojima et al.
Arachidonic acid is metabolized to biologically active (±)14(15)-epoxy-5Z,8Z,11Z-eicosatrienoic acid (14,15-EET), and suppression of this step is believed to be a drug developmental target in cancer treatment. Although the key 14,15-epoxid...
Opportunities for microphysiological systems from the view of Japanese industries [0.03%]
从日本产业的角度看微生理系统的机会
Hitoshi Naraoka,Takuma Iguchi,Kosuke Harada et al.
Hitoshi Naraoka et al.
Regulatory authorities and pharmaceutical companies in Europe and the United States have paid attention to microphysiological systems (MPS), and various consortia and academic societies have been established. They are actively working towar...
Advancements in Microphysiological systems: Exploring organoids and organ-on-a-chip technologies in drug development -focus on pharmacokinetics related organs [0.03%]
微生理系统研究进展：药物开发中类器官与芯片器官技术的应用——以药动学相关器官为重点
Hiroshi Kimura,Masaki Nishikawa,Naokata Kutsuzawa et al.
Hiroshi Kimura et al.
This study explored the evolving landscape of Microphysiological Systems (MPS), with a focus on organoids and organ-on-a-chip (OoC) technologies, which are promising alternatives to animal testing in drug discovery. MPS technology offers in...