A5015493095- Drug Transport and Resistance Mechanisms
- Pharmacological Effects and Toxicity Studies
- Pharmacogenetics and Drug Metabolism
- Antibiotics Pharmacokinetics and Efficacy
- Helicobacter pylori-related gastroenterology studies
- Gastroesophageal reflux and treatments
- Chronic Lymphocytic Leukemia Research
- Chronic Myeloid Leukemia Treatments
- Amino Acid Enzymes and Metabolism
- PI3K/AKT/mTOR signaling in cancer
- Lipid metabolism and biosynthesis
- HIV/AIDS drug development and treatment
- Analytical Methods in Pharmaceuticals
- Bipolar Disorder and Treatment
- Protein Kinase Regulation and GTPase Signaling
- Cancer therapeutics and mechanisms
- Gastrointestinal motility and disorders
- Peroxisome Proliferator-Activated Receptors
- Pesticide Residue Analysis and Safety
- Malaria Research and Control
- Epilepsy research and treatment
- Signaling Pathways in Disease
- Drug-Induced Hepatotoxicity and Protection
- 3D Printing in Biomedical Research
- Neuropeptides and Animal Physiology
Korea Research Institute of Bioscience and Biotechnology
2018-2024
Korea University of Science and Technology
2022-2024
University of Pennsylvania
2022
Korea Research Institute of Chemical Technology
2011-2019
Daewoong Pharmaceutical (South Korea)
2015-2018
Seoul National University
2009-2018
Toho University
2018
RIKEN Center for Sustainable Resource Science
2018
Korea Institute of Toxicology
2017
Gachon University
2017
We investigated whether human serum albumin (HSA) in suspended hepatocytes would affect the uptake clearance of anionic drugs with high binding to HSA and improve extrapolation vivo hepatic from vitro by via "albumin-mediated" mechanism. The clearances for total forms (<i>PS</i><sub>inf</sub>) unbound (<i>PS</i><sub>u,inf</sub>) 11 [all which were organic anion-transporting polypeptide (OATP) substrates] determined varying concentrations HSA. fraction (<i>f</i><sub>u</sub>) was using an...
Directed differentiation of hPSCs and transition from 3D intestinal organoids into functional hIECs.
The blood-brain-barrier (BBB) is made up of blood vessels whose permeability enables the passage some compounds. A predictive model BBB important in early stages drug development. predicted permeabilities drugs have been confirmed using a variety vitro methods to reduce quantities candidates needed preclinical and clinical trials. Most prior studies relied on animal or cell-culture models, which do not fully recapitulate human BBB. development microfluidic models human-derived cells could...
The objective of this study was to evaluate the permeability small molecules into brain via blood–brain barrier in zebrafish and investigate possibility using animal model as a screening tool during early stages drug discovery. Fifteen compounds were used understand permeation mice. ratio brain-to-plasma concentration compared between two models. partition coefficient (Kp,brain), estimated at designated times (0.167, 0.25, 0.5, or 2 h) after oral administrations (per os, p.o), ranged from...
A macrocyclic peptide scaffold with well-established structure-property relationship is desirable for tackling undruggable targets. Here, we adopted a natural macrocycle, cyclosporin O (
The increased use of plastics has led to severe environmental pollution, particularly by microplastics-plastic particles 5 mm or less in diameter. These are formed factors such as weathering and ultraviolet irradiation, thereby making pollution worse. This intensifies human exposure microplastics via food chains. Despite potential negative effects, few toxicity assessments on available. In this study, two sizes polytetrafluoroethylene (PTFE) microplastics, approximately μm 10-50 μm, were...
Decursinol is a major coumarin derived from the roots of Angelica gigas and has various pharmacological effects against inflammation, angiogenesis, nociceptive pain Alzheimer's disease. In vitro in vivo studies were conducted to characterize metabolism pharmacokinetics decursinol.Decursinol exhibited high stability oxidative glucuronic human rat liver microsomes.In Caco-2 cell monolayers, decursinol showed permeability (>14 × 10−6 cm/s) at all tested concentrations absorptive direction,...
Enavogliflozin is a sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor approved for clinical use in South Korea. As SGLT2 inhibitors are treatment option patients with diabetes, enavogliflozin expected to be prescribed various populations. Physiologically based pharmacokinetic (PBPK) modelling can rationally predict the concentration-time profiles under altered physiological conditions. In previous studies, one of metabolites (M1) appeared have metabolic ratio between 0.20 and 0.25....
This study aimed to characterise the pharmacokinetics of lurasidone, a new atypical anti-psychotic drug, in rats after intravenous and oral administration at dose range 0.5–2.5 2.5–10 mg/kg, respectively. Moreover, tissue distribution, liver microsomal stability plasma protein binding were estimated.
The potential inhibitory effect of quercetin, a major plant flavonol, on breast cancer resistance protein (BCRP) activity was investigated in this study. presence quercetin significantly increased the cellular accumulation and associated cytotoxicity BCRP substrate mitoxantrone human cervical cells (HeLa cells) concentration-dependent manner. transcellular efflux prazosin, stereotypical substrate, also reduced bidirectional transport assay using BCRP-overexpressing cells; further kinetic...
Scytonemin is a yellow-green ultraviolet sunscreen pigment present in different genera of aquatic and terrestrial blue-green algae, including marine cyanobacteria. In the study, anti-inflammatory activities scytonemin were evaluated vitro vivo. Topical application inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear swelling BALB/c mice. The expression tumor necrosis factor-α (TNF-α) inducible nitric oxide synthase (iNOS) was also suppressed by treatment TPA-treated addition,...
ABSTRACT: Twenty‐three powdered foods and ingredients were subjected to 2 treatments: temperature scan from ‐20 110 °C within hours, storage at 37 55 for 60 d. During scans, the spin‐spin relaxation time T values of individual samples determined using a nuclear magnetic resonance (NMR) technique, resulting in temperature‐T curve each sample. Four typical patterns identified found be closely related physical changes samples, including agglomeration, water vaporization, caking observed during...
Polo-like kinase-1 (Plk1) plays a key role in mitosis and has been identified as an attractive anticancer drug target. Plk1 consists of two drug-targeting sites, namely, N-terminal kinase domain (KD) C-terminal polo-box (PBD). As KD-targeting inhibitors are associated with severe side effects, here we report on the pyrazole-based PBD inhibitor, KBJK557, which showed remarkable vitro effect by inducing delocalization, mitotic arrest, apoptosis HeLa cells. Further, vivo optical imaging...
The clustered regularly interspaced short palindromic repeats (CRISPR)-Cas12a system is composed of a Cas12a effector that acts as DNA-cleaving endonuclease and crispr RNA (crRNA) guides the to target DNA. It considered key molecule for inducing target-specific gene editing in various living systems. Here, we improved efficiency specificity CRISPR-Cas12a through protein crRNA engineering. In particular, optimize at molecular level, used chimeric DNA-RNA guide chemically similar maximize...
A liquid chromatography-mass spectrometry (LC-MS) assay was developed and validated for the quantification of cilnidipine, a calcium channel antagonist, in human plasma. Plasma samples were processed by liquid-liquid extraction analyte, along with nimodipine (an internal standard), analyzed using selected ion monitoring (SIM) detection. The absolute recovery determined to be not less than 89.1% various concentrations. detector response specific linear cilnidipine concentrations range 0.5–50...
Fexuprazan is a new drug candidate in the potassium-competitive acid blocker (P-CAB) family. As proton pump inhibitors (PPIs), P-CABs inhibit gastric secretion and can be used to treat acid-related disorders such as gastroesophageal reflux disease (GERD). Physiologically based pharmacokinetic (PBPK) models predict interactions profiles biological matrices mechanistically simulated. Here, we propose an optimized validated PBPK model for fexuprazan by integrating vitro, vivo, silico data. The...
Olaparib is a first-in-class poly (ADP-ribose) polymerase oral inhibitor used to treat various tumors. In this study, we clarified the roles of ABCB1/Abcb1 and ABCG2/Abcg2 transporters in restricting olaparib distribution brain. was efficiently transported by human ABCG2, ABCB1, mouse Abcg2 vitro. vivo disposition study using single or combination knockout mice, systemic exposure did not differ significantly between strains over an 8-h period. However, brain-to-plasma unbound concentration...