A5009508431- PARP inhibition in cancer therapy
- Wnt/β-catenin signaling in development and cancer
- Drug Solubulity and Delivery Systems
- Cholinesterase and Neurodegenerative Diseases
- Bioactive Compounds and Antitumor Agents
- Alzheimer's disease research and treatments
- Analytical Methods in Pharmaceuticals
- Calcium signaling and nucleotide metabolism
- Lipid metabolism and biosynthesis
- Advanced Drug Delivery Systems
- Gene expression and cancer classification
- Cancer therapeutics and mechanisms
- Drug Transport and Resistance Mechanisms
- Cryospheric studies and observations
- Inflammation biomarkers and pathways
- Immunotherapy and Immune Responses
- Microbial Metabolism and Applications
- Plant-Microbe Interactions and Immunity
- International Maritime Law Issues
- Marine Sponges and Natural Products
- Language, Discourse, Communication Strategies
- Cancer-related gene regulation
- Advanced Neuroimaging Techniques and Applications
- Genomics, phytochemicals, and oxidative stress
- Antibiotic Resistance in Bacteria
Jeil Pharmaceutical (South Korea)
2010-2021
Asan Medical Center
2017
Chungnam National University
2017
Korea Research Institute of Bioscience and Biotechnology
2001-2010
University of Manitoba
2008
Hiroshima University
1999-2002
The Janus kinase (JAK) family comprises four members (JAK1, JAK2, JAK3, and Tyk2) that play a key role in mediating cytokine receptor signaling. JAK inhibition thus modulates cytokine-mediated effects. In particular, selective of JAK1 or JAK3 may provide an efficient therapeutic agent for the treatment inflammatory diseases, with minimized side this study, as part our continued efforts to develop inhibitor, series 1,2-disubstituted benzimidazole-5-carboxamide derivatives was prepared their...
The influence of ethanolic extracts Brassica campestris spp. rapa roots (EBR) on obesity was examined in imprinting control region (ICR) mice fed a high-fat diet (HFD) and 3T3-L1 adipocytes. ICR used were divided into regular diet, HFD, EBR (50 mg/kg/day administered orally), orlistat (10 orally) groups. molecular mechanism the anti-obesity effect investigated adipocytes as well HFD-fed mice. In obese mouse model, both weight gain epididymal fat accumulation highly suppressed by daily oral...
Polyene macrolides such as nystatin A1 and amphotericin B belong to a large family of very valuable antifungal polyketide compounds typically produced by soil actinomycetes. Recently, nystatin-like Pseudonocardia polyene (NPP) has been identified unique disaccharide-containing tetraene macrolide autotrophica. Despite its significantly increased water solubility decreased hemolytic activity, activity remains limited compared with that A1. In this study, we developed NPP B1, novel derivative...
Summary Excessive activation of poly ( ADP ‐ribose) polymerase‐1 PARP ‐1) is known to develop neuronal apoptosis, necrosis and inflammation after ischaemic brain injury. Therefore, ‐1 inhibition stroke has been attempted in successful animal studies. The purpose present work was a novel water soluble inhibitor JPI ‐289) explore its neuroprotective effect on injury an vitro model. half‐life ‐289 intravenous or oral administration rats relatively long (1.4‐1.5 hours) with 65.6%...
The precise mechanisms of resistance to camptothecin (CPT)-derived DNA topoisomerase (topo I) inhibitors and the determinants remain unclear. We found that a repair protein, O(6)-methylguanine-DNA methyltransferase (MGMT), participated in irinotecan hydrochloride (CPT-11), its active metabolite SN-38, novel CPT derivative, DX-8951f. In 17 human cancer cell lines, MGMT gene expression level closely correlated with sensitivity derivatives, inhibition activity by nontoxic 5 microM...
Glycogen synthase kinase-3β (GSK-3β), a serine/threonine kinase also known as tau protein I, has been implicated in the pathogenic conditions of Alzheimer's disease. Many investigators have focused on GSK-3 inhibitor therapeutic drug. In this study, we established cell-based assay for screening novel GSK-3β inhibitors. For purpose, four-repeat cDNAs were stably expressed human embryonic kidney 293 (HEK293) cells (HEK293-Tau). The proliferation HEK293-Tau was no different from that HEK293...
3113 Background: JPI-547 is an oral inhibitor of PARP 1/2 and Tankyrase 1/2. demonstrated anti-tumor activity in BRCA-deficient xenograft models as a single-agent combination with chemotherapy immune checkpoint inhibitors. Methods: This the first human (FIH) phase I study patients (pts) advanced solid tumors. For dose escalation phase, 3+3 design was used 4 doses from 50 to 200 mg QD on 21-day cycles. Primary objectives were assess safety tolerability determine RP2D, secondary included...
A network composed of activation and inactivation pathways to regulate mitomycin C (MMC) action is suggested exist in human cancer cells. COLO201 colon cells were stably transfected with NQO1 cDNA that encodes NAD(P)H:quinone oxidoreductase (DT-diaphorase, DTD), a clonal cell line about 57-fold elevated DTD activity was obtained. Northern analysis revealed expression the NADPH:cytochrome P450 reductase (P450 reductase) gene decreased transfectant, COLO201/NQO1, associated increase...
Abstract Poly(ADP‐ribose) polymerase (PARP)‐1 plays an important role in the pathogenic mechanism of ischemic stroke. A number studies have been undertaken to develop PARP‐1 inhibitors for clinical use. We report on newly developed inhibitors, among which 12a showed good activity (IC 50 =7.8 nM enzyme‐based assay and=0.73 µM a cell‐based assay) and pharmacokinetic profiles. Treatment middle cerebral artery (MCA) occluded rats with 3 mg/kg reduced infarct volume suggesting that, may be...
Abstract Poly (ADP-ribose) Polymerase (PARP) plays a critical role in DNA repair processes. Small molecule inhibitors of PARP for the treatment cancer are currently being investigated either single agents or combination therapy with other damaging agents. Based on recent published data, have shown promising results as powerful therapeutic anticancer agents, especially tumors deficient BRCA-1or BRCA-2 function. In this study, we present novel synthetic inhibitor poly polymerase their...
Two thousand sixty-eight multi-purpose expression clones for the 326 candidate genes related to gastric or liver cancers were constructed using Gateway system. These can be expressed as His, Glutathione-S-transferase (GST) Enhanced version of green fluorescent protein (EGFP) fusion proteins in E. coli, insect cells mammalian cells. For 246 coli clones, GST had greater efficiency and solubility than His proteins. Approximately 20% unexpected molecular weights. A detailed sequence analysis...
Promoter trap mutagenesis was used to isolate an etoposide resistant CHO cell line. This CHO-K1 line, named E91, showed cross resistance C2-ceramide (N-acetylsphingosine) mediated killing. The promoter retrovirus integrated into intron one-two of the Dlc-2 (Stard13) RhoGap gene. E91 cells elevated GTP bound RhoA levels compared with parental line suggesting that integration had inactivated one alleles. To test if were impaired in intracellular ceramide-regulated process not directly related...
The R47H coding variant of the triggering receptor expressed on myeloid cells-2 (TREM2) increases risk Alzheimer's disease (AD) similar to apolipoprotein E4. TREM2 has recently been shown have impaired binding damage-associated lipid or ligands. However, it is not known how this affects biochemical characteristics and alters pathogenesis AD. Human wild type mutation was inserted into pcDNA5-FRT/TO-HA. All experiments involving transient transfection were performed using Lipofectamine 2000....
Indapamide (4-chloro-N-(2-methyl-1-indolinyl)-3-sulfamoyl-benz-amide) is an oral antihypertensive diuretic agent indicated for the treatment of hypertensive. The and natriuretic effects are mainly due to structure o-chlorobenzenesulfonamide. objective this study was formulate sustained release indapamide granules assess their formulation variables. Granules were prepared by fluid bed coating method consist drug layer membrane layer. coated with HPC ethyl cellulose along plasticizer dibuthyl...
Venlafaxine, 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl] cyclohexanol hydrochloride is a novel, nontricyclic antidepressant. venlafaxine unique antidepressant that differs structurally from other currently available. The aim ot the study was to formulate sustained-release granules and assess their formulation variables. It consists of two layers, drug layer sustained release coating manufactured by fluidized bed process. could be increased double-control rising various components in...