A5086497721- Viral Infections and Immunology Research
- Hepatitis C virus research
- Hepatitis B Virus Studies
- HIV/AIDS drug development and treatment
- Viral gastroenteritis research and epidemiology
- RNA and protein synthesis mechanisms
- Respiratory viral infections research
- Animal Virus Infections Studies
- Mosquito-borne diseases and control
- Synthesis and biological activity
- Malaria Research and Control
- RNA regulation and disease
- Viral Infections and Vectors
- Monoclonal and Polyclonal Antibodies Research
- Cytomegalovirus and herpesvirus research
- HIV Research and Treatment
- Synthesis and Characterization of Heterocyclic Compounds
- Peroxisome Proliferator-Activated Receptors
- T-cell and Retrovirus Studies
- Quinazolinone synthesis and applications
- Cytokine Signaling Pathways and Interactions
- Immune Response and Inflammation
- Influenza Virus Research Studies
- Neuroinflammation and Neurodegeneration Mechanisms
- Protein purification and stability
National Health Research Institutes
2010-2022
Pharmaceutical Biotechnology (Czechia)
2004-2010
Chang Gung University
2002-2005
Dengue virus (DENV) causes disease globally, with an estimated 25 to 100 million new infections per year. At present, no effective vaccine is available, and treatment supportive. In this study, we identified BP2109, a potent selective small-molecule inhibitor of the DENV NS2B/NS3 protease, by high-throughput screening assay using recombinant protease complex consisting central hydrophilic portion NS2B N terminus domain. BP2109 inhibited (serotypes 1 4), but not Japanese encephalitis (JEV),...
Dengue virus (DENV) causes disease globally, resulting in an estimated 25 to 100 million new infections per year. No effective DENV vaccine is available, and the current treatment only supportive. Thus, there urgent need develop therapeutic agents cure this epidemic disease. In present study, we identified a potential small-molecule inhibitor, BP13944, via high-throughput screening (HTS) of 60,000 compounds using stable cell line harboring efficient luciferase replicon serotype 2 (DENV-2)....
When skeletons of Win compounds were used as templates, computer-assisted drug design led to the identification a novel series imidazolidinone derivatives with significant antiviral activity against enterovirus 71 (EV 71), infection which had resulted in about 80 fatalities during 1998 epidemic outbreak Taiwan. In addition inhibiting all genotypes (A, B, and C) EV submicromolar low micromolar range, 1 8 extensively evaluated variety viruses, showing potent coxsackievirus A9 (IC50 = 0.47−0.55...
ABSTRACT Enterovirus 71 (EV71) has emerged as an important virulent neurotropic enterovirus in young children. DTriP-22 (4{4-[(2-bromo-phenyl)-(3-methyl-thiophen-2-yl)-methyl]-piperazin-1-yl}-1-pheny-1 H -pyrazolo[3,4- d ]pyrimidine) was found to be a novel and potent inhibitor of EV71. The molecular target this compound identified by analyzing DTriP-22-resistant viruses. A substitution lysine for Arg163 EV71 3D polymerase rendered the virus drug resistant. exhibited ability inhibit viral...
Enterovirus A71 (EV-A71), a positive-stranded RNA virus of the Picornaviridae family, may cause neurological complications or fatality in children. We examined specific factors responsible for this virulence using chemical genetics approach. Known compounds from an anti-EV-A71 herbal medicine, Salvia miltiorrhiza (Danshen), were screened anti-EV-A71. identified natural product, rosmarinic acid (RA), as potential inhibitor EV-A71 by cell-based antiviral assay and vivo mouse model. Results...
Enterovirus 71 is one of the most important pathogens in family Picornaviridae that can cause severe complications postpoliovirus era, such as encephalitis, pulmonary edema, and even death. Pyridyl imidazolidinone a novel class potent selective human enterovirus inhibitor. was identified by using computer-assisted drug design. This virologic investigation demonstrates BPR0Z-194, pyridyl imidazolidinones, targets capsid protein VP1. Time course experiments revealed BPR0Z-194 effectively...
A series of pyridylimidazolidinone derivatives was synthesized and tested in vitro against enterovirus 71 (EV71). On the basis compound 33 (DBPR103), introduction a methyl group at 2- or 3-position linker between imidazolidinone biphenyl resulted markedly improved antiviral activity toward EV71 with IC50 values 5.0 nM (24b) 9.3 (14a), respectively. Increasing branched chain to propyl progressive decrease activity, while inserting different heteroatoms entirely rendered only weakly active....
In this study, we examine whether an anti‐inflammatory thiourea derivative, compound #326, actions on ion channels. The effects of #326 Ca 2+ ‐activated K + channels were evaluated by patch‐clamp recordings obtained in cell‐attached, inside‐out or whole‐cell configuration. pituitary GH 3 cells, increased the amplitude currents ( I K(Ca) ) with EC 50 value 11.6 μM, which was reversed verruculogen, but not tolbutamide TRAM‐34. Under configuration, a bath application raised probability...
The purpose of this study was to examine the in vivo activity rosmarinic acid (RA) – a phytochemical with antioxidant, anti-inflammatory, and antiviral properties against influenza virus (IAV). An antibody-based kinase array different vitro functional assays were also applied identify mechanistic underpinnings by which RA may exert its anti-IAV activity. We initially examined potential efficacy using an mouse model. A time-of-addition assay subsequently investigate mechanism-of-action...
Enterovirus 71 (EV-A71) is an important pathogen that can cause severe neurological symptoms and even death. Our aim was to identify potent anti-EV-A71 compounds study their underlying mechanisms in vivo activity. We identified a imidazolidinone derivative (abbreviated PR66) as inhibitor of EV-A71 infection from the screening subsequent structure-based modification. Time-course treatments resistant virus selection PR66 were employed mode mechanism PR66. In activity tested ICR strain new-born...
Starting from the initial lead 4-phenylthiazole 18, a modest HCV inhibitor (EC50 = 9440 nM), series of structurally related thiazole derivatives has been identified as novel chemical class potent and selective NS5A inhibitors. The introduction carboxamide group between pyrrolidine ring (42) compound 18 resulted in dramatic increase activity 0.92 nM). However, 42 showed only moderate pharmacokinetic properties limited oral bioavalability 18.7% rats. Further optimization substituents at...
BPR0C261 is a synthetic small molecule compound cytotoxic against human cancer cells and active prolonging the lifespan of leukemia mice. In present study, we further investigated mechanisms its anticancer action found that inhibited microtubule polymerization through interacting with colchicine binding sites on tubulins, disrupted arrangement caused cell cycle arrest at G(2)/M phase in cells. also clonogenic growths showed cytotoxicity cervical multidrug-resistant phenotype. addition,...
ABSTRACT Hepatitis C virus (HCV) is a global health problem, affecting approximately 3% of the world's population. The standard treatment for HCV infection often poorly tolerated and ineffective. Therefore, development novel or more effective strategies to treat chronic urgently needed. In this report, BP008, potent small-molecule inhibitor replication, was developed from class compounds with thiazol core structures by means utilizing cell-based replicon system. compound reduced reporter...
ABSTRACT Hepatitis C virus (HCV), a member of the Flaviviridae family, affects approximately 3% world's population and is becoming leading cause liver disease in world. Therefore, development novel or more effective treatment strategies to treat chronic HCV infection urgently needed. In our previous study, we identified potential NS5A inhibitor, BP008. After further systemic optimization, discovered potent DBPR110. DBPR110 reduced reporter expression HCV1b replicon with 50% concentration (EC...