Bifunctional Inhibitor
Mostrando 1-12 de 26 artigos, teses e dissertações.
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1. Evaluation of anti-Wnt/β-catenin signaling agents by pGL4-TOP transfected stable cells with a luciferase reporter system
Refractory and relapsed leukemia is a major problem during cancer therapy, which is due to the aberrant activation of Wnt/β-catenin signaling pathway. Activation of this pathway is promoted by wingless (Wnt) proteins and induces co-activator β-catenin binding to lymphoid enhancer factor (LEF)/T-cell factor protein (TCF). To provide a convenient system for
Brazilian Journal of Medical and Biological Research. Publicado em: 2010-10
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2. Construção de modelos de interação in silico e in vitro do inibidor do tipo Kunitz de Adenanthera pavonina L. para as enzimas cisteínicas e serínicas
Os inibidores de proteinases serínicas (IPs) estão extensamente distribuídos na natureza e inibem a atividade enzimática in vitro e in vivo. Estes IPs em sementes de leguminosas compreendem sete famílias, no entanto as famílias Bowman-Birk e do tipo Kunitz são as mais estudadas e representam um papel importante na primeira linha de defesa contra inset
Publicado em: 2008
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3. Adenylosuccinate Lyase from Leishmania major Friedlin and its role in the purine nucleotides salvage pathway / Adenylosuccinato lyase (ADSL) de leishmania major friedlin: sua relevância na via de recuperação de purino-nucleotídeos
Many species of Leishmania are responsible for serious visceral or skin diseases that exhibit high incidence in tropical and subtropical regions. The drugs currently employed in the treatment of parasitic diseases are potentially carcinogenic, often require prolonged treatment and patient hospitalization. An effective program of drug design requires the vali
Publicado em: 2006
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4. Novel Bifunctional Inhibitor of Xylanase and Aspartic Protease: Implications for Inhibition of Fungal Growth
A novel bifunctional inhibitor (ATBI) from an extremophilic Bacillus sp. exhibiting an activity against phytopathogenic fungi, including Alternaria, Aspergillus, Curvularia, Colletotricum, Fusarium, and Phomopsis species, and the saprophytic fungus Trichoderma sp. has been investigated. The 50% inhibitory concentrations of ATBI ranged from 0.30 to 5.9 μg/ml
American Society for Microbiology.
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5. Basic fibroblast growth factor as a growth inhibitor for cultured human tumor cells.
Basic fibroblast growth factor (bFGF) stimulates the proliferation of many cells and it is found in a wide variety of normal or transformed tissues. As demonstrated here, bFGF is also present in cultured human Ewing's sarcoma cells. Unexpectedly, however, bFGF isolated from these cells inhibits their own proliferation, indicating that bFGF can act as an endo
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6. Active site-directed inhibition of Ca2+/calmodulin-dependent protein kinase type II by a bifunctional calmodulin-binding peptide.
The activation of Ca2+/calmodulin (CaM)-dependent protein kinase II (CaM-KII) by Ca2+/CaM results in autophosphorylation and the generation of Ca2+/CaM-independent enzyme activity. We postulated that CaM binding and subsequent autophosphorylation alters the conformation of CaM-KII and exposes its substrate-binding and catalytic site(s). Previous peptide mapp
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7. Activation of Aurora-A kinase by protein phosphatase inhibitor-2, a bifunctional signaling protein
Aurora-A kinase is necessary for centrosome maturation, for assembly and maintenance of a bipolar spindle, and for proper chromosome segregation during cell division. Aurora-A is an oncogene that is overexpressed in multiple human cancers. Regulation of kinase activity apparently depends on phosphorylation of Thr-288 in the T-loop. In addition, interactions
National Academy of Sciences.
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8. Copurification of hydroxyethylthiazole kinase and thiamine-phosphate pyrophosphorylase of Saccharomyces cerevisiae: characterization of hydroxyethylthiazole kinase as a bifunctional enzyme in the thiamine biosynthetic pathway.
Mutants of Saccharomyces cerevisiae resistant to 2-amino-4-methyl-5-beta-hydroxyethylthiazole, an antimetabolite of 4-methyl-5-beta-hydroxyethylthiazole (hydroxyethylthiazole), which are deficient in the activities of both hydroxyethylthiazole kinase and thiamine-phosphate pyrophosphorylase, involved in the pathway of de novo synthesis of thiamine in S. cere
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9. BRUCE, a Giant E2/E3 Ubiquitin Ligase and Inhibitor of Apoptosis Protein of the trans-Golgi Network, Is Required for Normal Placenta Development and Mouse Survival
BRUCE is a highly conserved 528-kDa peripheral membrane protein of the trans-Golgi network. Owing to the presence of an N-terminal single baculovirus inhibitor repeat, BRUCE functions as an inhibitor of apoptosis protein and blocks apoptosis when overexpressed. In addition, due to the presence of a C-terminal ubiquitin-conjugating domain, BRUCE can covalentl
American Society for Microbiology.
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10. Changing the Dimensions of Suberin Lamellae of Green Cotton Fibers with a Specific Inhibitor of the Endoplasmic Reticulum-Associated Fatty Acid Elongases.
The fibers of the green lint mutant of cotton (Gossypium hirsutum L.) contain large amounts of wax and are suberized. More than 96% of the bifunctional aliphatic suberin monomers ([alpha],[omega]-alkanedioic acids and [omega]-hydroxyalkanoic acids) have chain lengths of C22 and C24 in green cotton fiber suberin. In fibers grown in the presence of S-ethyl-N,N
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11. A Simple Screen for Murein Transglycosylase Inhibitors
A simple assay for detection of compounds that bind to the active site in the transglycosylation domain of the essential bifunctional transglycosylase and transpeptidase penicillin-binding proteins (PBPs) is reported. The method is based on a competition with the specific transglycosylase inhibitor moenomycin. With moenomycin coupled to Affi-Gel beads, a sim
American Society for Microbiology.
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12. Mode of Action of cGMP-dependent Protein Kinase-specific Inhibitors Probed by Photoaffinity Cross-linking Mass Spectrometry*
The inhibitor peptide DT-2 (YGRKKRRQRRRPPLRKKKKKH) is the most potent and selective inhibitor of the cGMP-dependent protein kinase (PKG) known today. DT-2 is a construct of a PKG tight binding sequence (W45, LRKKKKKH, KI = 0.8 μm) and a membrane translocating sequence (DT-6, YGRKKRRQRRRPP, KI = 1.1 μm), that combined strongly inhibits PKG catalyzed phospho
American Society for Biochemistry and Molecular Biology.