• Title/Summary/Keyword: novel enzyme

Search Result 614, Processing Time 0.027 seconds

Design and Synthesis of Novel Epidermal Growth Factor Receptor Kinase Inhibitors

  • Ha, Jae-Du;Kang, Seung-Kyu;Kim, Kun-Do;Choi, Joong-Kwon;Kong, Jae-Yang;Ahn, Chang-H.
    • Bulletin of the Korean Chemical Society
    • /
    • v.26 no.6
    • /
    • pp.959-965
    • /
    • 2005
  • Investigation of structure-activity relationships of novel quinazolines has identified 7,8-dihydro-[1,4]dioxino-[2,3-g]quinazolines as a potent inhibitor of EGFR. These compounds have a benzodioxane framwork, which was prepared by regioselective O-alkylation of ethyl 3,4-dihydroxy benzoate by epoxide ring opening. Compounds 3f and 3k were more potent than ZD-1839 in EGF enzyme and EGFR autophosporylation inhibition assays.

Effect of AC-264, a Novel Indole Derivative, on Apoptosis in HL-60 Cells

  • Lee, Kyeong;Kwon, Ok-Kyoung;Xia, Yan;Ahn, Kyung-Seop
    • Bulletin of the Korean Chemical Society
    • /
    • v.31 no.12
    • /
    • pp.3777-3781
    • /
    • 2010
  • The anticancer effect and apoptotic mechanism of a novel indole derivative AC-264, a lead derived from a chemical library, were investigated in human promyelocytic leukemia HL-60 cells. HL-60 cells treated with AC-264 at various concentrations showed the morphological features of apoptosis, such as plasma membrane blebbing and cell shrinkage. AC-264 exhibited cytotoxic effect in various cancer cell lines with different degrees of potency. Especially, AC-264 was effective on increasing the population of apoptotic cells in HL-60 cells, as detected by the number of cells stained with Annexin V and PI. Furthermore, AC-264 activated caspase-3 enzyme activity and induced internucleosomal DNA fragmentation. These results indicated that AC-264 produces anti-cancer effect via apoptotic cell death by activating caspase-3 and inducing internucleosomal DNA fragmentation in HL-60 cells.

A Novel ABC Transporter Gene ABC2 Involved in Multidrug Susceptibility but not Pathogenicity in Rice Blast Fungus, Magnaporthe grisea

  • Lee, Young-Jin;Kyosuke Yamamoto;Hiroshi Hamamoto;Ryoji Nakaune;Tadaaki Hibi
    • Proceedings of the Korean Society of Plant Pathology Conference
    • /
    • 2003.10a
    • /
    • pp.21-22
    • /
    • 2003
  • Fungicide treatment is the most important method for the control of plant diseases caused by phytopathogenic fungi. But fungicide resistant strains have appeared in many phytopathogenic fungi. Until now, molecular mechanisms of fungicide resistance such as mutation of target protein, overproduction of target enzyme and detoxification of fungicide have been designated. Recently, it was demonstrated that active efflux of fungicides mediated by ATP-binding cassette (ABC) transporters also contributes to fungicide resistance in several filamentous fungi, such as Aspergillus nidulans, Penicillium digitatum and Botrytis cinerea.(중략)

  • PDF

Novel Liposome Immunoassay for Detection of Ultratrace Amount of Bioactive Substances : an Assay for Insulin

  • Lim, Soo-Jeong;Kim, Chong-Kook
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1996.04a
    • /
    • pp.281-281
    • /
    • 1996
  • The immunoassay method is frequently used for the identification and quantitation of ultratrace amount of bioactive substances. Homogeneous liposome immunoassays, which can avoid the use of radioisotopes and separation steps, have recently been reported in many publications. Cytolysin-mediated liposome immunoassay using melittin ever been studied but showed limited applications. Here, we designed a homogeneous liposome immunoassay using Clostridium perfringens phospholipase C (PLC), an enzyme which catalyzes the hydrolysis of phosphatidylcholine in biological membranes, as a cytolysin.

  • PDF

Aminoacyl-tRNA Synthetase Cofactor, p43, is a Novel Cytokine and an Immune Modulator: Implications for Autoimmune Diseases and Bacterial Infections

  • Kim, Sung-Hoon
    • Proceedings of the PSK Conference
    • /
    • 2003.04a
    • /
    • pp.77-77
    • /
    • 2003
  • p43 is a protein with complex biological activities. It is first found as a protein associated with macromolecular tRNA synthetase complex. Within this complex, p43 specifically interacts with arginyl-tRNA synthetase to help the substrate tRNA binding to the enzyme. It is also necessary for the cellular stability of arginyl-tRNA synthetase and the molecular association of a few complex-forming tRNA synthetases. (omitted)

  • PDF

Acceptor reaction of a novel transfructosylating enzyme from Bacillus sp.

  • Kim, Yeong-Mi;Sinha, Jayanta;Park, Jong-Pil;Yun, Jong-Won
    • 한국생물공학회:학술대회논문집
    • /
    • 2000.11a
    • /
    • pp.583-586
    • /
    • 2000
  • Many different oligosaccharides were produced by transferring the fructose residue of sucrose to maltose, cellobiose, lactose and sucrose (self-transfer), where their yields of fructosylated acceptor products accounted for $26{\sim}30%$ (w/w). The maximum conversion yield (30%) was obtained in fructosyl cellobioside formation with 500 g sucrose/l (substrate) and 200 g cellobiose/l (acceptor). These four acceptors gave various products having DP (degree of polymerization) $2{\sim}7$ by successive transfer reactions.

  • PDF

Enzymatic Dyeing for Wool (효소를 이용한 wool의 염색)

  • Hoon Sik Shin;Byong Dae Jeon;Artur Cavaco-Paulo;Mitsuo Ueda
    • Proceedings of the Korean Fiber Society Conference
    • /
    • 2001.10a
    • /
    • pp.59-62
    • /
    • 2001
  • Oxydoreductase enzymes such as laccases (benzenediol: oxygen oxidoreductase, EC 1.10.3.2) and horseradish peroxidase (donor: hydrogen peroxide oxidoreductase, HRP, EC 1.11.1.7) can provide novel ways for wool coloration in the face of actual state of the art of these enzymes. HRP has been reported as a very useful enzyme for the synthesis of phenolic polymers2). (omitted)

  • PDF

Lipase-catalyzed esterification processing in natural polymer containing microemulsion-based organogel systems

  • Nagayama, Kazuhito;Imai, Masanao
    • Proceedings of the Membrane Society of Korea Conference
    • /
    • 2004.05a
    • /
    • pp.187-190
    • /
    • 2004
  • Microemulsions gelled by the aid of natural polymers, i.e. microemulsion-based organogels (MBGs), have become of interest as novel tools for enzyme immobilization in hydrophobic solvents [1,2]. Sodium bis(2-ethylhexyl) sulfosuccinate (AOT)is frequently employed as an amphiphile for stable MBG formation.(omitted)

  • PDF