نتایج جستجو برای: uncompetitive inhibitor
تعداد نتایج: 211497 فیلتر نتایج به سال:
Sucrose synthase (EC 2.4.1.13) was purified to homogeneity from developing maize lZea mays L.) endosperm. Substrate saturation and inhibitor kinetics were examined for the sucrose synthase reaction. The Km-values for fructose and uridine diphosphate glucose (UDPGlc) were estimated to be 7.8 mM and 76 IlM, respectively. Fructose concentrations over 20 mM inhibited sucrose synthase in an uncompet...
Lansoprazole, a known H(+)/K(+)-ATPase inhibitor, is currently used as a therapeutical option for the initial treatment of gastroesophageal reflux disease. Recently, lansoprazole has been found to be an inhibitor of cytosolic PHOSPHO1 (a phosphatase which hydrolyses phosphocholine and phosphoethanolamine), providing a possible therapeutical target to cure pathological mineralization. Since PHOS...
Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway.
A high-throughput screen to discover inhibitors of p97 ATPase activity identified an indole amide that bound to an allosteric site of the protein. Medicinal chemistry optimization led to improvements in potency and solubility. Indole amide 3 represents a novel uncompetitive inhibitor with excellent physical and pharmaceutical properties that can be used as a starting point for drug discovery ef...
Natural tyrosinase inhibitors from herbal plants are promising therapeutic agents for skincare and cosmetic products. curcuminoids exhibit weak antityrosinase properties. The structural modification of curcumin, the major curcuminoid Curcuma longa, gave 14 analogues. inhibitory activity natural modified analogues on both L-tyrosine DOPA substrates were evaluated. inhibition kinetics also undert...
The inhibition mechanisms of the firefly luciferase (Luc) by three of the most important inhibitors of the reactions catalysed by Luc, dehydroluciferyl-coenzyme A (L-CoA), dehydroluciferin (L) and L-luciferin (L-LH(2)) were investigated. Light production in the presence and absence of these inhibitors (0.5 to 2 μM) has been measured in 50 mM Hepes buffer (pH = 7.5), 10 nM Luc, 250 μM ATP and D-...
Studies were carried out to natural papain inhibitor from papaya latex. Fresh latex from green fruits of Carica papaya was collected and immediately transported in ice bath to the lab, from which three fractions with inhibitor effect of esterase papain activity were isolated by latex dialysis, Sephadex G-25 gel filtration and ionic exchange chromatography in SP-Sephadex C-25. The isolated fract...
Linoleic acid was isolated from both the methanol extracts of proso and Japanese millet as a histone deacetylase inhibitor. It showed uncompetitive inhibitory activity toward histone deacetylase (IC(50)=0.51 mM) and potent cytotoxicity toward human leukemia K562 (IC(50)=68 microM) and prostate cancer LNCaP cells (IC(50)=193 microM). Millet containing linoleic acid might have anti-tumor activity.
BACKGROUND The isozymes of alkaline phosphatase, the tissue non-specific, intestinal and placental, have similar properties and a high degree of identity. The placental isozyme (PLAP) is an oncofetal antigen expressed in several malignancies including choriocarcinoma, seminoma and ovarian carcinoma. We had earlier attempted to isolate PLAP-specific scFv from a synthetic human immunoglobulin lib...
The kinetic mechanisms of Escherichia coli phosphofructokinase-2 (Pfk-2) and of the mutant enzyme Pfk-2 were investigated. Initial velocity studies showed that both enzymes have a sequential kinetic mechanism, indicating that both substrates must bind to the enzyme before any products are released. For Pfk-2, the product inhibition kinetics was as follows: fructose-1,6-P2 was a competitive inhi...
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