Abstract：
:A series of novel peptidyl-alpha-ketoamide compounds were evaluated as inhibitors of the deltaNS3-NS4A serine protease from the hepatitis C virus. These peptidyl-alpha-ketoamide inhibitors with Ki values ranging from 0.17 nM to 5.6 microM exhibited slow-binding inhibition. Kinetic studies established one-step kinetic mechanisms and dissociation rate constants in the 3-7 x 10(-5) s(-1) range for these compounds. The association rate constants, which ranged from 10 to 263,000 M(-1) s(-1), were responsible for the greater than four order of magnitude overall binding affinity range exhibited by this series. An X-ray crystal structure of a protease-inhibitor complex revealed an unusual interaction between the oxyanion of the adduct and the protein as well as a significant movement in the S1' region of the protein loop comprising residues 35-42. These results are quite different from peptidyl-alpha-ketoacid inhibition of HCV protease, which reportedly undergoes no notable conformational changes and proceeds with a two-step slow-binding kinetic mechanism.
journal_name
Arch Biochem Biophysjournal_title
Archives of biochemistry and biophysicsauthors
Liu Y,Stoll VS,Richardson PL,Saldivar A,Klaus JL,Molla A,Kohlbrenner W,Kati WMdoi
10.1016/j.abb.2003.11.013subject
Has Abstractpub_date
2004-01-15 00:00:00pages
207-16issue
2eissn
0003-9861issn
1096-0384pii
S0003-9861(03)00627-1journal_volume
421pub_type
杂志文章abstract：:We previously showed that iron chelated to the Pseudomonas aeruginosa siderophore pyochelin enhances oxidant-mediated injury to pulmonary artery endothelial cells by catalyzing hydroxyl radical (HO(*)) formation. Therefore, we examined pyochelin structural/chemical features that may be important in this process. Five ...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.2001.2517
更新日期：2001-09-15 00:00:00
abstract：:Synechococcus sp. strain PCC 7002 is a robust, genetically tractable cyanobacterium that produces six different xanthophyll carotenoids (zeaxanthin, cryptoxanthin, myxoxanthophyll (myxol-2'-fucoside), echinenone, 3'-hydroxyechinenone, and synechoxanthin) and tolerates many environmental stresses, including high light ...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/j.abb.2010.07.007
更新日期：2010-12-01 00:00:00
abstract：:An in vitro expression plasmid (pGRAP) that contained the cDNA coding for the rat mitochondrial aldehyde dehydrogenase precursor was constructed, mRNA was synthesized then translated, and the in vitro synthesized precursor of aldehyde dehydrogenase was used in an in vitro import assay. As expected the 19 amino acid si...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(89)90238-5
更新日期：1989-08-01 00:00:00
abstract：:Hippocampal-dependent cognitive functions rely on production of new neurons and maintenance of dendritic structures to provide the synaptic plasticity needed for learning and formation of new memories. Hippocampal formation is exquisitely sensitive to patho-physiological changes, and reduced antioxidant capacity and e...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章,评审
doi：10.1016/j.abb.2015.03.014
更新日期：2015-06-15 00:00:00
abstract：:Methylglyoxal (MGO), a reactive dicarbonyl metabolite is a potent arginine directed glycating agent which has implications for diabetes-related complications. Dicarbonyl metabolites are produced endogenously and in a state of misbalance, they contribute to cell and tissue dysfunction through protein and DNA modificati...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/j.abb.2018.02.019
更新日期：2018-05-01 00:00:00
abstract：:I had the fortune to be introduced to Helmut Sies during the mid 1980s, while working as a post-doctoral scientist at the University of California, Berkeley. At that time, Helmut was a frequent visitor of the Bruce Ames' laboratory and a leading authority in antioxidants and oxidative stress. His concepts, ideas and w...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章,评审
doi：10.1016/j.abb.2015.11.021
更新日期：2016-04-01 00:00:00
abstract：:The insulin receptor from rat skeletal muscle was characterized. Treatment of muscle membranes with the photoactive insulin analog, 125I[N-epsilonB29-monoazidobenzoyl]-insulin revealed a single protein band of 135,000 Da, the alpha subunit. Iodination of total membrane protein followed by Triton X-100 solubilization a...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(85)90611-3
更新日期：1985-01-01 00:00:00
abstract：:A glucose analog, N-(bromoacetyl)-D-glucosamine (GlcNBrAc), previously used to label the glucose binding sites of rat muscle Type II and bovine brain Type I hexokinases, also inactivates rat brain hexokinase (ATP:D-hexose 6-phosphotransferase, EC 2.7.1.1) with pseudo-first-order kinetics. Inactivation occurs predomina...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(87)90116-0
更新日期：1987-05-01 00:00:00
abstract：:Reactive oxygen species like hydrogen peroxide (H2O2) have been shown to serve as messengers in the induction of NF-kappa B and, hence, in the activation and replication of human immunodeficiency virus type 1 (HIV-1) in human cells. Several antioxidant compounds and iron chelators have been shown to interfere with bot...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.1995.1394
更新日期：1995-08-01 00:00:00
abstract：:In hepatocytes incubated in the presence of 20 mM glucose, strong stimulation of glycogen synthesis by LiCl was observed in cells from both normal and streptozotocin-induced diabetic rats. This stimulation was concentration- and time-dependent, and it was related to an increase in the glycogen synthase activity ratio....
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.1993.1164
更新日期：1993-03-01 00:00:00
abstract：:The gene of the human fatty acid omega-hydroxylase, CYP4A11, has been isolated from a human BAC library, and its complete genomic sequence has been determined. The CYP4A11 gene spanned 12,568 bp and contained 12 exons. The known PPAR recognition elements (PPRE), which were reported to be involved in the induction of C...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.2000.1831
更新日期：2000-06-15 00:00:00
abstract：:Two recombinant sesquiterpene synthases from grand fir, delta-selinene synthase and gamma-humulene synthase, each produce more than 30 sesquiterpene olefins from the acyclic precursor farnesyl diphosphate. These enzymes contain a pair of DDxxD motifs, on opposite lips of the presumptive active site, which are thought ...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/S0003-9861(02)00068-1
更新日期：2002-06-01 00:00:00
abstract：:The specific activity of cytochrome P450-linked coumarin 7-hydroxylase (COH) of hepatic mitoplasts from DBA/2N mice is up to 55% as great as the microsomal activity. According to Western blot and immunodiffusion analysis and inhibition studies with anti-P450Coh and metyrapone, the mitoplastic P450Coh had the same mole...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(88)90063-x
更新日期：1988-12-01 00:00:00
abstract：:Lipoxygenase-induced lipid oxidation contributes to plasma lipoprotein oxidation and may be an underlying pathogenic mechanism of atherogenesis. Since inactivation of the vasorelaxant actions of nitric oxide (.NO) plays a critical role in the impaired function of atherosclerotic vessels and because .NO reacts rapidly ...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.1995.9935
更新日期：1995-12-01 00:00:00
abstract：:We previously demonstrated that the expression of HSP20, a small heat shock protein, is inversely correlated with the progression of HCC. Inflammation is associated with HCC, and numerous cytokines, including TNF-α, act as key mediators in the progression of HCC. In the present study, we investigated whether HSP20 is ...
journal_title：Archives of biochemistry and biophysics
pub_type： 临床试验,杂志文章
doi：10.1016/j.abb.2014.10.010
更新日期：2015-01-01 00:00:00
abstract：:MICALs form a conserved multidomain protein family essential for cytoskeletal rearrangements. To complement structural information available, we produced the FAD-containing monooxygenase-like domain of human MICAL-1 (MICAL-MO) in forms differing for the presence and location of a His-tag, which only influences the pro...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/j.abb.2011.08.004
更新日期：2011-11-01 00:00:00
abstract：:The retinal pigment epithelium (RPE)-specific protein RPE65 is the major protein of the RPE microsomal membrane fraction. Though RPE65 lacks transmembrane domains or signal peptide, detergents are required for its maximally effective solubilization in isotonic buffers. However, in 0.75-1.0 M KCl, RPE65 is as soluble w...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.1997.0276
更新日期：1997-10-01 00:00:00
abstract：:We reported previously a highly purified phosphatidylinositol-specific phospholipase C (PI-PLC) from bovine brain and from human myelin which was stimulated by myelin basic protein. In this paper we report that the stimulation of the PI-PLC activity by myelin basic protein (MBP) requires arginine residues in peptide l...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.1993.1242
更新日期：1993-05-01 00:00:00
abstract：:Functional activities of isolated atria from 4-week diabetic rats and their anoxic tolerance and recovery were compared to those of control rats. The present study showed a two-fold increase in maximum developed contraction force (CF), the rate of force development, and the rate of relaxation in isolated atria from di...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(90)90479-i
更新日期：1990-05-15 00:00:00
abstract：:Factors influencing pyrroline 5-carboxylate (P5C) synthesis from glutamate by a subcellular fraction enriched in mitochondria of rat small intestinal mucosa have been studied. P5C synthesis decreased rapidly if this subcellular fraction was preincubated at 20 degrees C in the absence of substrates; this effect suggest...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(83)90340-5
更新日期：1983-10-15 00:00:00
abstract：:Dpo4 is a representative model of Y-family DNA polymerase and is therefore one of the most intensively studied DNA polymerase. 6 mA, an epigenetic marker, plays important roles in regulation of various biological processes. However, its effects on DNA replication by Dpo4 is completely unknown. Here, we found that 6 mA...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/j.abb.2019.108120
更新日期：2019-10-30 00:00:00
abstract：:A new fluorescent ATP analog, adenosine-5'-triphosphoro-gamma-1-(5-sulfonic acid)naphthyl ethylamidate (gamma-1,5-EDANS)ATP, containing the fluorophore N-(aminoethyl)-5-naphthylamine-1-sulfonic acid attached via a gamma-phosphoamidate bond was synthesized in good yield. It has absorption maxima at 255 and 344 nm and a...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(86)90311-5
更新日期：1986-05-01 00:00:00
abstract：:A type II ribosome-inactivating protein (RIP) was isolated from the bark tissue of Japanese elderberry (Sambucus sieboldiana) and named sieboldin-b. Sieboldin-b is a heterodimeric protein consisting of 27- and 33-kDa subunits and showed strong ribosome-inactivating activity in vitro but did not show in vivo toxicity. ...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.1997.9927
更新日期：1997-04-15 00:00:00
abstract：:Green tea (Camellia sinensis) is rich in catechins, of which (-)-epigallocatechin-3-gallate (EGCG) is the most abundant. Studies in animal models of carcinogenesis have shown that green tea and EGCG can inhibit tumorigenesis during the initiation, promotion and progression stages. Many potential mechanisms have been p...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章,评审
doi：10.1016/j.abb.2010.06.013
更新日期：2010-09-01 00:00:00
abstract：:Type III galactosemia is an inherited disease caused by mutations which affect the activity of UDP-galactose 4'-epimerase (GALE). We evaluated the impact of four disease-associated variants (p.N34S, p.G90E, p.V94M and p.K161N) on the conformational stability and dynamics of GALE. Thermal denaturation studies showed th...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/j.abb.2014.07.030
更新日期：2014-11-15 00:00:00
abstract：:Glycophorin from human red blood cells was exposed to ozone in aqueous solution. Amino acid analysis of glycophorin exposed to a 10-fold molar excess of ozone showed that the only residue affected was methionine. Both methionine residues of the protein were oxidized to methionine sulfoxide. Exposure of the oxidized pr...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(92)90491-e
更新日期：1992-05-15 00:00:00
abstract：:Elevation of cytosolic level of Ca(2+) was measured by spatial screening of freshly isolated dorsal root ganglion neurons loaded with Fura-2AM after subjecting them to a moderate hypoxic solution (pO(2)=10-40 mmHg). Short exposure of neurons to hypoxia resulted in a reversible elevation of intracellular Ca(2+) to abou...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/s0003-9861(02)00682-3
更新日期：2003-02-15 00:00:00
abstract：:The didecameric hemocyanin of the bivalve mollusc Nucula hanleyi, observed in the electron microscope in vitreous ice, was subjected to a three-dimensional (3D) reconstruction by the random conical tilt series method. The 3D volume was analyzed by computing solid-body surface representations and slices through the vol...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1006/abbi.1995.1287
更新日期：1995-05-10 00:00:00
abstract：:Primary cultures of rainbow trout hepatocytes were used to study the expression of CYP1A1 mRNA, its protein product (P4501A1), and catalytic activities (7-ethoxy-resorufin-O-deethylase, EROD) during a 96-h period after exposure of cells to beta-naphthoflavone (BNF) or 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD). Hepato...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(92)90072-5
更新日期：1992-01-01 00:00:00
abstract：:Hepatic cysteine sulfinic acid decarboxylase (EC 4.1.1.29) activity has been reported to decrease in response to both L-methionine (Met) feeding and adrenalectomy in rats. A series of experiments was conducted to (a) determine if CSAD depression was evident in female rats fed a methionine-supplemented diet; and (b) de...
journal_title：Archives of biochemistry and biophysics
pub_type： 杂志文章
doi：10.1016/0003-9861(92)90721-8
更新日期：1992-05-01 00:00:00
