Rat liver kininase, a serine peptidase.

Abstract:

:A serine peptidase (RLK1) was partially purified from rat liver homogenates. Its molecular weight was 80,000, and its optimum pH was 7.5. Bz-Tyr-O-Et was hydrolyzed by the enzyme, which was inhibited by Ip2PF, PMSF and by Tos-Phe-CH2Cl. The bonds cleaved by the enzyme were Phe5-Ser6 and Phe8-Arg9, when bradykinin was used as substrate.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Da Graça M,Mazzacoratti N,Sampaio CA

doi

10.1016/0006-2952(82)90466-x

subject

Has Abstract

pub_date

1982-03-01 00:00:00

pages

799-804

issue

5

eissn

0006-2952

issn

1873-2968

pii

0006-2952(82)90466-X

journal_volume

31

pub_type

杂志文章
  • Trimetazidine prevents palmitate-induced mitochondrial fission and dysfunction in cultured cardiomyocytes.

    abstract::Metabolic and cardiovascular disease patients have increased plasma levels of lipids and, specifically, of palmitate, which can be toxic for several tissues. Trimetazidine (TMZ), a partial inhibitor of lipid oxidation, has been proposed as a metabolic modulator for several cardiovascular pathologies. However, its mech...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2014.07.022

    authors: Kuzmicic J,Parra V,Verdejo HE,López-Crisosto C,Chiong M,García L,Jensen MD,Bernlohr DA,Castro PF,Lavandero S

    更新日期:2014-10-01 00:00:00

  • Understanding SOS (Son of Sevenless).

    abstract::Son of Sevenless (SOS) was discovered in Drosophila melanogaster. Essential for normal eye development in Drosophila, SOS has two human homologues, SOS1 and SOS2. The SOS1 gene encodes the Son of Sevenless 1 protein, a Ras and Rac guanine nucleotide exchange factor. This protein is composed of several important domain...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2011.07.072

    authors: Pierre S,Bats AS,Coumoul X

    更新日期:2011-11-01 00:00:00

  • Cardiac sensitivity to the inhibitory effects of chlorpromazine, imipramine and amitriptyline upon formation of flavins.

    abstract::Chlorpromazine, imipramine and amitriptyline, drugs structurally related to riboflavin, each inhibited the formation in vivo of flavin adenine dinucleotide (FAD) from riboflavin in rat heart at 2-5 mg/kg body weight, doses comparable on a weight basis to those used clinically. All three drugs inhibited FAD formation i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90632-3

    authors: Pinto J,Huang YP,Pelliccione N,Rivlin RS

    更新日期:1982-11-01 00:00:00

  • Structural elements pertinent to the interaction of cyclosporin A with its specific receptor protein, cyclophilin.

    abstract::Cyclophilin (163 amino acids; 17,737 daltons) is a ubiquitous cytosolic protein that specifically binds the potent immunosuppressive drug cyclosporin A (CsA). To characterize the structural details of this interaction, extensive use has been made of two-dimensional (2D) NMR methods. For studies on CsA, these methods a...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(90)90188-q

    authors: Hsu VL,Heald SL,Harding MW,Handschumacher RE,Armitage IM

    更新日期:1990-07-01 00:00:00

  • Cerebral and extracerebral cholesterol metabolism and CSF markers of Alzheimer's disease.

    abstract::The disturbances of the cholesterol synthesis and metabolism described in Alzheimer's disease (AD) may be both a consequence of the neurodegenerative process and a contributor to the pathogenesis. These putative relationships and their underlying mechanisms are not well understood. The aim of this study was to evaluat...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2012.12.007

    authors: Popp J,Meichsner S,Kölsch H,Lewczuk P,Maier W,Kornhuber J,Jessen F,Lütjohann D

    更新日期:2013-07-01 00:00:00

  • Evidence in vivo for elevation of intracellular free Ca2+ in the liver after diquat, acetaminophen, and CCl4.

    abstract::Several hepatotoxic agents with varied chemical mechanisms of toxicity (acetaminophen, diquat, and CCl4) depress membrane calcium pumps and/or enhance the permeability of membranes to calcium. To probe the relevance of these findings to maintenance of calcium homeostasis after toxins in vivo, we measured the activity ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(89)90016-6

    authors: Tsokos-Kuhn JO

    更新日期:1989-09-15 00:00:00

  • Inhibition by lipoxygenase products of TXA2-like responses of platelets and vascular smooth muscle. 14-Hydroxy from 22:6n-3 is more potent than 12-HETE.

    abstract::Lipoxygenase products, which are formed in great amounts in platelets during their activation, have been prepared from arachidonic acid (20:4n-6), the main polyunsaturated fatty acid (PUFA) esterified in platelet phospholipids, and from two major PUFAs of fish fat, eicosapentaenoic (20:5n-3) and docosahexaenoic (22:6n...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90782-4

    authors: Croset M,Sala A,Folco G,Lagarde M

    更新日期:1988-04-01 00:00:00

  • Inhibition of rat brain pyruvate dehydrogenase by thiamine analogs.

    abstract::The effects of thiamine thiazolone (TT) and thiamine thiazolone pyrophosphate (TTPP) on the in vitro and in vivo inhibition of pyruvate dehydrogenase complex (PDHC) from rat cortex and hippocampus were characterized. TTPP decreased PDHC activity in vitro but had no effect in vivo following its direct chronic administr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90620-x

    authors: Kandiko CT,Smith D,Yamamoto BK

    更新日期:1988-11-15 00:00:00

  • Acceleration of bone regeneration by local application of lithium: Wnt signal-mediated osteoblastogenesis and Wnt signal-independent suppression of osteoclastogenesis.

    abstract::Inhibition of glycogen synthase kinase (GSK)-3 and the consequent activation of the Wnt/β-catenin signaling pathway have been reported to increase bone volume. To develop a novel pharmacotherapy for injured bone, we investigated whether GSK-3 inhibitor was effective in promoting bone formation. In in vitro experiments...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2014.06.011

    authors: Arioka M,Takahashi-Yanaga F,Sasaki M,Yoshihara T,Morimoto S,Hirata M,Mori Y,Sasaguri T

    更新日期:2014-08-15 00:00:00

  • Sulfation of minoxidil by human liver phenol sulfotransferase.

    abstract::The N,O-sulfate of minoxidil (Mnx) is the active agent in producing the vasodilation and the hair-growth stimulating responses observed with Mnx treatment. In this report, Mnx sulfation activity was assayed in cytosol prepared from several normal human livers, and Mnx sulfation was shown to correlate significantly wit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(90)90489-8

    authors: Falany CN,Kerl EA

    更新日期:1990-09-01 00:00:00

  • Vaninolol: a new selective beta 1-adrenoceptor antagonist derived from vanillin.

    abstract::The beta-adrenoceptor blocking properties of vaninolol ((+/-)4-[4'-(2-hydroxy-3-tert-butyl-aminopropoxy)-3'-methoxyphenyl]- 3-buten-2-one), derived from vanillin, were first investigated under in vivo and in vitro conditions. Vaninolol (0.1, 0.5, 1.0 mg/kg, i.v.), as well as propranolol, produced a dose-dependent brad...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Wu BN,Hwang TL,Liao CF,Chen IJ

    更新日期:1994-07-05 00:00:00

  • Characteristics of iron(III) uptake by isolated fragments of rat small intestine in the presence of the hydroxypyrones, maltol and ethyl maltol.

    abstract::Accumulation of radioactive iron (59Fe) into isolated fragments of rat small intestine in the presence of two hydroxypyrones, maltol and ethyl maltol, was compared with that in the presence of another chelator of iron(III), nitrilotriacetic acid (NTA). The characteristics of uptake were similar with all three ligands....

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(88)90556-4

    authors: Levey JA,Barrand MA,Callingham BA,Hider RC

    更新日期:1988-05-15 00:00:00

  • CagA protein of Helicobacter pylori: a hijacker of gastric epithelial cell signaling.

    abstract::Epidemiological study has shown strong correlation between the Helicobacter pylori (H. pylori) infection and gastric carcinogenesis. However, the mechanism by which H. pylori induces gastric carcinogenesis is not known. In this review, we focused on the product of cytotoxin-associated gene A (CagA), one of the importa...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2006.10.022

    authors: Handa O,Naito Y,Yoshikawa T

    更新日期:2007-06-01 00:00:00

  • Relationship between NAD(P)H:quinone oxidoreductase 1 (NQO1) levels in a series of stably transfected cell lines and susceptibility to antitumor quinones.

    abstract::To investigate the importance of NAD(P)H:quinone oxidoreductase 1 (or DT-diaphorase; NQO1) in the bioactivation of antitumor quinones, we established a series of stably transfected cell lines derived from BE human colon adenocarcinoma cells. BE cells have no NQO1 activity due to a genetic polymorphism. The new cell li...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(01)00631-1

    authors: Winski SL,Swann E,Hargreaves RH,Dehn DL,Butler J,Moody CJ,Ross D

    更新日期:2001-06-15 00:00:00

  • Helenalin bypasses Bcl-2-mediated cell death resistance by inhibiting NF-κB and promoting reactive oxygen species generation.

    abstract::Evasion of cell death by overexpression of anti-apoptotic proteins, such as Bcl-2, is commonly observed in cancer cells leading to a lack of response to chemotherapy. Hence, there is a need to find new chemotherapeutic agents that are able to overcome chemoresistance mediated by Bcl-2 and to understand their mechanism...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2011.05.029

    authors: Hoffmann R,von Schwarzenberg K,López-Antón N,Rudy A,Wanner G,Dirsch VM,Vollmar AM

    更新日期:2011-09-01 00:00:00

  • Dual cytotoxic mechanisms of submicromolar taxol on human leukemia HL-60 cells.

    abstract::Taxol-induced mitotic block and apoptosis were investigated using taxol-sensitive human leukemia HL-60 cells at submicromolar concentrations of the drug. Cells exposed to either 20 nM taxol for 1 hr or 10 nM taxol for 12 hr were able to resume normal growth, whereas cells exposed to 60 nM taxol for 1 hr or 10 nM taxol...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(97)82450-1

    authors: Lieu CH,Chang YN,Lai YK

    更新日期:1997-06-01 00:00:00

  • Studies on the mechanism by which tyrosine raises urinary catecholamines.

    abstract::The source of urinary catecholamines and the mechanisms by which tyrosine administration raises these compounds were investigated in rats. Adrenalectomy blocked the tyrosine-induced rise in urinary epinephrine but not dopamine or norepinephrine. Following chemical sympathectomy with 6-hydroxydopamine (6-OHDA), the tyr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(82)90578-0

    authors: Agharanya JC,Wurtman RJ

    更新日期:1982-11-15 00:00:00

  • Inhibition of bacterial cell division protein FtsZ by cinnamaldehyde.

    abstract::Cinnamaldehyde is a natural product from spices that inhibits cell separation in Bacillus cereus. Cell division is regulated by FtsZ, a prokaryotic homolog of tubulin. FtsZ assembles into the Z-ring at the site of cell division. Here, we report the effect of cinnamaldehyde on FtsZ and hence on the cell division appara...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2007.06.029

    authors: Domadia P,Swarup S,Bhunia A,Sivaraman J,Dasgupta D

    更新日期:2007-09-15 00:00:00

  • The bioactivation of amodiaquine by human polymorphonuclear leucocytes in vitro: chemical mechanisms and the effects of fluorine substitution.

    abstract::Amodiaquine, a 4-aminoquinoline antimalarial, has been associated with hepatitis and agranulocytosis in humans. Drug hypersensitivity reactions, especially agranulocytosis, have been attributed to reactive intermediates generated by the oxidants discharged from stimulated polymorphonuclear leucocytes (PMN). The metabo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(95)00236-s

    authors: Tingle MD,Jewell H,Maggs JL,O'Neill PM,Park BK

    更新日期:1995-09-28 00:00:00

  • A conserved antioxidant response element (ARE) in the promoter of human carbonyl reductase 3 (CBR3) mediates induction by the master redox switch Nrf2.

    abstract::Carbonyl reductase activity catalyzes the two electron reduction of several endogenous and exogenous carbonyl substrates. Recent data indicate that the expression of human carbonyl reductase 3 (CBR3) is regulated by the master redox switch Nrf2. Nrf2 binds to conserved antioxidant response elements (AREs) in the promo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2011.09.027

    authors: Cheng Q,Kalabus JL,Zhang J,Blanco JG

    更新日期:2012-01-01 00:00:00

  • The effects of bucillamine on glutathione and glutathione-related enzymes in the mouse.

    abstract::The effect of bucillamine (BA) on glutathione (GSH) and GSH-related enzymes was investigated in C57 mouse. Administration of high doses of BA (150-400 mg/kg) produced a dose-dependent depletion (20-44%) of hepatic GSH, which was similar in magnitude to that produced by equimolar doses of other sulphydryl drugs studied...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90045-7

    authors: Yeung JH

    更新日期:1991-07-25 00:00:00

  • CYP2C19 polymorphisms account for inter-individual variability of drug metabolism in cynomolgus macaques.

    abstract::CYP2C19 (formerly known as CYP2C75), highly homologous to human CYP2C19, has been identified in cynomolgus and rhesus macaques, non-human primate species widely used in drug metabolism studies. CYP2C19 is predominantly expressed in liver and encodes a functional drug-metabolizing enzyme. Genetic variants in human CYP2...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2014.07.004

    authors: Uno Y,Matsushita A,Shukuya M,Matsumoto Y,Murayama N,Yamazaki H

    更新日期:2014-09-15 00:00:00

  • Contribution of different phospholipases and arachidonic acid metabolites in the response of gallbladder smooth muscle to cholecystokinin.

    abstract::Guinea pig gallbladder muscle strips were used to investigate the contribution of different sources of diacylglicerol (DAG) in the cholecystokinin (CCK)-induced contraction. The involvement of arachidonic acid (AA) in this response was also investigated. Three distinct pathways for DAG production were investigated wit...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(02)01259-5

    authors: Alcón S,Morales S,Camello PJ,Pozo MJ

    更新日期:2002-10-01 00:00:00

  • Antagonistic effect of the cardioprotector (+)-1,2-bis(3,5-dioxopiperazinyl-1-yl)propane (ICRF-187) on DNA breaks and cytotoxicity induced by the topoisomerase II directed drugs daunorubicin and etoposide (VP-16).

    abstract::The effect of the bisdioxopiperazine cardioprotector ICRF-187 (ADR-529, dexrazoxan) on drug-induced DNA damage and cytotoxicity was studied. Using alkaline elution assays, ICRF-187 in a dose-dependent manner inhibited the formation of DNA single strand breaks (SSBs) as well as DNA-protein cross-links induced by drugs ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90514-w

    authors: Sehested M,Jensen PB,Sørensen BS,Holm B,Friche E,Demant EJ

    更新日期:1993-08-03 00:00:00

  • Catestatin decreases macrophage function in two mouse models of experimental colitis.

    abstract::Mucosal inflammation in patients with inflammatory bowel disease (IBD) is characterized by an alteration of prohormone chromogranin A (CgA) production. The recent demonstration of an implication of CgA in collagenous colitis and immune regulation provides a potential link between CgA-derived peptides (catestatin, CTS)...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2014.03.003

    authors: Rabbi MF,Labis B,Metz-Boutigue MH,Bernstein CN,Ghia JE

    更新日期:2014-06-01 00:00:00

  • Implications of selective type II IMP dehydrogenase (IMPDH) inhibition by the 6-ethoxycarbonyl-3,3-disubstituted-1,5-diazabicyclo[3.1.0]hexane-2,4-diones on tumor cell death.

    abstract::It was shown previously that three 1,5-diazabicyclo[3.1.0]hexane-2,4-diones selectively inhibited human Type II IMP dehydrogenase (IMPDH) from Tmolt4 cell leukemia [Barnes et al., Biochemistry 2000;39:13641-50]. The agents acted as competitive inhibitors of this isoform, yet when tested against human Type I at concent...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(01)00649-9

    authors: Barnes BJ,Eakin AE,Izydore RA,Hall IH

    更新日期:2001-07-01 00:00:00

  • Effects of chronic administration of the peroxisome proliferator, clofibrate, on cytosolic acetyl-CoA hydrolase in rat liver.

    abstract::The hypolipidemic drug ethyl chlorophenoxyisobutyrate (clofibrate) is known to induce peroxisome proliferation and to be carcinogenic after long term administration to rats and mice. We examined the effects of treatment with this drug for periods of up to 18 months on cytosolic ATP-stimulated and ADP-inhibited acetyl-...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90038-x

    authors: Nakanishi Y,Okamoto K,Isohashi F

    更新日期:1993-04-06 00:00:00

  • Protective effect of erythropoietin on the oxidative damage of erythrocyte membrane by hydroxyl radical.

    abstract::Treatment of red blood cells with the copper (II) ascorbate system causes increased lipid peroxidation, increased membrane microviscosity, and phospholipid translocation with a concurrent decrease in cytosolic catalase and glutathione peroxidase activities. All these changes are prevented if the cells are treated with...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(99)00277-4

    authors: Chattopadhyay A,Choudhury TD,Bandyopadhyay D,Datta AG

    更新日期:2000-02-15 00:00:00

  • Site-directed mutagenesis at the human B2 receptor and molecular modelling to define the pharmacophore of non-peptide bradykinin receptor antagonists.

    abstract::Combining site-directed mutagenesis with information obtained from molecular modelling of the bradykinin (BK) human B2 receptor (hB2R) as derived from the bovine rhodopsin crystal structure [Science 289 (2000) 739], we previously defined a putative binding mode for the non-peptide B2 receptor antagonists, FR173657 and...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2003.09.034

    authors: Meini S,Cucchi P,Bellucci F,Catalani C,Faiella A,Rotondaro L,Quartara L,Giolitti A,Maggi CA

    更新日期:2004-02-15 00:00:00

  • Protective effect of ellagic acid, a natural polyphenolic compound, in a murine model of Crohn's disease.

    abstract::Current epidemiological and experimental studies support a beneficial role of dietary polyphenols in several gastrointestinal diseases, including inflammatory bowel disease. The aim of this study was to gain a better understanding of the effects of a naturally occurring polyphenol, ellagic acid, present in some fruits...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2011.06.043

    authors: Rosillo MA,Sanchez-Hidalgo M,Cárdeno A,de la Lastra CA

    更新日期:2011-10-01 00:00:00