Specific, high-affinity bradykinin binding by purified porcine kidney post-proline cleaving enzyme.

Abstract:

:Post-proline cleaving enzyme (PPCE) was purified from porcine kidney cytosol. The purified enzyme bound [125I-Tyr5]-bradykinin but neither [125I-Tyr1]-kallidin nor [125I-Tyr8]-bradykinin. Scatchard analysis of the data was consistent with a single class of binding sites with a Kassoc = 1.3 +/- 0.1 X 10(8) M-1. The optimal pH for [125I-Tyr5]-bradykinin binding was 6.8. The specificity of binding was evaluated with sixty-seven bradykinin analogs. The catalytic activity of the enzyme was measured with N-benzyloxycarbonyl-Gly-Pro-methylcoumarinyl-7-amide (Z-Gly-Pro-MCA). The optimal pH for hydrolysis of this substrate was broad and centered at 8.3. The apparent Km and Vmax were obtained from Lineweaver and Burk plots and were 4.8 +/- 0.4 X 10(-5) M and 42 +/- 5 mumoles X mg-1 X min-1 respectively. The IC50 values for bradykinin, diisopropylfluorophosphate (DFP), and N-benzyloxycarbonyl-Pro-Prolinal (Z-Pro-Prolinal) to inhibit Z-Gly-Pro-MCA hydrolysis by PPCE were 5.9 +/- 1.4 X 10(-7) M, 8.8 +/- 3.1 X 10(-7) and 7.9 +/- 0.3 X 10(-9) M respectively. Corresponding values for inhibition of [125I-Tyr5]-bradykinin binding by PPCE were 5.1 +/- 2.3 X 10(-9) M, 1.2 +/- 0.3 X 10(-6) M and 1.4 +/- 0.6 X 10(-8) M.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Odya CE,Dally RD,Georgiadis KE

doi

10.1016/0006-2952(87)90380-7

subject

Has Abstract

pub_date

1987-01-01 00:00:00

pages

39-49

issue

1

eissn

0006-2952

issn

1873-2968

pii

0006-2952(87)90380-7

journal_volume

36

pub_type

杂志文章
  • Inhibiting cancer metastasis via targeting NAPDH oxidase 4.

    abstract::Cancer metastasis is a major cause for cancer-related death and inhibiting cancer metastasis is an alternative way to treat cancer. Several lines of reported evidence suggest that NADPH oxidase 4 (NOX4) is a potential target for intervention of cancer metastasis, as the reactive oxygen species (ROS) generated by this ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2013.05.011

    authors: Zhang B,Liu Z,Hu X

    更新日期:2013-07-15 00:00:00

  • Effects of sulfobromophthalein and ethacrynic acid on glyceryl trinitrate relaxation.

    abstract::The effects of sulfobromophthalein (SBP) and ethacrynic acid (ECA), both inhibitors of glutathione S-transferase (GST), or glyceryl trinitrate (GTN)-induced vasorelaxation were investigated in rabbit aortic strips. The aortic strips were pre-contracted with phenylephrine, followed by relaxation with 0.5 microM GTN, wi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(92)90184-k

    authors: Lau DT,Benet LZ

    更新日期:1992-05-28 00:00:00

  • Relative contribution of rat cytochrome P450 isoforms to the metabolism of caffeine: the pathway and concentration dependence.

    abstract::The aim of the present study was to estimate the relative contribution of rat P450 isoforms to the metabolism of caffeine and to assess the usefulness of caffeine as a marker substance for estimating the activity of P450 in rat liver and its potential for pharmacokinetic interactions in pharmacological experiments. Th...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2007.12.017

    authors: Kot M,Daniel WA

    更新日期:2008-04-01 00:00:00

  • Microglia-neuron interactions in the models of neuropathic pain.

    abstract::Chronic pain is a debilitating condition that often emerges as a clinical symptom of inflammatory diseases. It has therefore been widely accepted that the immune system critically contributes to the pathology of chronic pain. Microglia, a type of immune cell in the central nervous system, has attracted researchers' at...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1016/j.bcp.2019.08.016

    authors: Tozaki-Saitoh H,Tsuda M

    更新日期:2019-11-01 00:00:00

  • Effect of okadaic acid on immunologic and non-immunologic histamine release in rat mast cells.

    abstract::We have studied the effect of the protein phosphatase (PP) inhibitor, okadaic acid (OKA) on histamine release elicited by immunologic and non-immunologic stimuli in peritoneal and pleural rat mast cells. When cells were stimulated with antigen (egg albumin), OKA strongly inhibited histamine release. This finding sugge...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90194-5

    authors: Estévez MD,Vieytes MR,Louzao MC,Botana LM

    更新日期:1994-02-09 00:00:00

  • Functional expression of intestinal dipeptide/beta-lactam antibiotic transporter in Xenopus laevis oocytes.

    abstract::An intestinal active transport system specific to small peptides and peptide-like drugs such as beta-lactam antibiotics was functionally expressed in Xenopus laevis oocytes after microinjection of messenger RNA (mRNA) derived from rat intestinal mucosal cells. The transport activity was evaluated by measuring the upta...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90358-1

    authors: Tamai I,Tomizawa N,Kadowaki A,Terasaki T,Nakayama K,Higashida H,Tsuji A

    更新日期:1994-08-30 00:00:00

  • Mechanisms of toxicity of 3'-azido-3'-deoxythymidine. Its interaction with adenylate kinase.

    abstract::Recent experiments from our laboratory have indicated that the inhibitory effect of 3'-azido-3'-deoxythymidine (AZT) on oxidative phosphorylation may occur directly, in addition to being brought about by its inhibition of mtDNA replication. We report here studies on the effect of AZT on adenylate kinase, an enzyme cru...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(94)90564-9

    authors: Barile M,Valenti D,Hobbs GA,Abruzzese MF,Keilbaugh SA,Passarella S,Quagliariello E,Simpson MV

    更新日期:1994-10-07 00:00:00

  • The role of adenosine A2A and A2B receptors in the regulation of TNF-alpha production by human monocytes.

    abstract::Adenosine is an endogenous nucleoside that regulates many physiological processes through the activation of its four receptors: A(1), A(2A), A(2B) and A(3). Previous studies have identified the involvement of A(2) receptors in the inhibitory activity of adenosine analogues on tumor necrosis factor-alpha (TNF-alpha) pr...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2004.12.008

    authors: Zhang JG,Hepburn L,Cruz G,Borman RA,Clark KL

    更新日期:2005-03-15 00:00:00

  • Suppressive effects of tranilast on the expression of inducible cyclooxygenase (COX2) in interleukin-1beta-stimulated fibroblasts.

    abstract::We investigated the effects of tranilast on inducible cyclooxygenase (COX2)-mediated prostaglandin E2 (PGE2) production and enzyme induction in interleukin-lbeta (IL-1beta)-stimulated cultured dermal fibroblasts. IL-1beta enhanced PGE2 production in cultured fibroblasts. Tranilast did not affect constitutive cyclooxyg...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(97)00187-1

    authors: Inoue H,Ohshima H,Kono H,Yamanaka M,Kubota T,Aihara M,Hiroi T,Yago N,Ishida H

    更新日期:1997-06-15 00:00:00

  • Inhibition of cellular thymidylate synthesis by cytotoxic propenal derivatives of pyrimidine bases and deoxynucleosides.

    abstract::A series of cytotoxic propenal (3-oxoprop-1-enyl) derivatives of pyrimidine bases and deoxynucleosides was evaluated for their ability to block thymidylate synthesis in intact and permeabilized murine leukemia L1210 cells. Several were potent inhibitors of this process, likely contributing to their cytotoxicity. The I...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90732-k

    authors: Kalman TI,Marinelli ER,Xu B,Reddy AR,Johnson F,Grollman AP

    更新日期:1991-07-05 00:00:00

  • 2',2'-Difluoro-deoxycytidine (gemcitabine) incorporation into RNA and DNA of tumour cell lines.

    abstract::Gemcitabine (dFdC) is a new cytidine analogue which is active mainly by the incorporation of its triphosphate (dFdCTP) into DNA, leading to cell death. We determined incorporation of dFdC into nucleic acids of two solid tumour cell lines: the murine colon carcinoma cell line Colon 26-10, the human ovarian carcinoma ce...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90566-f

    authors: Ruiz van Haperen VW,Veerman G,Vermorken JB,Peters GJ

    更新日期:1993-08-17 00:00:00

  • Effects of metyrapone on microsomal-dependent Salmonella mutagenesis. Studies with chloroallyl ethers and model compounds.

    abstract::Metyrapone (2-methyl-1,2-di-3-pyridyl-1-propanone, MTP) is used as an inhibitor of cytochrome P-450 enzymes, particularly those induced by phenobarbital (PB). We examined the effects of MTP on the microsomal dependent mutagenesis of a newly isolated promutagen, 3-(2-chloroethoxy)-1,2-dichloropropene (CP), three S-chlo...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(83)90144-2

    authors: Distlerath LM,Loper JC,Tabor MW

    更新日期:1983-12-15 00:00:00

  • Molecular mechanisms underlying the anti-obesity potential of prunetin, an O-methylated isoflavone.

    abstract::Prunetin is an O-methylated isoflavone, which is a type of flavonoid. There are a limited number of reports detailing the biological activities of prunetin. Although an anti-inflammatory effect of prunetin has been reported in vitro, to our knowledge, there have been no reports on anti-adipogenic effects of prunetin i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2013.02.020

    authors: Ahn TG,Yang G,Lee HM,Kim MD,Choi HY,Park KS,Lee SD,Kook YB,An HJ

    更新日期:2013-05-15 00:00:00

  • Effects of full and partial beta-adrenergic agonists and antagonists on human lung adenylate cyclase.

    abstract::The beta-adrenergic stimulation of adenylate cyclase in membranes from human lung was compared to that of adenylate cyclase in membranes with a majority of beta 2-adrenergic receptors (from rat lung) and in membranes with a homogeneous population of beta 2-adrenergic receptors (from rat erythrocytes and reticulocytes)...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(83)90046-1

    authors: Delhaye M,Taton G,Camus JC,Chatelain P,Robberecht P,Waelbroeck M,Christophe J

    更新日期:1983-06-15 00:00:00

  • Inhibition of desmethylimipramine 2-hydroxylation by drugs in human liver microsomes.

    abstract::The 2-hydroxylation of desmethylimipramine (DMI) correlates strongly with the 4-hydroxylation of debrisoquine (D) both in human volunteers and in vitro comparing human liver microsomes from different individuals. D competitively inhibits the 2-hydroxylation of DMI in vitro suggesting that DMI is hydroxylated by the 'd...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90533-7

    authors: von Bahr C,Spina E,Birgersson C,Ericsson O,Göransson M,Henthorn T,Sjöqvist F

    更新日期:1985-07-15 00:00:00

  • Effects of chronic low-level lead exposure on mRNA expression, ADP-ribosylation and photoaffinity labeling with [alpha-32P]guanine triphosphate-gamma-azidoanilide of GTP-binding proteins in neurons isolated from the brain of neonatal and adult rats.

    abstract::The effects of chronic lead exposure on mRNA expression, ADP-ribosylation and photoaffinity labeling with [alpha-32P]guanine triphosphate-gamma-azidoanilide ([32P]GTP-A) of alpha i or alpha s subunit of G protein were investigated in neurons isolated from the brain of neonatal and adult rats exposed to lead acetate or...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(93)90255-u

    authors: Singh AK

    更新日期:1993-03-09 00:00:00

  • Characterization of sequence-dependent synergy between ZD1839 ("Iressa") and oxaliplatin.

    abstract:UNLABELLED:ZD1839 ("Iressa"), a selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI), is currently undergoing preclinical and clinical evaluation in several solid tumors. The present study aimed to assess the effect of ZD1839 in combination with oxaliplatin in the colon cancer cell lines HT-2...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/s0006-2952(03)00291-0

    authors: Xu JM,Azzariti A,Severino M,Lu B,Colucci G,Paradiso A

    更新日期:2003-08-15 00:00:00

  • RETRACTED: Glutathione as a mediator of apoptotic cell signaling pathways.

    abstract::This article has been retracted consistent with Elsevier Policy on Article Withdrawal. Please see . The Publisher apologises for any inconvenience this may cause. ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2006.03.026

    authors: Cristofanon S,Dicato M,Ghibelli L,Diederich M

    更新日期:2006-04-18 00:00:00

  • Hepatic subcellular distribution of manganese in manganese and manganese-bilirubin induced cholestasis.

    abstract::Administration of non-cholestatic doses of manganese (Mn2+) followed by injection of bilirubin (BR) results in a severe reduction in rat bile flow. Male Sprague-Dawley rats were given various doses of Mn2+ (2, 4.5, 8, and 18 mg/kg, i.v.) and killed 0.25, 1, 3, or 5 hr later. 54Mn2+ was used to evaluate Mn2+ content (m...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(85)90435-6

    authors: Ayotte P,Plaa GL

    更新日期:1985-11-01 00:00:00

  • Andrographolide derivative ameliorates dextran sulfate sodium-induced experimental colitis in mice.

    abstract::The therapeutic efficacy of immunosuppressive agents has been intensively studied for colitis management. We synthesized a series of andrographolide derivatives and reported their structure-activity-relationship and anti-inflammatory activity in our previous studies. Among these derivatives, compound 3b exhibited the ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2019.03.019

    authors: Guo BJ,Liu Z,Ding MY,Li F,Jing M,Xu LP,Wang YQ,Zhang ZJ,Wang Y,Wang D,Zhou GC,Wang Y

    更新日期:2019-05-01 00:00:00

  • Enhancement by beraprost sodium, a stable analogue of prostacyclin, in thrombomodulin expression on membrane surface of cultured vascular endothelial cells via increase in cyclic AMP level.

    abstract::Prostacyclin and beraprost sodium (beraprost), a stable analogue of prostacyclin, increased cyclic AMP (cAMP) levels of cultured human umbilical vein endothelial cells (HUVEC) in a concentration-dependent manner. The elevation of cAMP by beraprost was sustained longer than that by prostacyclin. The expression of throm...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(91)90651-k

    authors: Kainoh M,Maruyama I,Nishio S,Nakadate T

    更新日期:1991-04-15 00:00:00

  • Licochalcone A is a potent inhibitor of TEL-Jak2-mediated transformation through the specific inhibition of Stat3 activation.

    abstract::Aberrant activation of Jak/Stat signaling causes a number of hematopoietic disorders and oncogenesis, and therefore the effective inhibitors of the Jak/Stat signaling pathway may be therapeutically useful. TEL-Jak2 gene fusion, which has been identified in human leukemia, encodes a chimeric protein endowed with consti...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2008.09.012

    authors: Funakoshi-Tago M,Tago K,Nishizawa C,Takahashi K,Mashino T,Iwata S,Inoue H,Sonoda Y,Kasahara T

    更新日期:2008-12-15 00:00:00

  • Azelastine and flezelastine as reversing agents of multidrug resistance: pharmacological and molecular studies.

    abstract::The effects of two new phthalazinone derivatives, azelastine (AZ) and flezelastine (FZ), on the reversal of resistance to doxorubicin (dox) were studied using two variants of the rat C6 glioblastoma cell line, selected with dox (C6 0.5) or with vincristine (C6 1V). Both lines presented a multidrug-resistant phenotype ...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(95)00130-r

    authors: Hu YP,Robert J

    更新日期:1995-07-17 00:00:00

  • Isolation, synthesis and characterization of ω-TRTX-Cc1a, a novel tarantula venom peptide that selectively targets L-type Cav channels.

    abstract::Spider venoms are replete with peptidic ion channel modulators, often with novel subtype selectivity, making them a rich source of pharmacological tools and drug leads. In a search for subtype-selective blockers of voltage-gated calcium (CaV) channels, we isolated and characterized a novel 39-residue peptide, ω-TRTX-C...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2014.02.008

    authors: Klint JK,Berecki G,Durek T,Mobli M,Knapp O,King GF,Adams DJ,Alewood PF,Rash LD

    更新日期:2014-05-15 00:00:00

  • Regulation of nicotinic acetylcholine receptors on human neuroblastoma cells during differentiation.

    abstract::Neuronal nicotinic acetylcholine receptors are expressed on a variety of cells in the nervous system where they play key roles in synaptic transmission and information transfer. Little is known, however, about the molecular mechanisms that control their expression, distribution, and function during nervous system deve...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(95)02067-5

    authors: Halvorsen SW,Jiang N,Malek R

    更新日期:1995-11-09 00:00:00

  • Molecular and functional characterization of flavin-containing monooxygenases in cynomolgus macaque.

    abstract::Flavin-containing monooxygenases (FMOs), drug-metabolizing enzymes essential for the metabolism of endogenous biochemicals and foreign compounds, have been characterized in human (including FMO1-5 and FMO6P), but remain to be investigated in cynomolgus macaque. In this study, cDNAs of cynomolgus FMO1-5 and FMO6 were i...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2013.04.012

    authors: Uno Y,Shimizu M,Yamazaki H

    更新日期:2013-06-15 00:00:00

  • Novel mode of cytotoxicity obtained by coupling inactive anthracycline to a polymer.

    abstract::The inactive anthracycline analog 4-demethoxy-7,9-di-epi-daunorubicin was covalently coupled to polyglutaraldehyde microspheres. The polymer-bound analog acquired significant cytostatic activity as evaluated with doxorubicin resistant and sensitive murine L1210 leukemia cells. A suggested multiple membrane interaction...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(84)90315-0

    authors: Rogers KE,Tökés ZA

    更新日期:1984-02-15 00:00:00

  • A contribution to the mechanism of action of SAD-128.

    abstract::SAD-128 was found to be an effective protector of acetylcholinesterase against inhibition by soman, due to its ability to function as a reversible inhibitor and allosteric modifier of the AChE active site. It also attenuated aging of the soman-inhibited enzyme. In order to study the connection between some of these ef...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/0006-2952(90)90093-z

    authors: Stalc A,Sentjurc M

    更新日期:1990-12-01 00:00:00

  • Thioredoxin reductase 1 knockdown enhances selenazolidine cytotoxicity in human lung cancer cells via mitochondrial dysfunction.

    abstract::Thioredoxin reductase (TR1) is a selenoprotein that is involved in cellular redox status control and deoxyribonucleotide biosynthesis. Many cancers, including lung, overexpress TR1, making it a potential cancer therapy target. Previous work has shown that TR1 knockdown enhances the sensitivity of cancer cells to antic...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2010.09.024

    authors: Poerschke RL,Moos PJ

    更新日期:2011-01-15 00:00:00

  • Ca2+/calmodulin-dependent protein kinase II regulation by inhibitor 1 of protein phosphatase 1 alleviates necroptosis in high glucose-induced cardiomyocytes injury.

    abstract::Ca2+/calmodulin-dependent protein kinase II (CaMKII) plays an important role in the cardiovascular system. However, the potential protective role of inhibitor 1 of protein phosphatase 1 (I1PP1), which is able to regulate CaMKII, in high glucose-induced cardiomyocytes injury remains unknown. In the present study, cardi...

    journal_title:Biochemical pharmacology

    pub_type: 杂志文章

    doi:10.1016/j.bcp.2019.02.022

    authors: Sun L,Chen Y,Luo H,Xu M,Meng G,Zhang W

    更新日期:2019-05-01 00:00:00