当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Inactivation by acivicin of carbamoyl-phosphate synthetase II of human colon carcinoma.

Inactivation by acivicin of carbamoyl-phosphate synthetase II of human colon carcinoma.

Abstract：

:The effect of the anti-tumor, anti-glutamine drug acivicin, L-(alpha S,5S)-alpha-amino-3-chloro-4,5-dihydro-5-isoxazoleacetic acid, was determined on the activity of the rate-limiting enzyme of de novo pyrimidine biosynthesis, carbamoyl-phosphate synthetase II (glutamine-hydrolyzing) (EC 6.3.5.5), in human colon carcinoma. The synthetase II activity in human colon carcinoma was elevated 2- to 3-fold over values of the normal colon mucosa, and the substrate kinetic constants were similar for the enzyme in normal and neoplastic colon. The Km for glutamine was 17 microM (colon carcinoma) and 23 microM (normal mucosa), whereas the Km for ATP was 2.1 and 1.7 mM in tumor and mucosa respectively. The synthetase II activity in colon carcinoma was inhibited to a similar extent by UMP, UDP and UTP (36-41%). The three uracil nucleotides were also equally effective in inhibiting the enzyme from normal mucosa (39-46%). Both enzymes were activated by PRPP (63 and 57%) in mucosa and carcinoma respectively. Acivicin in vitro selectively inactivated the glutamine-dependent synthetase II from human colon carcinoma, and it did not affect the ammonia-dependent activity. The acivicin inactivation constant (Kinact) was 100 microM, and the minimum inactivation half-time (T) was 0.7 min. Acivicin most likely exerts its effect against human colon synthetase II by acting as an active site directed affinity analogue of L-glutamine.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Sebolt JS,Aoki T,Eble JN,Glover JL,Weber G

doi

10.1016/0006-2952(85)90106-6

subject

Has Abstract

pub_date

1985-01-01 00:00:00

pages

97-100

issue

1

eissn

0006-2952

issn

1873-2968

pii

0006-2952(85)90106-6

journal_volume

34

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • Inhibition of human red blood cell glutathione reductase by valproic acid.

    abstract：:Glutathione reductase (GR) one of the enzymes of the glutathione redox cycle, plays a salient role in maintaining appropriate cellular levels of reduced glutathione. The enzyme in human red blood cells is inhibited in vitro by the anticonvulsant drug valproic acid (VPA). The inhibition is dose-dependent, reversible, u...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(92)90559-2

    authors： Cotariu D,Evans S,Lahat E,Theitler J,Bistritzer T,Zaidman JL

    更新日期：1992-02-04 00:00:00

  • Regulation on SIRT1-PGC-1α/Nrf2 pathway together with selective inhibition of aldose reductase makes compound hr5F a potential agent for the treatment of diabetic complications.

    abstract：:(R,E)-N-(3-(2-acetamido-3-(benzyloxy) propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide (hr5F) was design-synthesized based on bioactivity focus strategy as a potential agent to treat diabetic complicates. With in vitro enzyme assay, it is confirmed that hr5F is an effective ALR2 inhibitor with IC50 value of ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2018.01.034

    authors： Wang Z,Yuan S,Li Y,Zhang Z,Xiao W,Tang D,Ye K,Liu Z,Wang C,Zheng Y,Nie H,Chen H

    更新日期：2018-04-01 00:00:00

  • Stimulation and inhibition of adenylyl cyclase by distinct 5-hydroxytryptamine receptors.

    abstract：:5-Hydroxytryptamine (serotonin, 5-HT) stimulates basal adenylyl cyclase activity in membranes from guinea pig or rat hippocampi, but 5-HT inhibits forskolin-stimulated adenylyl cyclase activity in these same membranes. The opposing effects of 5-HT on adenylyl cyclase activity indicate that distinct 5-HT receptors, pos...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90453-r

    authors： De Vivo M,Maayani S

    更新日期：1990-10-01 00:00:00

  • Thymoquinone poly (lactide-co-glycolide) nanoparticles exhibit enhanced anti-proliferative, anti-inflammatory, and chemosensitization potential.

    abstract：:Thymoquinone (TQ), derived from the medicinal spice Nigella sativa (also called black cumin), has been shown to exhibit anti-inflammatory and anti-cancer activities. In this report we employed polymer-based nanoparticle approach to improve upon its effectiveness and bioavailability. TQ was encapsulated with 97.5% effi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,收录出版

    doi：10.1016/j.bcp.2010.01.023

    authors： Ravindran J,Nair HB,Sung B,Prasad S,Tekmal RR,Aggarwal BB

    更新日期：2010-06-01 00:00:00

  • Effects of five anion channel blockers on thrombin- and ionomycin-activated platelet functions.

    abstract：:The inhibitory effects of anion channel blockers were evaluated on aggregation, intracellular Ca2+ rises, and the production of arachidonic acid metabolites in human platelets. Inhibitors included five anion channel blockers: phloretin, probenecid, pyridoxal phosphate, 4,4'-diisothiocyano-2,2'-disulfonic acid stilbene...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90069-5

    authors： Ozaki Y,Matsumoto Y,Yatomi Y,Higashihara M,Kariya T,Shoji K

    更新日期：1989-07-01 00:00:00

  • Reduction of dihydroxyphenylacetic acid by a novel enzyme in the rat brain.

    abstract：:A novel enzyme that converts dihydroxyphenylacetic acid (DOPAC) to dihydroxyphenylethanol (DOPET) was found to be present in the microdialysate of the rat brain. The enzyme, named DOPAC reductase, was inhibited by EDTA and stimulated by divalent cations like Zn2+, Mn2+, Co2+ and Cu2+. Its Km, pH optimum and temperatur...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)02092-6

    authors： Xu CL,Sim MK

    更新日期：1995-10-26 00:00:00

  • A study of correlation between NPM-translocation and apoptosis in cells induced by daunomycin.

    abstract：:Human leukemia K562 and HeLa cells were treated with daunomycin (DA) for 1-4 hr. With the indirect immunofluorescence technique, we observed that the nucleolar protein nucleophosmin/B23 (NPM) shifted its location from the nucleolus to the nucleoplasm (NPM-translocation). The degree of NPM-translocation was determined ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00043-x

    authors： Chan PK,Chan FY

    更新日期：1999-06-01 00:00:00

  • Pharmacological characterization of glucocorticoid receptors in primary human bronchial epithelial cells.

    abstract：:Bronchial epithelial cells play an important role in amplifying and perpetuating airway inflammation and may be a target for inhaled steroids. We have characterized glucocorticoid receptors in primary human bronchial epithelial cells. Northern and western blot analyses demonstrated the expression of glucocorticoid rec...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00008-8

    authors： LeVan TD,Babin EA,Yamamura HI,Bloom JW

    更新日期：1999-05-01 00:00:00

  • Src, N-methyl-D-aspartate (NMDA) receptors, and synaptic plasticity.

    abstract：:The protein tyrosine kinase Src is expressed widely in the central nervous system and is abundant in neurons. Over the past several years, evidence has accumulated showing that one function of Src is to regulate the activity of N-methyl-D-aspartate (NMDA) receptors and other ion channels. NMDA receptors are a principa...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/s0006-2952(98)00124-5

    authors： Salter MW

    更新日期：1998-10-01 00:00:00

  • The anti-inflammatory actions of LCY-2-CHO, a carbazole analogue, in vascular smooth muscle cells.

    abstract：:LCY-2-CHO has anti-inflammatory actions on macrophages. To understand its therapeutic implication in atherosclerosis, we examined its effects on the expressions of anti-inflammatory and inflammatory proteins in cultured rat aortic vascular smooth muscle cells (VSMC). LCY-2-CHO is able to induce heme oxygenase-1 (HO-1)...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2007.04.008

    authors： Ho FM,Kang HC,Lee ST,Chao Y,Chen YC,Huang LJ,Lin WW

    更新日期：2007-07-15 00:00:00

  • Snake three-finger α-neurotoxins and nicotinic acetylcholine receptors: molecules, mechanisms and medicine.

    abstract：:Snake venom three-finger α-neurotoxins (α-3FNTx) act on postsynaptic nicotinic acetylcholine receptors (nAChRs) at the neuromuscular junction (NMJ) to produce skeletal muscle paralysis. The discovery of the archetypal α-bungarotoxin (α-BgTx), almost six decades ago, exponentially expanded our knowledge of membrane rec...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2020.114168

    authors： Nirthanan S

    更新日期：2020-11-01 00:00:00

  • Decreased polyphenol transport across cultured intestinal cells by a salivary proline-rich protein.

    abstract：:Tannins are polyphenols commonly found in plant-derived foods. When ingested they can have various harmful effects, but salivary proline-rich proteins (PRPs) may provide protection against dietary tannins. The aim of this study was to investigate whether basic PRPs, a major family of salivary proteins, can prevent int...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2006.02.013

    authors： Cai K,Hagerman AE,Minto RE,Bennick A

    更新日期：2006-05-28 00:00:00

  • Resveratrol inhibits BK-induced COX-2 transcription by suppressing acetylation of AP-1 and NF-κB in human rheumatoid arthritis synovial fibroblasts.

    abstract：:Bradykinin (BK) induces inflammation in rheumatoid arthritis (RA). Resveratrol is a potent activator of Sirt1 which could modulate inflammation through deacetylating histones of transcription factors. Here, we investigated the mechanisms underlying BK-induced COX-2 expression which is modulated by resveratrol/Sirt1 in...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2017.03.003

    authors： Yang CM,Chen YW,Chi PL,Lin CC,Hsiao LD

    更新日期：2017-05-15 00:00:00

  • Rosuvastatin reduces platelet recruitment by inhibiting NADPH oxidase activation.

    abstract：:Rosuvastatin increased vascular endothelial NO and attenuated platelet activation after ischemia-reperfusion in mice; nevertheless, the influence of rosuvastatin on the activation of human platelets and the underlying mechanism has never been investigated. In an in vitro study platelets from 8 healthy donors were incu...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2012.09.011

    authors： Pignatelli P,Carnevale R,Di Santo S,Bartimoccia S,Nocella C,Vicario T,Loffredo L,Angelico F,Violi F

    更新日期：2012-12-15 00:00:00

  • A 62 kDa protein is photoaffinity labelled by [3H]felodipine in vascular smooth muscle, but not in cardiac and skeletal muscle.

    abstract：:Irradiation of a cytosolic fraction from vascular smooth muscle in the presence of [3H]felodipine resulted in the labelling of a protein with an apparent molecular weight of 62 kDa. The labelling was seen on UV-irradiation at 360 nm, but not at 254, 278 or at wavelengths above 410 nm. The photolabelling was enhanced i...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90516-9

    authors： Nilsson A,Westerlund C,Boström S

    更新日期：1989-12-01 00:00:00

  • Inhibition of soluble glutathione S-transferase by diuretic drugs.

    abstract：:Glutathione transferases are believed to play an important protective role in the various tissues of animals and man by catalysing the glutathione conjugation of electrophilic drugs and electrophilic drug metabolites. Many of these compounds have the potential to react with vital cellular macromolecules in the absence...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90549-5

    authors： Ahokas JT,Davies C,Ravenscroft PJ,Emmerson BT

    更新日期：1984-06-15 00:00:00

  • Effect of superoxide dismutase on glomerular nephritis.

    abstract：:The antiinflammatory effect of superoxide dismutase was studied in rats with kidney intoxication induced by the injection of nephrotoxic serum. The urinary excretion of protein was increased significantly by the administration of an intravenous injection of nephrotoxic serum. The daily injection of superoxide dismutas...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(86)90536-8

    authors： Adachi T,Fukuta M,Ito Y,Hirano K,Sugiura M,Sugiura K

    更新日期：1986-01-15 00:00:00

  • Inhibition of heart mitochondrial lipid peroxidation by non-toxic concentrations of carvedilol and its analog BM-910228.

    abstract：:Carvedilol, a non-selective beta-adrenoreceptor blocker, has been shown to possess a high degree of cardioprotection in experimental models of myocardial damage. Reactive oxygen species have been proposed to be implicated in such situations, and antioxidants have been demonstrated to provide partial protection to the ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00522-0

    authors： Santos DJ,Moreno AJ

    更新日期：2001-01-15 00:00:00

  • The influence of tumour microenvironmental factors on the efficacy of cisplatin and novel platinum(IV) complexes.

    abstract：:The chemotherapeutic drug cisplatin is an important treatment for many types of solid tumours, in particular non-small cell lung cancer (NSCLC). Platinum(IV) complexes offer several advantages to cisplatin due to their requirement for reduction to the active platinum(II) form to elicit cytotoxicity. This should minimi...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2005.07.016

    authors： Mellor HR,Snelling S,Hall MD,Modok S,Jaffar M,Hambley TW,Callaghan R

    更新日期：2005-10-15 00:00:00

  • Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in human myeloid leukemia cell lines.

    abstract：:We investigated the effect of aphidicolin, an inhibitor of DNA polymerase alpha and delta, on the induction of apoptosis by arabinosyl nucleosides in a human promyelocytic leukemia cell line, HL-60. Pretreatment of HL-60 cells with aphidicolin (2 microM) significantly increased the number of morphologically apoptotic ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(93)90631-6

    authors： Kuwakado K,Kubota M,Hirota H,Adachi S,Matsubara K,Kasai Y,Akiyama Y,Mikawa H

    更新日期：1993-12-03 00:00:00

  • The in vitro ketone reduction of warfarin and analogues. Substrate stereoselectivity, product stereoselectivity and species differences.

    abstract：:The in vitro metabolic ketone reduction of warfarin and its 4'-analogues acenocoumarol (4'-nitrowarfarin) and 4'-chlorowarfarin has been investigated using microsomal and cytosolic fractions of several species. Both subcellular fractions showed ketone reductase activity. The cytosolic fractions, in most species, exhib...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90635-7

    authors： Hermans JJ,Thijssen HH

    更新日期：1989-10-01 00:00:00

  • Binding of [3H]perhydrohistrionicotoxin and [3H]phencyclidine to the nicotinic receptor-ion channel complex of Torpedo electroplax. Inhibition by histrionicotoxins and derivatives.

    abstract：:Histrionicotoxin, a spiropiperidine alkaloid, and twenty-two analogs inhibited binding of [3H]perhydrohistrionicotoxin [( 3H]H12-HTX) and of [3H]phencyclidine [( 3H]PCP) to sites on the acetylcholine receptor-ion complex of Torpedo electroplax membranes. Structural alterations to the nitrogen (secondary amine) or oxyg...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(85)90145-5

    authors： Aronstam RS,King CT Jr,Albuquerque EX,Daly JW,Feigl DM

    更新日期：1985-09-01 00:00:00

  • Histamine H3-receptor signaling in cardiac sympathetic nerves: Identification of a novel MAPK-PLA2-COX-PGE2-EP3R pathway.

    abstract：:We hypothesized that the histamine H(3)-receptor (H(3)R)-mediated attenuation of norepinephrine (NE) exocytosis from cardiac sympathetic nerves results not only from a Galpha(i)-mediated inhibition of the adenylyl cyclase-cAMP-PKA pathway, but also from a Gbetagamma(i)-mediated activation of the MAPK-PLA(2) cascade, c...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2007.01.001

    authors： Levi R,Seyedi N,Schaefer U,Estephan R,Mackins CJ,Tyler E,Silver RB

    更新日期：2007-04-15 00:00:00

  • Isoprenaline induction of cAMP-phosphodiesterase in guinea-pig macrophages occurs in the presence, but not in the absence, of the phosphodiesterase type IV inhibitor rolipram.

    abstract：:The long-term effects of incubating freshly isolated, elicited guinea-pig peritoneal macrophages with the beta-adrenoceptor agonist isoprenaline and the selective inhibitor of phosphodiesterase (PDE) IV rolipram, on adenosine-3',5'-cyclic phosphate (cAMP)-specific PDE IV activity have been investigated. The level of c...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)02104-3

    authors： Kochetkova M,Burns FM,Souness JE

    更新日期：1995-12-22 00:00:00

  • Stimulation by gamma-carboline derivatives (simplified analogues of antitumor ellipticines) of site specific DNA cleavage by calf DNA topoisomerase II.

    abstract：:gamma-Carbolines are tricyclic aromatic compounds which intercalate into DNA base pairs and exhibit significant cytotoxic and antitumor activities. These compounds which are structurally related to ellipticine by deletion of an aromatic ring, induce DNA breaks in cultured L1210 cells. Since the mechanism of cytotoxic ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(90)90144-a

    authors： Fossé P,René B,Saucier JM,Nguyen CH,Bisagni E,Paoletti C

    更新日期：1990-02-15 00:00:00

  • Experimental and computer graphics simulation analyses of the DNA interaction of 1,8-bis-(2-diethylaminoethylamino)-anthracene-9,10-dione, a compound modelled on doxorubicin.

    abstract：:The crystal structure of the anthraquinone derivative 1,8-bis-(2-diethylaminoethylamino)-anthracene-9,10-dione has been established. This compound was prepared as a potential DNA-intercalating agent based on the proven intercalators doxorubicin and mitoxantrone. Its DNA-binding properties have been examined experiment...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(83)90095-3

    authors： Islam SA,Neidle S,Gandecha BM,Brown JR

    更新日期：1983-09-15 00:00:00

  • Quercetin pretreatment increases the bioavailability of pioglitazone in rats: involvement of CYP3A inhibition.

    abstract：:Herbal antidiabetic preparations are often used as an add-on therapy in diabetes and such herbal preparations often contains quercetin that can inhibit cytochrome P450 (CYP) 3A4. This enzyme is responsible for metabolizing pioglitazone, a commonly used antidiabetic agent. Hence, it was speculated that quercetin may in...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2008.01.010

    authors： Umathe SN,Dixit PV,Kumar V,Bansod KU,Wanjari MM

    更新日期：2008-04-15 00:00:00

  • Measurement of affective state during chronic nicotine treatment and withdrawal by affective taste reactivity in mice: the role of endocannabinoids.

    abstract：:Despite tobacco being highly addictive, it is unclear if nicotine has significant affective properties. To address this, we studied taste reactions to gustatory stimuli, palatable sucrose and unpalatable quinine, which are believed to reflect ongoing affective state. Taste reactivity was assessed during chronic nicoti...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2009.06.017

    authors： Wing VC,Cagniard B,Murphy NP,Shoaib M

    更新日期：2009-10-01 00:00:00

  • Distinction of microsomal prostaglandin E synthase-1 (mPGES-1) inhibition from cyclooxygenase-2 inhibition in cells using a novel, selective mPGES-1 inhibitor.

    abstract：:Inflammation-induced microsomal prostaglandin E synthase-1 (mPGES-1) is the terminal enzyme that synthesizes prostaglandin E(2) (PGE(2)) downstream of cyclooxygenase-2 (COX-2). The efficacy of nonsteroidal anti-inflammatory drugs and COX-2 inhibitors in the treatment of the signs and symptoms of osteoarthritis, rheuma...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2010.01.003

    authors： Mbalaviele G,Pauley AM,Shaffer AF,Zweifel BS,Mathialagan S,Mnich SJ,Nemirovskiy OV,Carter J,Gierse JK,Wang JL,Vazquez ML,Moore WM,Masferrer JL

    更新日期：2010-05-15 00:00:00

  • Characterization of heme oxygenase activity in Leydig and Sertoli cells of the rat testes. Differential distribution of activity and response to cadmium.

    abstract：:Leydig and Sertoli cells of the rat testes differ with respect to the activities of the enzymes of the heme and hemoprotein degradative pathway and in their responses to Cd2+ treatment. The microsomal heme oxygenase activity in the Leydig cell preparations was nearly 9- to 10-fold greater than in Sertoli cell preparat...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(84)90418-0

    authors： Maines MD

    更新日期：1984-05-01 00:00:00