当前位置： SCI文献检索 > BIOCHEMICAL PHARMACOLOGY期刊下所有文献 > Activation of human leukemia protein kinase C by tumor promoters and its inhibition by N-trifluoroacetyladriamycin-14-valerate (AD 32).

Activation of human leukemia protein kinase C by tumor promoters and its inhibition by N-trifluoroacetyladriamycin-14-valerate (AD 32).

Abstract：

:N-Trifluoroacetyladriamycin-14-valerate (AD 32), a lipophilic, DNA non-binding analog of Adriamycin (ADR), was found to be a potent inhibitor of the membrane-bound enzyme, protein kinase C (PKC). PKC was isolated and purified from human leukemia ML-1 cells, and the enzyme activity was shown to be activated by the tumor promoters 12-O-tetradecanoylphorbol-13-acetate (TPA) and phorbol-12,13-dibutyrate (PDBu). AD 32, nevertheless, inhibited the activation of PKC by TPA or PDBu. The IC50 values for AD 32 inhibition of PKC activation were 0.85 microM for TPA and 1.25 microM for PDBu. Under the same assay conditions, ADR demonstrated much higher IC50 values: 550 microM for TPA and greater than 350 microM for PDBu. The inhibition of PKC by AD 32 was further shown to be competitive in nature; AD 32 inhibited the binding of [3H]PDBu to PKC. Therefore, AD 32 competes with the tumor promoter for the PKC binding site and prevents the latter from both interacting with the phospholipid and binding to PKC. These effects of AD 32 were reproduced in situ; incubation of human leukemia ML-1 cells with TPA showed an increased phosphorylation of cellular proteins, and the TPA-induced protein phosphorylation was inhibited by the addition of AD 32 to the cultured cells.

journal_name

Biochem Pharmacol

journal_title

Biochemical pharmacology

authors

Chuang LF,Kung HF,Israel M,Chuang RY

doi

10.1016/0006-2952(92)90254-g

subject

Has Abstract

pub_date

1992-02-18 00:00:00

pages

865-72

issue

4

eissn

0006-2952

issn

1873-2968

pii

0006-2952(92)90254-G

journal_volume

43

pub_type

杂志文章

相关文献

BIOCHEMICAL PHARMACOLOGY文献大全
  • Effect of aspirin on induction of apoptosis in HT-29 human colon adenocarcinoma cells.

    abstract：:Aspirin (ASA) and other nonsteroidal anti-inflammatory drugs (NSAIDs) inhibit colorectal tumorigenesis. Apoptosis is a critical determinant of tissue mass homeostasis and may play a role in carcinogenesis. We studied the effect of ASA on the survival of a human colon cancer cell line using more sensitive methods than ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(97)00400-0

    authors： Qiao L,Hanif R,Sphicas E,Shiff SJ,Rigas B

    更新日期：1998-01-01 00:00:00

  • Instability of (ara-C) DNA under alkaline conditions.

    abstract：:We employed both [5-3H] ara-C and ([2-14C] ara-C labeled L1210 DNA for analysis following exposure to alkali under various conditions. The results demonstrated that the tritium label on C5 of ara-C molecules incorporated in DNA was exchanged with water under alkaline conditions and, therefore, radioactivity was subseq...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90475-0

    authors： Major PP,Egan EM,Herrick D,Kufe DW

    更新日期：1982-03-01 00:00:00

  • Differential signaling of human Mel1a and Mel1b melatonin receptors through the cyclic guanosine 3'-5'-monophosphate pathway.

    abstract：:Cyclic guanosine 3'-5'-monophosphate (cGMP) has recently been shown to constitute a second messenger for Xenopus laevis melatonin Mel1c receptors. To verify whether cGMP levels are also modulated by mammalian melatonin receptors, we cloned the genes encoding the human Mel1a and Mel1b receptor subtypes and expressed th...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00134-3

    authors： Petit L,Lacroix I,de Coppet P,Strosberg AD,Jockers R

    更新日期：1999-08-15 00:00:00

  • Cross talk of cAMP and flavone in regulation of cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channel and Na+/K+/2Cl- cotransporter in renal epithelial A6 cells.

    abstract：:We have reported that in renal epithelial A6 cells flavones stimulate the transepithelial Cl- secretion by activating the cystic fibrosis transmembrane conductance regulator (CFTR) Cl- channel and/or the Na+/K+/2Cl- cotransporter. On the other hand, it has been established that cAMP activates the CFTR Cl- channel and ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2003.10.026

    authors： Niisato N,Nishino H,Nishio K,Marunaka Y

    更新日期：2004-02-15 00:00:00

  • Molecular pharmacology of endothelin converting enzymes.

    abstract：:A critical processing step in endothelin biosynthesis is the conversion of the intermediate "big endothelin" to its biologically active product catalysed by endothelin converting enzyme (ECE). In this commentary we discuss critically the cellular location, structure, and activity of the isoforms of ECE. The current ev...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/0006-2952(95)02036-5

    authors： Turner AJ,Murphy LJ

    更新日期：1996-01-26 00:00:00

  • N-butyldeoxygalactonojirimycin: a more selective inhibitor of glycosphingolipid biosynthesis than N-butyldeoxynojirimycin, in vitro and in vivo.

    abstract：:N-Butyldeoxynojirimycin (NB-DNJ) inhibits the ceramide glucosyltransferase which catalyses the first step in glycosphingolipid (GSL) biosynthesis. It has the potential to be used for the treatment of the GSL lysosomal storage diseases and is currently in clinical trials for the treatment of type 1 Gaucher's disease. H...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00384-6

    authors： Andersson U,Butters TD,Dwek RA,Platt FM

    更新日期：2000-04-01 00:00:00

  • Lipocortin 1 and the control of cPLA2 activity in A549 cells. Glucocorticoids block EGF stimulation of cPLA2 phosphorylation.

    abstract：:Epidermal growth factor (EGF) rapidly stimulates the release of arachidonic acid in A549 cells by a mechanism that is sensitive to pertussis toxin [1]. We show that EGF treatment of A549 cells stimulates phosphorylation of cytosolic phospholipase A2 (cPLA2) through a mechanism that is similarly inhibited by pertussis ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)02442-5

    authors： Croxtall JD,Choudhury Q,Newman S,Flower RJ

    更新日期：1996-07-26 00:00:00

  • HIF-1: master and commander of the hypoxic world. A pharmacological approach to its regulation by siRNAs.

    abstract：:The hypoxia-inducible factor-1 (HIF-1) is primarily involved in the sensing and adapting of cells to changes in the O2 level, which is essential for their viability. It is important that this critical transcription factor be tightly regulated in order for cells to respond to a wide range of O2 concentrations. HIF-1 re...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.bcp.2004.04.022

    authors： Mazure NM,Brahimi-Horn MC,Berta MA,Benizri E,Bilton RL,Dayan F,Ginouvès A,Berra E,Pouysségur J

    更新日期：2004-09-15 00:00:00

  • Mechanism for Helicobacter pylori stimulation of interleukin-8 production in a gastric epithelial cell line (MKN 28): roles of mitogen-activated protein kinase and interleukin-1beta.

    abstract：:Although it is known that the pathogenic mechanism of Helicobacter pylori involves the stimulated production of interleukin-8 (IL-8) as an inflammatory mediator, the details of the pathway remain unclear. The role of mitogen-activated protein kinase (MAPK) in IL-8 production by H. pylori has been examined in an in vit...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(01)00628-1

    authors： Yamada H,Aihara T,Okabe S

    更新日期：2001-06-15 00:00:00

  • Hydroxypropyl-beta-cyclodextrin as delivery system for thyroid hormones, regulating glutathione S-transferase expression in rat hepatocyte co-cultures.

    abstract：:Thyroid hormones play a role in the regulation of glutathione S-transferase (GST) expression. Here, co-cultures of rat hepatocytes with bile duct epithelial cells have been used to study the direct effects of both triiodothyronine (T3) and thyroxine (T4) on GST activities and proteins. Because T3 and T4 are poorly wat...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(01)00557-3

    authors： Vanhaecke T,Derde MP,Vercruysse A,Rogiers V

    更新日期：2001-05-01 00:00:00

  • On the binding of a 3-alpha-methylated digitoxigenin-glucoside to ouabain receptors in heart muscle homogenate.

    abstract：:3-alpha-Methyl substituted digitoxigenin-3-beta-glucoside (methyl-dtg-gluc) displays unusual features, e.g. a high dissociation rate constant from its binding site leading to rapid reversibility of the inotropic and toxic effects, and a flat dose-response curve attaining higher inotropic maxima thus indicating an incr...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(82)90059-4

    authors： Lüllmann H,Mohr K

    更新日期：1982-08-01 00:00:00

  • The Bcr-Abl inhibitor GNF-7 inhibits necroptosis and ameliorates acute kidney injury by targeting RIPK1 and RIPK3 kinases.

    abstract：:Necroptosis is a form of programmed, caspase-independent cell death that is involved in various pathologic disorders such as ischemia/reperfusion injury, acute kidney injury and inflammatory bowel diseases. Identification of necroptosis inhibitors has great therapeutic potential for the treatment of necroptosis-associ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2020.113947

    authors： Qin X,Hu L,Shi SN,Chen X,Zhuang C,Zhang W,Jitkaew S,Pang X,Yu J,Tan YX,Wang HY,Cai Z

    更新日期：2020-07-01 00:00:00

  • Formation and retention and biological activity of N10-propargyl-5,8-dideazafolic acid (CB3717) polyglutamates in L1210 cells in vitro.

    abstract：:The formation, retention and biological activity of the polyglutamate metabolites of the thymidylate synthase (TS) inhibitor N10-propargyl-5,8-dideazafolic acid (CB3717) has been investigated in L1210 murine leukaemia cells grown in vitro. CB3717 polyglutamates were measured by HPLC using high specific activity 3H-CB3...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(88)90094-9

    authors： Sikora E,Jackman AL,Newell DR,Calvert AH

    更新日期：1988-11-01 00:00:00

  • Prodrug research: futile or fertile?

    abstract：:The objective of this Commentary is to help clarify and illustrate what prodrugs are, what they are not, which benefits they can offer, and what their limits are. To this end, a number of criteria of classification and evaluation are presented. This is followed by a discussion of the pharmaceutical, pharmacokinetic an...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2004.07.005

    authors： Testa B

    更新日期：2004-12-01 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

  • Prevention of UVB-induced photoinflammation and photoaging by a polymethoxy flavonoid, nobiletin, in human keratinocytes in vivo and in vitro.

    abstract：:Exposure to ultraviolet B (UVB) irradiation induces acute skin inflammation such as erythema (sunburn) and edema, and prostaglandin (PG)E2 in the epidermis plays an important role as its prominent mediator. In the present study, we investigated the effect of nobiletin (5,6,7,8,3',4'-hexamethoxy flavone) from Citrus de...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2004.04.006

    authors： Tanaka S,Sato T,Akimoto N,Yano M,Ito A

    更新日期：2004-08-01 00:00:00

  • Effect of D- or L-methionine and cysteine on the growth inhibitory effects of feeding 1% paracetamol to rats.

    abstract：:Rats fed 1% paracetamol in the diet failed to grow and a dose-dependent inhibition of growth was observed and found to be independent of hepatoxicity. Addition of 0.5% D- or L-methionine, or L-cysteine to a diet containing 1% paracetamol restored growth. Addition of L-methionine to the drinking water was equally effec...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(89)90048-8

    authors： McLean AE,Armstrong GR,Beales D

    更新日期：1989-01-15 00:00:00

  • Metabolism and mode of selective inhibition of human immunodeficiency virus replication by 3'-azido-2',3'-dideoxy-5-iodouridine and 3'-azido-2',3'-dideoxy-5-bromouridine.

    abstract：:3'-Azido-2',3'-dideoxy-5-iodouridine (AzIdUrd) and 3'-azido-2',3'-dideoxy-5-bromouridine (AzBdUrd), previously shown to be potent and selective inhibitors of human immunodeficiency virus replication in vitro were minimally toxic to the uninfected human lymphoid cell line H9 (IC50 = 197 and 590 microM, respectively). B...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(93)90396-e

    authors： August EM,Qian HY,Birks EM,Thombre UA,Lin TS,Prusoff WH

    更新日期：1993-01-07 00:00:00

  • Bioavailability of phylloquinone and menaquinones after oral and colorectal administration in vitamin K-deficient rats.

    abstract：:Rats were made vitamin K-deficient by feeding them a diet devoid of vitamin K and by rigorously preventing coprophagy. After one week, circulating prothrombin concentrations were between 5 and 10% of initial values, and various amounts of phylloquinone, menaquinone-4, and menaquinone-9 were given in a single dose eith...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(95)00202-b

    authors： Groenen-van Dooren MM,Ronden JE,Soute BA,Vermeer C

    更新日期：1995-09-07 00:00:00

  • Induction of human neutrophil apoptosis by nitric oxide donors: evidence for a caspase-dependent, cyclic-GMP-independent, mechanism.

    abstract：:This study investigated the regulatory effects of the major inflammatory mediator, nitric oxide (NO), on human neutrophil apoptosis in vitro. Co-culture of human neutrophils with the NO donors GEA 3162 (1,2,3,4-oxatriazolium,5-amino-3-(3,4-dichlorophenyl)-chloride) (10-100 microM) and 3-morpholino-sydnonimine (SIN-1) ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(99)00329-9

    authors： Ward C,Wong TH,Murray J,Rahman I,Haslett C,Chilvers ER,Rossi AG

    更新日期：2000-02-01 00:00:00

  • Cytotoxicity of dichloromethane diphosphonate and of 1-hydroxyethane-1,1-diphosphonate in the amoebae of the slime mould Dictyostelium discoideum. A 31P NMR study.

    abstract：:Two pyrophosphate analogues, dichloromethane diphosphonate (Cl2MDP), and 1-hydroxyethane-1,1-diphosphonate (EHDP), at concentrations of 0.5-1 mM, efficiently inhibited the growth of amoebae of the slime mould Dictyostelium discoideum. Cell viability decreased markedly upon incubation with the diphosphonates. The mecha...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(92)90342-g

    authors： Pelorgeas S,Martin JB,Satre M

    更新日期：1992-12-01 00:00:00

  • Changes in hepatic and intestinal cholesterol regulatory enzymes. The influence of metformin.

    abstract：:The effect of metformin (N,N-dimethylbiguanide) on the rate-limiting enzymes of cholesterol metabolism was observed. 3-Hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA reductase) and acyl-CoA-cholesterol acyltransferase (ACAT) activities were estimated in hepatic microsomal and intestinal cell preparations from normal ...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(83)90583-x

    authors： Scott LM,Tomkin GH

    更新日期：1983-03-01 00:00:00

  • Inhibition of cytochrome P-450p (P450IIIA1) gene expression during liver regeneration from two-thirds hepatectomy in the rat.

    abstract：:Regenerating liver from partial hepatectomy (HPX) is known to exhibit a strong and transient deficiency in both spectrally detectable microsomal cytochrome P-450 (P-450) and related monooxygenase activities. Male Wistar rats (250-300 g) were HPX or sham operated and liver was excised at different times after operation...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(88)90705-8

    authors： Marie IJ,Dalet C,Blanchard JM,Astre C,Szawlowski A,Saint Aubert B,Joyeux H,Maurel P

    更新日期：1988-09-15 00:00:00

  • Kinetics of sulphate conjugation in extracts of human foetal liver cells in culture.

    abstract：:Sulphate conjugation was investigated using extracts of human foetal liver cells in culture. The three reactions which are involved in sulphate conjugation were measured singly or in combination: they are (i) the PAPS generation catalyzed by ATP-sulphurylase and adenosine 5'-phosphosulphate (APS)-kinase, (ii) the phen...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(88)90331-0

    authors： Tan TM,Sit KH,Wong KP

    更新日期：1988-12-15 00:00:00

  • Electron paramagnetic resonance spectrometry evidence for bioreduction of tirapazamine to oxidising free radicals under anaerobic conditions.

    abstract：:Tirapazamine (SR 4233) is a bioreductive antitumour drug in Phase III clinical trial which is activated in hypoxic tumour regions to generate a cytotoxic species. Electron paramagnetic resonance (EPR) spectrometry was used to investigate directly the formation of free radicals as the result of tirapazamine reduction b...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(00)00487-1

    authors： Patterson LH,Taiwo FA

    更新日期：2000-12-15 00:00:00

  • Protein S-glutathionylation and platelet anti-aggregating activity of disulfiram.

    abstract：:Blood platelets are central to haemostasis, and reactions in platelets involving sulfhydryl groups play important roles in platelet function. Reduced glutathione (GSH) plays an important role in platelet aggregation and glutathione-depleting chemicals inhibit platelet aggregation. The lipophilic drug disulfiram, becau...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2006.05.021

    authors： Rossi R,Giustarini D,Dalle-Donne I,Milzani A

    更新日期：2006-08-28 00:00:00

  • Protection by schisanhenol against adriamycin toxicity in rat heart mitochondria.

    abstract：:The effects of schisanhenol (Sal) on Adriamycin (ADM)-induced rat heart mitochondrial toxicity in vitro were investigated. Malondialdehyde formation, lysis, disintegration and membrane rigidification in mitochondria treated with ADM were reduced significantly by Sal. In the electron spin resonance studies, Sal did not...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(91)90519-b

    authors： Lin TJ,Liu GT,Pan Y,Liu Y,Xu GZ

    更新日期：1991-10-09 00:00:00

  • EMMPRIN-mediated induction of uterine and vascular matrix metalloproteinases during pregnancy and in response to estrogen and progesterone.

    abstract：:Pregnancy is associated with uteroplacental and vascular remodeling in order to adapt for the growing fetus and the hemodynamic changes in the maternal circulation. We have previously shown upregulation of uterine matrix metalloproteinases (MMPs) during pregnancy. Whether pregnancy-associated changes in MMPs are local...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/j.bcp.2013.06.030

    authors： Dang Y,Li W,Tran V,Khalil RA

    更新日期：2013-09-15 00:00:00

  • Inhibition of the release of prostaglandins, leukotrienes and lysosomal acid hydrolases from macrophages by selective inhibitors of lecithin biosynthesis.

    abstract：:The release of the inflammatory mediators, prostaglandins (PGs), leukotrienes (LT) and lysosomal acid hydrolases (LAH), by macrophages is stimulated by endocytic stimuli such as zymosan. This process can be interfered with by specific inhibitors of phosphatidylcholine (PC) biosynthesis. The diphenylsulfone dapsone and...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/0006-2952(83)90568-3

    authors： Bonney RJ,Wightman PD,Dahlgren ME,Sadowski SJ,Davies P,Jensen N,Lanza T,Humes JL

    更新日期：1983-01-15 00:00:00

  • Cross-resistance to antifolates in multidrug resistant cell lines with P-glycoprotein or multidrug resistance protein expression.

    abstract：:Resistance to some (lipophilic) antifolates has been associated with P-glycoprotein (P-gp)-mediated multidrug resistance (MDR). A possible relationship with non-P-gp MDR has not been established. We studied resistance to antifolates in SW-1573 human lung carcinoma cells, a P-gp overexpressing variant SW-1573/2R160 and...

    journal_title：Biochemical pharmacology

    pub_type： 杂志文章

    doi：10.1016/s0006-2952(97)82448-3

    authors： van Triest B,Pinedo HM,Telleman F,van der Wilt CL,Jansen G,Peters GJ

    更新日期：1997-06-15 00:00:00