Trifluoromethanesulfonamide anthelmintics. Protonophoric uncouplers of oxidative phosphorylation.

abstract：:The role of the intracellular messengers inositol 1,4,5-triphosphate (IP3) and protein kinase C (PKC) in the thrombin (3 U/mL)-induced contraction of endothelium-denuded porcine pulmonary arteries was investigated. Thrombin induced a sustained contractile response with an initial transient increase in IP3 to about 160...

journal_title：Biochemical pharmacology

authors： Bretschneider E,Paintz M,Glusa E

更新日期：1995-01-06 00:00:00

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

authors： Nirthanan S

更新日期：2020-11-01 00:00:00

abstract：:Celastrol, a quinone methide triterpenoid, was isolated as an inhibitor of NF-kappaB from Celastrus orbiculatus. This compound dose-dependently inhibited a variety of stimuli-induced NF-kappa B-regulated gene expression and the DNA-binding of NF-kappa B in different cell lines without affecting DNA-binding activity of...

journal_title：Biochemical pharmacology

authors： Lee JH,Koo TH,Yoon H,Jung HS,Jin HZ,Lee K,Hong YS,Lee JJ

更新日期：2006-11-15 00:00:00

abstract：:The inhibition of rat liver monoamine oxidase by a number of N-propargyl and alpha-methyl amine derivatives has been examined. The results indicate that alpha-methyl-substituted primary and secondary amine derivatives tend to show selectivity as reversible inhibitors towards the A-form of the enzyme. The structural fe...

journal_title：Biochemical pharmacology

authors： Tipton KF,McCrodden JM,Kalir AS,Youdim MB

更新日期：1982-04-01 00:00:00

abstract：:Two resistant K562 sublines have been developed by treatment with AZQ (2,5-bis(carboethoxyamino)-3,6-diaziridinyl-1,4-benzoquinone) and BZQ (2,5-bis(2-hydroxyethylamino)-3,6-diaziridinyl-1,4-benzoquinone). The ID50 values of for AZQ on K562, the AZQ-resistant sublines (AZQR) and the BZQ-resistant sublines (BZQR) were ...

journal_title：Biochemical pharmacology

authors： Ward TH,Haran MS,Whittaker D,Watson AJ,Howard TD,Butler J

更新日期：1995-08-08 00:00:00

abstract：:The role of calcium in the stimulation of phosphoinositide (PIn) hydrolysis by norepinephrine and the calcium ionophore A23187 was investigated in chopped cerebral cortex in which the PIns had been labeled previously with ([3H]myo-inositol. The accumulation of the newly formed [3H]inositol phosphate ([3H]IPs) was used...

journal_title：Biochemical pharmacology

authors： Knepper SM,Rutledge CO

更新日期：1987-09-15 00:00:00

abstract：:Characteristics of methotrexate (MTX) inhibition of dihydrofolic acid reductase (DHFR) enzyme activity and the effects of NADPH and NADH on enzyme-drug interaction were studied. Two highly sensitive assay procedures were used. The first utilized tritium-labeled MTX to measure direct binding properties of the enzyme an...

journal_title：Biochemical pharmacology

authors： Kamen BA,Whyte-Bauer W,Bertino JR

更新日期：1983-06-15 00:00:00

abstract：:Two radiolabelled derivatives of deferrioxamine B (DF) have been synthesized: methyl-DF and acetyl-DF. Both derivatives are non cytotoxic and stable in cell culture but they are degraded in human plasma and more extensively in rat plasma. Methyl-DF, acetyl-DF and DF mobilize radioiron to the same extent from hepatocyt...

journal_title：Biochemical pharmacology

authors： Laub R,Schneider YJ,Octave JN,Trouet A,Crichton RR

更新日期：1985-04-15 00:00:00

abstract：:Aldehydes generated during radical-induced lipid peroxidation, in particular 4-hydroxynonenal, are known to inhibit growth of certain cells. To extend our arguments that free radicals might be involved in the host response against malaria parasites we tested 26 carbonyls (n-alkanals, C6-C11; 2-alkenals, C3-C9; 2,4-alk...

journal_title：Biochemical pharmacology

authors： Clark IA,Butcher GA,Buffinton GD,Hunt NH,Cowden WB

更新日期：1987-02-15 00:00:00

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

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

abstract：:Metabolic activation of a potent mutagen, 6-aminochrysene, to genotoxic products in a newly developed tester strain, Salmonella typhimurium NM2009, was studied in a rat liver microsomal monooxygenase system containing cytochrome P450 (P450). Since the tester strain was constructed by introducing an O-acetyltransferase...

journal_title：Biochemical pharmacology

authors： Yamazaki H,Shimada T

更新日期：1992-09-01 00:00:00

abstract：:It has been hypothesized that oxidative modification of low density lipoprotein plays a key role in the pathogenesis of atherosclerosis. In order to elucidate the role of lipid oxidation and its inhibition in vivo, apolipoprotein E and alpha-tocopherol (alphaT) transfer protein double knockout (ApoE(-/-)alpha-TTP(-/-)...

journal_title：Biochemical pharmacology

authors： Yoshida Y,Hayakawa M,Itoh N,Habuchi Y,Inoue R,Chen ZH,Cao J,Cynshi O,Jishage K,Niki E

更新日期：2007-10-01 00:00:00

abstract：:Inhibitory effects of Delta(9)-tetrahydrocannabinol (Delta(9)-THC), cannabidiol (CBD), and cannabinol (CBN), the three major constituents in marijuana, on catalytic activities of human cytochrome P450 (CYP) 1 enzymes were investigated. These cannabinoids inhibited 7-ethoxyresorufin O-deethylase activity of recombinant...

journal_title：Biochemical pharmacology

authors： Yamaori S,Kushihara M,Yamamoto I,Watanabe K

更新日期：2010-06-01 00:00:00

abstract：:We previously demonstrated that the widely used immunosuppressive drugs cyclosporin A (CsA) and tacrolimus (FK506), independent of immunophilin binding, can activate profibrogenic transforming growth factor β (TGFβ)/Smad signaling cascades in rat renal mesangial cells (MC). Here we report that both peptidyl-prolyl cis...

journal_title：Biochemical pharmacology

authors： Akool el-S,Gauer S,Osman B,Doller A,Schulz S,Geiger H,Pfeilschifter J,Eberhardt W

更新日期：2012-01-15 00:00:00

abstract：BACKGROUND:Rho-Associated kinases ROCK1 and ROCK2 have been extensively investigated in the pathogenesis of cardiovascular disease. However, their roles are not fully understood in carcinogenesis. In this study, we investigated whether ROCK1 or ROCK2 is required for the survival and growth of hepatocellular carcinoma (...

journal_title：Biochemical pharmacology

authors： Wu H,Chen Y,Li B,Li C,Guo J,You J,Hu X,Kuang D,Qi S,Liu P,Li L,Xu C

更新日期：2020-12-02 00:00:00

abstract：:The PI3K/AKT/mTOR signaling pathway regulates cell proliferation, survival and angiogenesis. The mammalian target of rapamycin (mTOR) is a protein kinase ubiquitously expressed within cells that regulates cell growth and survival by integrating nutrient and hormonal signals. mTOR exists in two complexes, mTORC1 and mT...

journal_title：Biochemical pharmacology

authors： Espona-Fiedler M,Soto-Cerrato V,Hosseini A,Lizcano JM,Guallar V,Quesada R,Gao T,Pérez-Tomás R

更新日期：2012-02-15 00:00:00

abstract：:The mechanism by which the substituted benzimidazole sulphoxide BY 1023/SK&F 96022 inhibited the (H+ + K+)-ATPase, the enzyme responsible for hydrogen ion secretion in the stomach, was studied in a variety of in vitro preparations. In gastric preparations that were capable of active hydrogen ion transport with consequ...

journal_title：Biochemical pharmacology

authors： Simon WA,Keeling DJ,Laing SM,Fallowfield C,Taylor AG

更新日期：1990-06-01 00:00:00

abstract：:A new analogue of methotrexate was synthesized from 4-amino-4-deoxy-N10-methylpteroic acid and D,L-homocysteic acid. The product (mAPA-HCysA) was bound tightly to L1210 mouse leukemia dihydrofolate reductase (IC50 = 1 nM), inhibited L1210 cell proliferation in culture (IC50 = 0.3 microM), and prolonged the survival of...

journal_title：Biochemical pharmacology

authors： Rosowsky A,Moran RG,Forsch R,Colman P,Uren J,Wick M

更新日期：1984-01-01 00:00:00

abstract：:Tumor necrosis factor (TNF) is a pleiotropic cytokine that mediates different cellular responses including cytotoxicity, cytostasis, proliferation, differentiation and expression of specific genes. Recent studies have demonstrated that chemotherapeutic drugs that inhibit the nuclear enzyme DNA topoisomerase II synergi...

journal_title：Biochemical pharmacology

authors： Valenti M,Cimoli G,Mariani GL,Conte PF,Parodi S,Russo P

更新日期：1993-10-05 00:00:00

abstract：:Steroidal and non-steroidal antioestrogens, steroidal compounds with (disubstituted) dialkyl amino side chain, cholesterol derivatives, histaminic and (anti)-progestational compounds were tested for their ability to compete with [3H]tamoxifen for the specific antioestrogen binding site (AEBS) in the post-mitochondrial...

journal_title：Biochemical pharmacology

authors： van den Koedijk CD,Vis van Heemst C,Elsendoorn GM,Thijssen JH,Blankenstein MA

更新日期：1992-06-23 00:00:00

abstract：:Dravet syndrome (DS) is a catastrophic epileptic encephalopathy characterised by childhood-onset polymorphic seizures, multiple neuropsychiatric comorbidities, and increased risk of sudden death. Heterozygous loss-of-function mutations in one allele of SCN1A, the gene encoding the voltage-gated sodium channel 1.1 (NaV...

journal_title：Biochemical pharmacology

authors： Chow CY,Chin YKY,Ma L,Undheim EAB,Herzig V,King GF

更新日期：2020-11-01 00:00:00

abstract：:Addition of halothane to the incubation medium is shown to lower respiratory control and transmembrane potential and to increase ATPase activity in isolated rat liver mitochondria. Evidence is presented that L-carnitine is able to substantially decrease the negative effects of halothane on the energy-linked processes ...

journal_title：Biochemical pharmacology

authors： Toninello A,Branca D,Scutari G,Siliprandi N,Vincenti E,Giron G

更新日期：1986-11-15 00:00:00

abstract：:Guanylate cyclase in high speed supernatant fractions obtained from rat thoracic aorta or human coronary arteries pretreated with nitroglycerin exhibited a marked desensitization to activation by nitroglycerin, nitroprusside, and nitric oxide. However, activation of soluble guanylate cyclase by arachidonic acid was un...

journal_title：Biochemical pharmacology

authors： Waldman SA,Rapoport RM,Ginsburg R,Murad F

更新日期：1986-10-15 00:00:00

abstract：:Azithromycin is considered an effective drug to treat the perinatal mycoplasma infection. However, there is a lack of studies on developmental toxicity of azithromycin. In this study, we observed the developmental toxicity of fetal liver induced by prenatal azithromycin exposure (PAE) in mice and explored the potentia...

journal_title：Biochemical pharmacology

authors： Liu K,Wang G,Li L,Chen G,Gong X,Zhang Q,Wang H

更新日期：2020-10-01 00:00:00

abstract：:DT-diaphorase has been implicated in the activation and mechanism of cytotoxicity of the investigational indoloquinone anticancer drug EO9. Here, we have used a highly purified DT-diaphorase isolated from rat Walker tumour cells to provide unambiguous evidence for the ability of this enzyme to catalyze reduction of EO...

journal_title：Biochemical pharmacology

authors： Bailey SM,Lewis AD,Knox RJ,Patterson LH,Fisher GR,Workman P

更新日期：1998-09-01 00:00:00

abstract：:Human red blood cells and male Sprague-Dawley rats were treated in vitro and in vivo, respectively, with phenylhydrazine in order to determine whether the release of volatile hydrocarbons can serve as a suitable index for phenylhydrazine-induced red blood cell peroxidation. Lipid peroxidation following phenylhydrazine...

journal_title：Biochemical pharmacology

authors： Clemens MR,Remmer H,Waller HD

更新日期：1984-06-01 00:00:00

abstract：:The pregnane X-receptor (PXR) is a promiscuous nuclear receptor primarily responsible for the induction of genes from the cytochrome P450 3A family. In this study, we used a previously described PXR/SRC tethered protein to establish two in vitro assays for identifying PXR ligands: automated ligand identification syste...

journal_title：Biochemical pharmacology

authors： Xiao L,Nickbarg E,Wang W,Thomas A,Ziebell M,Prosise WW,Lesburg CA,Taremi SS,Gerlach VL,Le HV,Cheng KC

更新日期：2011-03-01 00:00:00

abstract：:Sulfasalazine (SF) promotes remyelination and improves the outcome of multiple sclerosis (MS) patients. However, the underlining mechanism remains elusive. Here, we examined whether SF blocks microglia switching to a pro-inflammatory M1-like phenotype through a competing endogenous RNA (ceRNA) effects in cuprizone-ind...

journal_title：Biochemical pharmacology

authors： Duan C,Liu Y,Li Y,Chen H,Liu X,Chen X,Yue J,Zhou X,Yang J

更新日期：2018-09-01 00:00:00

abstract：:The molecular mechanism(s) underlying induction of the hepatic microsomal cytochrome P4502E1 (2E1) by xenobiotics (e.g. ethanol and acetone) is controversial. Proposed mechanisms include increased rates of enzyme synthesis due to elevated 2E1 mRNA levels, enhanced translation of pre-existing mRNA, or stabilization of ...

journal_title：Biochemical pharmacology

authors： Kraner JC,Lasker JM,Corcoran GB,Ray SD,Raucy JL

更新日期：1993-04-06 00:00:00

abstract：:A series of protein modifying reagents were tested for their effects on the specific binding of [3H]MK801 to adult rat brain membranes. N-Bromosuccinimide, acetyl imidazole, 2,3-butanedione, 5,5'-dithiobis-(2-nitrobenzoic acid) and dithiothreitol all had no significant effect on binding. The carboxylic acid residue mo...

journal_title：Biochemical pharmacology

authors： Chazot PL,Fotherby A,Stephenson FA

更新日期：1993-02-09 00:00:00