3-(13-Hydroxytridecyl)-1-[13-(3-pyridyl)tridecyl]pyridinium chloride (YM-53792), a novel inhibitor of NF-AT activation.

abstract：:The chiral inversion properties of 4-(4-methylphenyl)-2-methylthiomethyl-4-oxobutanoic acid (KE-748), an active metabolite of 2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (KE-298), were compared with those of ibuprofen in rats. After administration of R(-)-[2 alpha-2H]KE-748, S(+)-KE-748 was present in the...

journal_title：Biochemical pharmacology

authors： Yoshida H,Kohno Y,Endo H,Yamaguchi J,Fukushima K,Suwa T,Hayashi M

更新日期：1997-01-24 00:00:00

abstract：:Phomopsin A is an antimitotic cyclic peptide containing a 13-member ring including an ether linkage. It was isolated from the fungus Phomopsis leptostromiformis as the causal agent of lupinosis. Phomopsin A strongly inhibited microtubule assembly (IC50: 2.4 microM). Our study using radiolabeled phomopsin A, prepared b...

journal_title：Biochemical pharmacology

authors： Li Y,Kobayashi H,Tokiwa Y,Hashimoto Y,Iwasaki S

更新日期：1992-01-22 00:00:00

abstract：:The response and engagement of host normal tissues in malignant disease are major factors in therapeutic resistance. Physically, solid tumors have regions of hypoxia and acidosis. These physical stresses can lead to a more aggressive malignant phenotype through activation of HIF, GLUT-1, carbonic anhydrase IX, and sub...

journal_title：Biochemical pharmacology

authors： Teicher BA

更新日期：2009-06-01 00:00:00

abstract：:Raf kinase inhibitor protein (RKIP) is a member of the phosphatidylethanolamine-binding protein (PEBP) family. RKIP plays a pivotal modulatory role in several protein kinase signaling cascades. RKIP binds inhibits Raf-1-mediated phosphorylation of MEK through binding to Raf-1. Protein kinase C (PKC) phosphorylates RKI...

journal_title：Biochemical pharmacology

authors： Keller ET,Fu Z,Brennan M

更新日期：2004-09-15 00:00:00

abstract：:Hepatic fibrosis is characterized by excess type I collagen deposition and exacerbated inflammatory response. Naltrexone, an opioid receptor antagonist used for treating alcohol abuse, attenuates hepatocellular injury in fibrotic animal models, which can be accompanied by deleterious side effects. Additionally, opioid...

journal_title：Biochemical pharmacology

authors： Day SA,Lakner AM,Moore CC,Yen MH,Clemens MG,Wu ES,Schrum LW

更新日期：2011-04-15 00:00:00

abstract：:Our previous study showed that nicardipine and its structural analog, methyl 2-(N-benzyl-N-methylamino)ethyl-2,6-dimethyl-4-(2-isopropyl-pyrazolo[1,5 -a]pyridine-3-yl)-1,4-dihydro-pyridine-3,5-dicarboxylate (AHC-52), which is devoid of calcium channel blocking activity, were equally effective in inhibiting natural kil...

journal_title：Biochemical pharmacology

authors： Yamashiro T,Watanabe N,Kobayashi Y

更新日期：1997-07-01 00:00:00

abstract：:C-1748 is a DNA-binding agent with potent antitumor activity, especially towards prostate and colon carcinoma xenografts in mice. Here, we elucidated the nature of cellular response of human colon carcinoma HCT8 and HT29 cells to C-1748 treatment, at biologically relevant concentrations (EC(90) and their multiplicity)...

journal_title：Biochemical pharmacology

authors： Augustin E,Moś-Rompa A,Nowak-Ziatyk D,Konopa J

更新日期：2010-05-01 00:00:00

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

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

更新日期：2007-09-15 00:00:00

abstract：:Several monoclonal antibodies against human liver glutathione S-transferase mu were developed. One of these monoclonal antibodies, called GST-3H4 was further characterized and used in this study. In hepatic tissue, after immunoblotting, GST-3H4 strains a 27 kDa protein with a pI value of 6.2. GST-3H4 recognizes other ...

journal_title：Biochemical pharmacology

authors： Peters WH,Kock L,Nagengast FM,Roelofs HM

更新日期：1990-02-01 00:00:00

abstract：:The effects of the enantiomers of 2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridyl]methyl]-sulfinyl ]- 1H-benzimidazole (lansoprazole, AG-1749) on acid formation in isolated canine parietal cells and (H+ + K+)-ATPase activity in canine gastric microsomes were investigated. Both the (+)-and the (-)-enantiomer of lanso...

journal_title：Biochemical pharmacology

authors： Nagaya H,Inatomi N,Nohara A,Satoh H

更新日期：1991-10-24 00:00:00

abstract：:The turnover rate of vitamin E is slow in nerve tissue. Therefore, we have developed in vitro techniques to study the biochemical reactions of this nutrient in brain. Subcellular fractions were isolated from the cerebral hemispheres of 4-month-old, male, Fisher 344 rats. Aliquots of fractions (500 micrograms protein) ...

journal_title：Biochemical pharmacology

authors： Vatassery GT

更新日期：1993-06-09 00:00:00

abstract：:A comparison of the effects of various phosphodiesterase (PDE) inhibitors upon cellular cAMP levels was undertaken in human neuroblastoma SH-SY5Y cells. When inhibitors such as rolipram and Ro 20 1724 (selective for the low Km cAMP-specific PDE) were used, cAMP levels were seen to rise dramatically under basal (< or =...

journal_title：Biochemical pharmacology

authors： Morgan AJ,Murray KJ,Challiss RA

更新日期：1993-06-22 00:00:00

abstract：:The present study was designed to evaluate the effects of novel and recognised compounds at human recombinant A(2B) adenosine receptors expressed in Chinese hamster ovary (hA(2B)CHO), in human embryonic kidney 293 (hA(2B)HEK-293) and at endogenous A(2B) receptors in human mast cells (HMC-1). Saturation binding experim...

journal_title：Biochemical pharmacology

authors： Varani K,Gessi S,Merighi S,Vincenzi F,Cattabriga E,Benini A,Klotz KN,Baraldi PG,Tabrizi MA,Lennan SM,Leung E,Borea PA

更新日期：2005-11-25 00:00:00

abstract：:The ability of benzazepine D-1 dopamine agonists with varying efficacies in stimulating adenylate cyclase and to induce contralateral circling was investigated in rats with unilateral 6-hydroxydopamine lesions of the medial forebrain bundle. In the 6-hydroxydopamine lesioned rats, the benzazepines SKF 38393 (7,8-dihyd...

journal_title：Biochemical pharmacology

authors： Gnanalingham KK,Hunter AJ,Jenner P,Marsden CD

更新日期：1995-05-11 00:00:00

abstract：:N-Nitrosoguanidines are potential carcinogens. However, the toxicity of these agents is attenuated significantly in laboratory rodents by processes that remove the nitroso group to generate the relatively innocuous parent guanidinium compound. The denitrosation of 1,3-dimethyl-2-cyano-1-nitrosoguanidine (CyanoDMNG) me...

journal_title：Biochemical pharmacology

authors： Jensen DE,Belka GK,Dworkin C

更新日期：1997-05-09 00:00:00

abstract：:Enhanced aggregation of platelets was observed in platelet-rich plasma, but not in washed platelet suspension (WPS), during acute inflammation in rats. Incubation of WPS with inflammatory plasma increased the aggregatory response to ADP, but the plasma itself did not cause aggregation of platelets. It potentiated the ...

journal_title：Biochemical pharmacology

authors： Srivastava R,Srimal RC

更新日期：1990-07-15 00:00:00

abstract：:The widely used muscarinic receptor ligand [3H]quinuclidinyl benzilate ([3H]QNB) was found to bind in a site-specific but artifactual manner to rat intestinal mucus, obscuring specific binding to muscarinic receptors on intestinal epithelial cells. Atropine inhibited [3H]QNB binding to mucus with an apparent IC50 of 2...

journal_title：Biochemical pharmacology

authors： Rimele TJ,Gaginella TS

更新日期：1982-02-15 00:00:00

abstract：:The localization of [3H]forskolin binding to microscope slide mounted sections of rat kidney has been examined using autoradiography. Saturation studies showed [3H]forskolin binding to two sites, a high affinity site (KD = 8.7 nM, Bmax = 0.14 pmol/mg protein) and a low affinity site (KD = 6.7 microM, Bmax = 11.0 pmol/...

journal_title：Biochemical pharmacology

authors： McMartin LR,Summers RJ

更新日期：1990-03-15 00:00:00

abstract：:Pelargonidin is a natural red pigment found in fruits and vegetables, and has been reported to exhibit various effects potentially beneficial for human health. However, the possible preventive effects of pelargonidin toward atherosclerosis and mechanisms involved have not been investigated to date. Here, we compared t...

journal_title：Biochemical pharmacology

authors： Son JE,Jeong H,Kim H,Kim YA,Lee E,Lee HJ,Lee KW

更新日期：2014-05-15 00:00:00

abstract：:When rat peritoneal leucocytes were incubated with carbon tetrachloride, a PLA2 was activated, eicosanoids were generated and lysosomal and cytoplasmic enzymes were released. The predominant eicosanoid generated was TXB2 with lesser amounts of PGE2, 6-keto PGF1 alpha and LTB4. Preincubation of the cells with two struc...

journal_title：Biochemical pharmacology

authors： Lynch TJ,Blackwell GJ,Moncada S

更新日期：1985-05-01 00:00:00

abstract：:cis-platinum(II) (cis-diammine dichloroplatinum; cisplatin) is a potent antitumor compound that is widely used for the treatment of many malignancies. An important side-effect of cisplatin is nephrotoxicity, which results from injury to renal tubular epithelial cells and can be manifested as either acute renal failure...

journal_title：Biochemical pharmacology

authors： Lee RH,Song JM,Park MY,Kang SK,Kim YK,Jung JS

更新日期：2001-10-15 00:00:00

abstract：:Endothelins exert their physiological effects through interaction with cell surface receptors that are members of the G-protein-coupled receptor family. The endothelin receptor subtype B (ET(B) receptor) is abundantly expressed in rat cerebellum. Since agonist binding to G-protein-coupled receptors may be modulated by...

journal_title：Biochemical pharmacology

authors： Ceccarelli F,Giusti L,Bigini G,Costa B,Grillotti D,Fiumalbi E,Lucacchini A,Mazzoni MR

更新日期：2001-09-01 00:00:00

abstract：:We tested the ability of a wide variety of organic compounds, including benzene and phenol derivatives, aromatic amines, pyrazoline derivatives and other non-steroidal anti-inflammatory drugs, to act as cosubstrates during the horseradish peroxidase/hydrogen peroxide-mediated oxygenation of arachidonic acid. Structura...

journal_title：Biochemical pharmacology

authors： Lehmann FM,Bretz N,von Bruchhausen F,Wurm G

更新日期：1989-04-15 00:00:00

abstract：:The possible role of fluroacetate in the toxicity and antitumour activity of the fluroethylnitrosoureas, BFNU and FCNU has been studied in CBA mice bearing the TLX5 lymphoma either sensitive (TLXS) or resistant (TLXRT) to nitrosoureas. Treatment of mice bearing either TLXS or TLXRT tumours with either BFNU or FCNU cau...

journal_title：Biochemical pharmacology

authors： Tisdale MJ,Brennan RA

更新日期：1985-09-15 00:00:00

abstract：:Bcr-abl kinase inhibitors have provided proof of principal that targeted therapy holds great promise for the treatment of cancer. However, despite the success of these agents in treating chronic myelogenous leukemia (CML), the majority of patients continue to present with minimal residual disease contained within the ...

journal_title：Biochemical pharmacology

authors： Nair RR,Tolentino J,Hazlehurst LA

更新日期：2010-09-01 00:00:00

abstract：:In this review, I summarize the sequence of events involved in characterizing the functional role of GABA(B) receptors in the CNS and their involvement in synaptic transmission. The story was launched with the realization that baclofen was a selective agonist of GABA(B) receptors. This lead to the discovery in the CNS...

journal_title：Biochemical pharmacology

authors： Nicoll RA

更新日期：2004-10-15 00:00:00

abstract：:Cardiac steroids are used to treat various diseases including congestive heart failure and cancer. The aim of this study was to investigate the anti-leukemic activity of UNBS1450, a hemi-synthetic cardenolide belonging to the cardiac steroid glycoside family. Here, we report that, at low nanomolar concentrations, UNBS...

journal_title：Biochemical pharmacology

authors： Juncker T,Cerella C,Teiten MH,Morceau F,Schumacher M,Ghelfi J,Gaascht F,Schnekenburger M,Henry E,Dicato M,Diederich M

更新日期：2011-01-01 00:00:00

abstract：:Protein phosphatases are responsible for keeping the signaling output of stimulus-activated protein kinases in check; but protein phosphatases are also themselves targets and conveyors of biological signals. Among the major serine/threonine phosphatases, protein phosphatase 2A (PP2A) appears to play a privileged role ...

journal_title：Biochemical pharmacology

authors： Goldberg Y

更新日期：1999-02-15 00:00:00

abstract：:Human CYP2A6 is a cytochrome P450 (CYP) isoform responsible for the metabolism of nicotine, coumarin, tegafur, and valproic acid, and metabolic activation of nitrosamines. Genetic polymorphisms of the CYP2A6 gene are a major causal factor of the large interindividual differences in nicotine metabolism. In the present ...

journal_title：Biochemical pharmacology

authors： Fukami T,Nakajima M,Higashi E,Yamanaka H,McLeod HL,Yokoi T

更新日期：2005-09-01 00:00:00

abstract：:The bactericidal effect of metronidazole on Escherichia coli and Bacteroides fragilis can be partially reversed by cysteamine under conditions that lead to the formation of an adduct, the thioether, 4-(2-aminoethyl)thio-2-methylimidazole-1-ethanol (4-ATME). This adduct, which is not mutagenic for the Ames histidine au...

journal_title：Biochemical pharmacology

authors： Yeung TC,Goldman P

更新日期：1983-11-01 00:00:00