Binding of colchiceine to tubulin. Mechanisms of ligand association with tubulin.

abstract：:HO-1 (heme oxygenase-1), an antioxidant enzyme, induced by rosiglitazone (PPAR ligands) can be a potential treatment of inflammation. However, the mechanisms of rosiglitazone-induced HO-1 expression in human pulmonary alveolar epithelial cells (HPAEpiCs) remain largely unknown. In this study, we found that upregulatio...

journal_title：Biochemical pharmacology

authors： Cho RL,Lin WN,Wang CY,Yang CC,Hsiao LD,Lin CC,Yang CM

更新日期：2018-02-01 00:00:00

abstract：:Chiral derivatives of several substituted halopyridyl and thiazolyl PETT compounds were synthesized as non-nucleoside inhibitors of the reverse transcriptase (RT) enzyme of the human immunodeficiency virus (HIV-1). Molecular modeling studies indicated that because of the asymmetric geometry of the non-nucleoside inhib...

journal_title：Biochemical pharmacology

authors： Venkatachalam TK,Mao C,Uckun FM

更新日期：2004-05-15 00:00:00

abstract：:Since ginsenoside-Rg(3), one of the panaxadiol saponins isolated from the ginseng root, significantly inhibited the secretion of catecholamines from bovine adrenal chromaffin cells stimulated by acetylcholine (ACh), the properties of ginsenoside-Rg(3) inhibition were investigated. Although ginsenoside-Rg(3) inhibited ...

journal_title：Biochemical pharmacology

authors： Tachikawa E,Kudo K,Nunokawa M,Kashimoto T,Takahashi E,Kitagawa S

更新日期：2001-10-01 00:00:00

abstract：:In the rat, the highly potent anti-herpes drug (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVdUrd) is rapidly converted to its base (E)-5-(2-bromovinyl)uracil (BVUra) through the action of pyrimidine nucleoside phosphorylases. However, BVdUrd can be regenerated or even generated de novo from BVUra by a pentosyl transfer rea...

journal_title：Biochemical pharmacology

authors： Desgranges C,De Clercq E,Razaka G,Drouillet F,Belloc I,Bricaud H

更新日期：1986-05-15 00:00:00

abstract：:Members of the homologous series of nine antitumour dimethanesulphonic acid esters, with the exception of ethylene dimethanesulphonate (EDMS), were found to cause DNA-DNA interstrand crosslinking in cells derived from the transplantable rodent Yoshida lymphosarcoma. The ability of the series to induce interstrand cros...

journal_title：Biochemical pharmacology

authors： Bedford P,Fox BW

更新日期：1983-08-01 00:00:00

abstract：:Daunorubicin (DNR) is a well known anticancer drug believed to act mainly by topoisomerase II inhibition and mitochondria-mediated free radical generation. Though several studies were dedicated to elucidate the mechanism of action of DNR, however the mechanism still remains illusive. DNR is reported to affect mitochon...

journal_title：Biochemical pharmacology

authors： Paul MK,Patkari M,Mukhopadhayay AK

更新日期：2007-09-15 00:00:00

abstract：:Metabolic and cardiovascular disease patients have increased plasma levels of lipids and, specifically, of palmitate, which can be toxic for several tissues. Trimetazidine (TMZ), a partial inhibitor of lipid oxidation, has been proposed as a metabolic modulator for several cardiovascular pathologies. However, its mech...

journal_title：Biochemical pharmacology

authors： Kuzmicic J,Parra V,Verdejo HE,López-Crisosto C,Chiong M,García L,Jensen MD,Bernlohr DA,Castro PF,Lavandero S

更新日期：2014-10-01 00:00:00

abstract：:Dinucleotides of adenosine and thymidine in the ApnT series (n = 3,4,5 and 6) and their corresponding phosphonate analogues, where a methylene group replaces the oxygen between the alpha and beta phosphorus atoms adjacent to thymidine, have been evaluated as inhibitors of human leukaemic thymidylate kinase (dTMP kinas...

journal_title：Biochemical pharmacology

authors： Orr RM,Davies LC,Stock JA,Taylor GA,Powles RL,Harrap KR

更新日期：1988-02-15 00:00:00

abstract：BACKGROUND:Salvinorin A (SA) is a potent anti-inflammatory diterpene isolated from the Mexican plant S. divinorum. Recently we showed that the novel SA analog, PR-38 has an inhibitory effect on mouse gastrointestinal (GI) motility mediated by opioid and cannabinoid (CB) receptors. The aim of the study was to characteri...

journal_title：Biochemical pharmacology

authors： Sałaga M,Polepally PR,Zakrzewski PK,Cygankiewicz A,Sobczak M,Kordek R,Zjawiony JK,Krajewska WM,Fichna J

更新日期：2014-12-15 00:00:00

abstract：:There is evidence to suggest that the oxidative metabolism of hydralazine (HP), an antihypertensive drug, may represent a toxic pathway which could account for some of the adverse effects of the drug. Experiments were done to determine whether the hepatic oxidative metabolism of HP is associated with the formation of ...

journal_title：Biochemical pharmacology

authors： LaCagnin LB,Colby HD,Dalal NS,O'Donnell JP

更新日期：1987-08-15 00:00:00

abstract：:The intraperitoneal injection of methylglyoxal bis(cyclohexylamidinohydrazone) (MGBC), an inhibitor of S-adenosylmethionine decarboxylase and spermidine synthase, markedly increased (7-fold of the basal level at 4 hr) ornithine decarboxylase (ODC) activity in normal mouse liver. ODC activity was also increased 2.5-fol...

journal_title：Biochemical pharmacology

authors： Hibasami H,Maekawa S,Murata T,Nakashima K

更新日期：1988-11-01 00:00:00

abstract：:Most studies have reported an up-regulation of retinoic acid receptor (RAR) mRNA expression by all-trans retinoic acid (RA). We aimed to study the effect of RA on RAR protein levels in MCF-7 human breast cancer cells. Incubation of these cells with 10(-6) M RA induced a rapid breakdown of both RARalpha and RARgamma in...

journal_title：Biochemical pharmacology

authors： Tanaka T,Rodríguez de la Concepción ML,De Luca LM

更新日期：2001-06-01 00:00:00

abstract：:DNA methylation is a mammalian epigenetic mark that participates to define where and when genes are expressed, both in normal cells and in the context of diseases. Like other epigenetic marks, it is reversible and can be modulated by chemical agents. Because it plays an important role in cancer by silencing certain ge...

journal_title：Biochemical pharmacology

authors： Pechalrieu D,Etievant C,Arimondo PB

更新日期：2017-04-01 00:00:00

abstract：:The kidney plays an important role in the homeostasis of carnitine by its ability to reabsorb carnitine almost completely from the glomerular filtrate. The transport process responsible for this reabsorption has been investigated thus far only in laboratory animals. Here we report on the characteristics of carnitine u...

journal_title：Biochemical pharmacology

authors： Huang W,Shaikh SN,Ganapathy ME,Hopfer U,Leibach FH,Carter AL,Ganapathy V

更新日期：1999-10-15 00:00:00

abstract：:Microsomal epoxide hydrolase (mEH) catalyzes the hydrolysis of epoxide intermediates derived from drugs and environmental chemicals. The response of in vivo (embryo) and in vitro (embryo fibroblast) tests were analyzed using mEH-null and wild-type mice to determine the relative role of maternal and embryonic mEH in th...

journal_title：Biochemical pharmacology

authors： Miyata M,Motoki K,Tamura E,Furukawa M,Gonzalez FJ,Yamazoe Y

更新日期：2002-03-15 00:00:00

abstract：:Polychlorinated biphenyls (PCBs) induce drug metabolism that may lead to the bioactivation of PCBs themselves or alternatively may lead to oxidative events within the cell. The goal of the present study was to determine the influence of congeneric PCBs, selected as substrates for or inducers of drug metabolism, upon h...

journal_title：Biochemical pharmacology

authors： Twaroski TP,O'Brien ML,Robertson LW

更新日期：2001-08-01 00:00:00

abstract：:Reduction of exogenous lipoic acid to dihydrolipoate is known to occur in several mammalian cells and tissues. Dihydrolipoate is a potent radical scavenger, and may provide significant antioxidant protection. Because lipoic acid appears in the bloodstream after oral administration, we have examined the reduction of ex...

journal_title：Biochemical pharmacology

authors： Constantinescu A,Pick U,Handelman GJ,Haramaki N,Han D,Podda M,Tritschler HJ,Packer L

更新日期：1995-07-17 00:00:00

abstract：:The anti-anginal agent bepridil blocks slow Ca2+ channels in a variety of tissues. Since bepridil accumulates inside cells, the possibility exists that bepridil acts, at least partially, from inside the cell. To test this possibility, we examined the effects of a quaternary ammonium analog of bepridil, methylated bepr...

journal_title：Biochemical pharmacology

authors： Wahler GM,Doane JD,Ousterhout JM,Sperelakis N,Lamar JC,Busch N,Biswas JC,Rogers TB

更新日期：1986-07-15 00:00:00

abstract：:Acetaminophen (AP) is a widely-used analgesic agent that has been linked to human liver and kidney disease with prolonged or high-dose usage. In rodents, the target organs that are affected include liver, kidney, and the olfactory mucosa. AP toxicity requires cytochrome P450(CYP)-mediated metabolic activation, and the...

journal_title：Biochemical pharmacology

authors： Genter MB,Liang HC,Gu J,Ding X,Negishi M,McKinnon RA,Nebert DW

更新日期：1998-06-01 00:00:00

abstract：AIMS:Protein Kinase R (PKR) plays a key role in inflammation and insulin resistance. Cytokines, high fat diet, infection and various stress signals can activate PKR. However, the functional significance of PKR in diabetic cardiomyopathy (DCM) is not explored so far. Thus the aim of the present study was to investigate ...

journal_title：Biochemical pharmacology

authors： Mangali S,Bhat A,Jadhav K,Kalra J,Sriram D,Vamsi Krishna Venuganti V,Dhar A

更新日期：2020-07-01 00:00:00

abstract：:The ability of adrenergic catechol derivatives, including dobutamine, dopamine, and isoproterenol, to inhibit lipid peroxidation was examined. All the catechol derivatives we tested strongly inhibited lipid peroxidation. Dobutamine was a more powerful inhibitor of iron-catalyzed lipid peroxidation than the other agent...

journal_title：Biochemical pharmacology

authors： Miura T,Muraoka S,Ogiso T

更新日期：1998-06-15 00:00:00

abstract：:The present investigation addressed the role of verapamil for oral pharmacokinetics of morphine-6-beta-glucuronide (M6G). Male Sprague-Dawley rats received 62.5 mg kg(-1) M6G-dihydrate orally w/wo pre-treatment with 70 mg kg(-1) verapamil. Intravenous M6G (3.9 mg kg(-1) ) and oral morphine (52.7 mg kg(-1) morphine-hyd...

journal_title：Biochemical pharmacology

authors： Lötsch J,Sperker B,Kroemer HK,Geisslinger G

更新日期：2002-04-15 00:00:00

abstract：:We investigated the amplification of bleomycin-induced DNA cleavage by synthetic triamides containing N-methylpyrrole (Py) and/or N-methylimidazole (Im), PyPyPy, PyPyIm, PyImPy, and PyImIm, using 32P-labeled DNA fragments obtained from the human c-Ha-ras-1 and p53 genes. Peplomycin, a bleomycin analog, plus Fe(II) cau...

journal_title：Biochemical pharmacology

authors： Hiraku Y,Oikawa S,Kuroki K,Sugiyama H,Saito I,Kawanishi S

更新日期：2001-02-01 00:00:00

abstract：:Angiogenesis, the development of neovessels from pre-existing vessels, is obligatory for solid tumors survival, growth, invasion, and metastasis. Many anti-angiogenic agents are small molecules originated from natural sources. Recently, angiosuppressive effects of indirubin and its derivatives, the active components i...

journal_title：Biochemical pharmacology

authors： Chan YK,Kwok HH,Chan LS,Leung KS,Shi J,Mak NK,Wong RN,Yue PY

更新日期：2012-03-01 00:00:00

abstract：:a synthetic seleno-organic compound, 2-phenyl-1,2-benzoisoselenazol-3(2H)-one (PZ 51), exhibits GSH peroxidase-like activity in vitro, in contrast to its sulfur analog, PZ 25. In addition, PZ 51 behaves as an antioxidant shown by a temporary protection of rat liver microsomes against ascorbate/ADP-Fe-induced lipid per...

journal_title：Biochemical pharmacology

authors： Müller A,Cadenas E,Graf P,Sies H

更新日期：1984-10-15 00:00:00

abstract：:B-Raf kinase is the key point in a main branch of mitogen-activated protein kinase pathways and some of its mutations, such as the V600E mutation, lead to the persistent activation of ERK signaling and the trigger of severe diseases, including melanoma and other somatic cancers. Several potent drugs have been approved...

journal_title：Biochemical pharmacology

authors： Wang PF,Qiu HY,Wang ZF,Zhang YJ,Wang ZC,Li DD,Zhu HL

更新日期：2017-05-15 00:00:00

abstract：:The partition coefficients (Kp) of three prototype Ca2+ antagonists, nitrendipine, (-)-desmethoxyverapamil and flunarizine were determined in native synaptic plasma membranes (SPM) isolated from sheep brain cortex and in liposomes prepared with the total lipids extracted from the membranes. We found that at 25 degrees...

journal_title：Biochemical pharmacology

authors： Carvalho CM,Oliveira CR,Lima MP,Leysen JE,Carvalho AP

更新日期：1989-07-01 00:00:00

abstract：:A serine peptidase (RLK1) was partially purified from rat liver homogenates. Its molecular weight was 80,000, and its optimum pH was 7.5. Bz-Tyr-O-Et was hydrolyzed by the enzyme, which was inhibited by Ip2PF, PMSF and by Tos-Phe-CH2Cl. The bonds cleaved by the enzyme were Phe5-Ser6 and Phe8-Arg9, when bradykinin was ...

journal_title：Biochemical pharmacology

authors： Da Graça M,Mazzacoratti N,Sampaio CA

更新日期：1982-03-01 00:00:00

abstract：:Understanding the receptor activation mechanism is essential for the rational design of pharmacologically active ligand molecules. However, the activation mechanism of most cytokine receptors remains still unclear, and while agonism and antagonism have been described for ligand-mimetic peptides, there has been no repo...

journal_title：Biochemical pharmacology

authors： Kawahara M,Ishii S,Tsumoto K,Kumagai I,Ueda H,Nagamune T

更新日期：2004-08-01 00:00:00

abstract：:Elevated glucose levels in diabetes mellitus is associated with increased oxidized low density lipoprotein (oxLDL). High glucose (HG) and oxLDL are key inducers of oxidative stress and inflammatory processes responsible for diabetic vascular disorders. Rosmarinic acid is a polyphenol with antioxidant, anti-inflammator...

journal_title：Biochemical pharmacology

authors： Nyandwi JB,Ko YS,Jin H,Yun SP,Park SW,Kim HJ

更新日期：2020-12-01 00:00:00