Novel mode of cytotoxicity obtained by coupling inactive anthracycline to a polymer.

abstract：:Extracellular ATP suppressed the growth of HL-60 leukemia cells and induced their differentiation as revealed by N-formyl-methionyl-leucyl-phenylalanine-induced beta-glucuronidase release. ATP degraded to ADP, AMP, and adenosine, and the effect of ATP on cell growth was mimicked by these metabolites added to the cultu...

journal_title：Biochemical pharmacology

authors： Conigrave AD,van der Weyden L,Holt L,Jiang L,Wilson P,Christopherson RI,Morris MB

更新日期：2000-12-01 00:00:00

abstract：:The glycolipid alpha-galactosylceramide (alpha-GalCer), when presented on CD1 molecules by antigen presenting cells (APCs) to invariant NKT (iNKT cells), is a potent immunomodulator. Indoleamine 2,3-dioxygenase (IDO), an enzyme catalyzing the catabolism of L-tryptophan along the kynurenine pathway, is inducible in APC...

journal_title：Biochemical pharmacology

authors： Fallarini S,Paoletti T,Panza L,Lombardi G

更新日期：2008-09-15 00:00:00

abstract：:AKT1 (c-AKT, PKBalpha) is the cellular homolog of the protein-serine/threonine kinase oncogene, v-akt. AKT1 is activated through the insulin and platelet-derived growth factor signaling pathways in transfected fibroblasts, but little is known about the regulation of endogenous AKT1 in tumor cells. AKT1 levels were hig...

journal_title：Biochemical pharmacology

authors： Ahmad S,Singh N,Glazer RI

更新日期：1999-08-01 00:00:00

abstract：:The microsomal fraction of bone marrow contains cytochrome P-450 (39 +/- 11 pmoles/mg microsomal protein) and monooxygenase activity could be demonstrated by the O-dealkylation of 7-ethoxycoumarin (114 +/- 65 pmoles/(min X mg microsomal protein] and the hydroxylation of benzene to phenol (51 +/- 8.6 pmol/45 min X mg m...

journal_title：Biochemical pharmacology

authors： Gollmer L,Graf H,Ullrich V

更新日期：1984-11-15 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：:Fundamental progresses have been made in pain research with a comprehensive understanding of the neuronal pathways which convey painful sensations from the periphery and viscera to the central nervous system and of the descending modulating pathways. Nevertheless, many patients still suffer from various painful condit...

journal_title：Biochemical pharmacology

authors： Ceruti S

更新日期：2020-12-28 00:00:00

abstract：:The acute effects of carbon tetrachloride (CCl4) on the membrane structure of rat liver microsomes were studied using 31P-NMR and spin-labeling techniques. 31P-NMR spectra of rat liver microsomes were not changed appreciably after the oral administration of CCl4, indicating that the surface structures of microsomal me...

journal_title：Biochemical pharmacology

authors： Utsumi H,Murayama J,Hamada A

更新日期：1985-01-01 00:00:00

abstract：:The cytoprotective effect of the natural dietary constituent indole-3-carbinol (I-3-C) on carbon tetrachloride (CCl4) mediated hepatotoxicity in mice was examined. I-3-C pretreatment by gavage 1 hr prior to intraperitoneal injection of CCl4 produced a 63% decrease in CCl4-mediated centrolobular necrosis and a related ...

journal_title：Biochemical pharmacology

authors： Shertzer HG,Berger ML,Tabor MW

更新日期：1988-01-15 00:00:00

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

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

abstract：:The discovery and development of medications to treat addiction and notably, cocaine addiction, have been frustrated by both the complexity of the disorder and the lack of target validation in human subjects. The dopamine transporter has historically been a primary target for cocaine abuse medication development, but ...

journal_title：Biochemical pharmacology

authors： Rothman RB,Baumann MH,Prisinzano TE,Newman AH

更新日期：2008-01-01 00:00:00

abstract：:Cisplatin is a potent chemotherapeutic drug widely used for the treatment of human cancer. However, its efficacy against hepatocellular carcinoma (HCC) is poor for reasons that remain unclear. We show here that prothymosin-alpha (PTMA) is overexpressed in HCC cell lines. Silencing PTMA using short-hairpin RNA sensitiz...

journal_title：Biochemical pharmacology

authors： Lin YT,Liu YC,Chao CC

更新日期：2016-12-15 00:00:00

abstract：:The effect of non-insulin-dependent diabetes on the hepatic microsomal cytochrome P450-dependent mixed-function oxidase system and on cytosolic glutathione S-transferase activity was determined using the spontaneously obese-diabetic (ob/ob) mouse model. The activities of the xenobiotic-metabolizing cytochrome P450 pro...

journal_title：Biochemical pharmacology

authors： Barnett CR,Abbott RA,Bailey CJ,Flatt PR,Ioannides C

更新日期：1992-04-15 00:00:00

abstract：:Western blotting and densitometric analysis of extracts obtained from EDTA extraction of skin segments showed greater extracellular Lipocortin 1 (LC1) in skin sites from steroid-treated animals compared to that seen in matched vehicle treated animals. Extracellular LC1 was maximal 3 hr after steroid, less was found in...

journal_title：Biochemical pharmacology

authors： Ahluwalia A,Mohamed RW,Flower RJ

更新日期：1994-10-18 00:00:00

abstract：:The effect of oxygen concentration and Ca2+ omission on CCl4-induced hepatotoxicity was studied in a non-recirculating and hemoglobin-free liver perfusion system using phenobarbital-pretreated rats. With 95% O2-saturated perfusate, infusion of 0.5 mM CCl4 caused an instantaneous increase of thiobarbituric acid reactiv...

journal_title：Biochemical pharmacology

authors： Masuda Y,Nakamura Y

更新日期：1990-10-15 00:00:00

abstract：:Treatment of normolipidemic rats by alkylthiopropionic acid (CETTD), resulted in a dose- and time-dependent increase in total dihydroxyacetone phosphate acyltransferase (DHAPAT) activity, in extent comparable to that of 3-thiadicarboxylic acid (BCMTD) and alkylthioacetic acid (CMTTD). Thus, in CETTD- and CMTTD-treated...

journal_title：Biochemical pharmacology

authors： Skorve J,Ruyter B,Rustan AC,Christiansen EN,Drevon CA,Berge RK

更新日期：1990-11-01 00:00:00

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

authors： Testa B

更新日期：2004-12-01 00:00:00

abstract：:The effects of the P2-purinoceptor antagonist, suramin, on ADP-induced increases in human platelet cytosolic calcium concentration ([Ca2+]i) and inhibition of prostaglandin E1 (PGE1)-stimulated adenylate cyclase activity were investigated. Suramin (50-200 microM) acted as an antagonist of ADP-induced increases in [Ca2...

journal_title：Biochemical pharmacology

authors： Hall DA,Hourani SM

更新日期：1994-03-15 00:00:00

abstract：:Epoxyeicosatrienoic acids (EETs), a family of cytochrome P450 epoxygenase metabolites of arachidonic acid, are believed to have an autocrine or paracrine role in the regulation of neurons or neuroendocrine cells. The effects of 14,15-EET on ionic currents were investigated in rat pituitary GH(3) cells. In the whole-ce...

journal_title：Biochemical pharmacology

authors： Wu SN,Li HF,Chiang HT

更新日期：2000-07-15 00:00:00

abstract：:The reactivities of sulfite (SO23-) with DNA in the presence of metal ions were investigated by a DNA sequencing technique using 32P-labeled DNA fragments obtained from human c-Ha-ras-1 protooncogene. Sulfite caused DNA damage in the presence of Co2+, Cu2+ and Mn2+, although sulfite alone or metal ion alone did not. T...

journal_title：Biochemical pharmacology

authors： Kawanishi S,Yamamoto K,Inoue S

更新日期：1989-10-15 00:00:00

abstract：:The salt-induced condensation of chromatin has been studied with flow-linear dichroism technique using an intercalative dye (methylene blue) to selectively monitor the linker orientation. At low ionic strength both linkers and chromatosomes (with their flat faces) are oriented preferentially parallel to the chromatin ...

journal_title：Biochemical pharmacology

authors： Kubista M,Nielsen PE,Nordén B

更新日期：1988-05-01 00:00:00

abstract：:Aminoglycoside antibiotics induce a lysosomal phospholipidosis in kidney proximal tubules after conventional therapy in animals and man. We have previously demonstrated that these drugs bind to negatively charged phospholipid bilayers at acid pH and inhibit the activity of lysosomal acid phospholipases in vitro and in...

journal_title：Biochemical pharmacology

authors： Brasseur R,Carlier MB,Laurent G,Claes PJ,Vanderhaeghe HJ,Tulkens PM,Ruysschaert JM

更新日期：1985-04-01 00:00:00

abstract：:The activity of tyrosine hydroxylase (TH) in the corpus striatum of haloperidol treated and control rats has been examined. The activation of TH by haloperidol caused a decrease in the Km for tetrahydrobiopterin but no change in the Vmax. This effect was totally abolished when homogenates were prepared at high values ...

journal_title：Biochemical pharmacology

authors： Mann SP,Hill MW

更新日期：1983-11-15 00:00:00

abstract：:A 1.57kb BamH1 fragment containing a full-length human debrisoquine 4-hydroxylase cytochrome P450 (CYP2D6) cDNA was inserted into the BglII site of the yeast expression plasmid pMA91 and the resulting recombinant plasmid, PELT1, introduced into Saccharomyces cerevisiae strain AH22. Microsomes prepared from AH22/pELT1 ...

journal_title：Biochemical pharmacology

authors： Ellis SW,Ching MS,Watson PF,Henderson CJ,Simula AP,Lennard MS,Tucker GT,Woods HF

更新日期：1992-08-18 00:00:00

abstract：:The nuclear retinoid X receptor-α (RXRα) plays critical roles in cell homeostasis and in many physiological processes mainly through its transcriptional function. However, an N-terminal truncated form of RXRα, tRXRα, was frequently described in various cancer cells and tumor tissues, thus representing a new promising ...

journal_title：Biochemical pharmacology

authors： Wang PY,Zeng WJ,Liu J,Wu YL,Ma Y,Zeng Z,Pang JY,Zhang XK,Yan X,Wong AST,Zeng JZ

更新日期：2017-01-15 00:00:00

abstract：:Andrographis paniculata has long been part of the traditional herbal medicine system in Asia and in Scandinavia. Andrographolide was isolated as a major bioactive constituent of A. paniculata in 1951, and since 1984, andrographolide and its analogs have been scrutinized with modern drug discovery approach for anti-inf...

journal_title：Biochemical pharmacology

authors： Tan WSD,Liao W,Zhou S,Wong WSF

更新日期：2017-09-01 00:00:00

abstract：:Sepsis is a complex clinical syndrome that results from a harmful host response to infection, in which foreign bacteria and lipopolysaccharide (LPS) are potent activators of different immune cells, including monocytes and macrophages. To date, there are currently few effective adjuvant therapies in clinical use except...

journal_title：Biochemical pharmacology

authors： Yibin G,Jiang Z,Hong Z,Gengfa L,Liangxi W,Guo W,Yongling L

更新日期：2005-07-15 00:00:00

abstract：:Nonsteroidal anti-inflammatory drugs (NSAIDs) are now understood to fall into one of two agent classes in clinical use. Traditional NSAIDs inhibit both cyclooxygenases-1 and 2 (COX-1, 2), which act as key enzymes catalyzing the same reaction in the production of prostaglandins (PGs), while the second class of NSAIDs s...

journal_title：Biochemical pharmacology

authors： Imanishi J,Morita Y,Yoshimi E,Kuroda K,Masunaga T,Yamagami K,Kuno M,Hamachi E,Aoki S,Takahashi F,Nakamura K,Miyata S,Ohkubo Y,Mutoh S

更新日期：2011-10-01 00:00:00

abstract：:Bromodomains are epigenetic readers of histone acetylation involved in chromatin remodeling and transcriptional regulation. The human proteome comprises 46 bromodomain-containing proteins with a total of 61 bromodomains, which, despite highly conserved structural features, recognize a wide array of natural peptide lig...

journal_title：Biochemical pharmacology

authors： Ferri E,Petosa C,McKenna CE

更新日期：2016-04-15 00:00:00

abstract：:Ellipticine is a potent antineoplastic agent whose mechanism of action is considered to be based mainly on DNA intercalation and/or inhibition of topoisomerase II. Recently, we found that ellipticine also forms covalent DNA adducts and that the formation of the major adduct is dependent on the activation of ellipticin...

journal_title：Biochemical pharmacology

authors： Frei E,Bieler CA,Arlt VM,Wiessler M,Stiborová M

更新日期：2002-07-15 00:00:00

abstract：:The addition of agents, such as tumor necrosis factor-alpha, to human peripheral neutrophils (HPPMN) induces priming, which enhances the receptor-mediated superoxide (O2-) generation and tyrosine phosphorylation of several HPPMN proteins. Lidocaine, a local anesthetic, inhibited both enhanced O2- generation and tyrosi...

journal_title：Biochemical pharmacology

authors： Kanbara T,Tomoda MK,Sato EF,Ueda W,Manabe M

更新日期：1993-04-22 00:00:00