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关键词:'M10050'
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B C Waldman et al.
Biochimica et biophysica acta, 1308(3), 241-250 (1996-09-11)
Inhibition of poly(ADP-ribosylation) reduces random genomic integration of transfected DNA and mildly stimulates intrachromosomal homologous recombination in mammalian cells. We investigated the effect of inhibition of poly(ADP-ribosylation) on the efficiency of gene targeting in Chinese hamster ovary (CHO) cell line
T Tsujiuchi et al.
Carcinogenesis, 11(10), 1783-1787 (1990-10-01)
The effects of inhibitors of poly(ADP-ribose)polymerase, 3-aminobenzamide (ABA), luminol and 3-methoxybenzamide (MBA) on the rat liver tumor promotion activity of phenobarbital (PB) were assessed. Fischer 344 male rats were initiated with N-nitrosodiethylamine (200 mg/kg) and placed on either basal diet
R C Tasker et al.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 18(12), 1346-1356 (1998-12-16)
In the infant brain, ischemia-induced ionic and enzyme mechanisms may independently lead to cell death by energy depletion: resequestration of calcium mobilized from intracellular stores consumes ATP, and activated poly(ADP-ribose) polymerase (PARP) uses oxidized nicotinamide adenine dinucleotide to form polyADP-ribosyl
Lloyd G Czaplewski et al.
Bioorganic & medicinal chemistry letters, 19(2), 524-527 (2008-12-10)
3-Methoxybenzamide is a weak inhibitor of the essential bacterial cell division protein FtsZ. Exploration of the structure-activity relationships of 3-methoxybenzamide analogues led to the identification of potent anti-staphylococcal compounds.
B C Waldman et al.
Nucleic acids research, 18(20), 5981-5988 (1990-10-25)
We determined the effect of 3-methoxybenzamide (3-MB), a competitive inhibitor of poly(ADP-ribose)polymerase (E.C. 2.4.2.30), on illegitimate and extrachromosomal homologous recombination in mouse Ltk- cells. Cells were transfected with a wild type Herpes thymidine kinase (tk) gene or with two defective
H Y Dong et al.
Mutation research, 331(2), 197-204 (1995-10-01)
To investigate the origin of DNA repair in rat pleural mesothelial cells (RPMC) exposed to asbestos fibers, poly(ADP-ribose) polymerase (PARP) activity was measured in the asbestos-treated cells. As bleomycin has been shown to activate poly(ADP-ribose) synthesis in several cell systems
Neil R Stokes et al.
Antimicrobial agents and chemotherapy, 57(1), 317-325 (2012-11-02)
The bacterial cell division protein FtsZ is an attractive target for small-molecule antibacterial drug discovery. Derivatives of 3-methoxybenzamide, including compound PC190723, have been reported to be potent and selective antistaphylococcal agents which exert their effects through the disruption of intracellular
D R Taylor et al.
Acta tropica, 50(2), 141-150 (1991-12-01)
We have demonstrated here that while many amastigotes of both Leishmania mexicana amazonensis and Leishmania mexicana mexicana differentiate to promastigotes when placed in culture at 27 degrees C, many others remain as amastigotes in their proliferative cycle. We have used
D Weltin et al.
International journal of immunopharmacology, 17(4), 265-271 (1995-04-01)
6(5H)-phenanthridinone, a recently identified poly(ADP-ribose)polymerase (PARP) inhibitor, is able, at micromolar concentrations, to inhibit concanavalin A-induced lymphocyte proliferation and to potentiate the effect of gamma radiation upon murine spleen cells. When added at the onset of a mixed lymphocyte culture
U Armato et al.
Biochemical and biophysical research communications, 182(3), 1066-1074 (1992-02-14)
Four tumor promoters, i.e. PB, TPA, NAF, and DDT, added singly to a calcium-deprived synthetic medium, elicited early and late mitogenic effects and concurrent surges of nuclear poly(ADP-ribose) polymerase (pADPRP) activity in primary neonatal rat hepatocytes mutagenized with an intra-uterine
S Hauschildt et al.
Advances in experimental medicine and biology, 419, 249-252 (1997-01-01)
Stimulating monocytes/macrophages with bacterial lipopolysaccharide (LPS) results in TNF-alpha, IL-1, IL-6 and nitrite (NO2-) formation. Inhibitors of poly(ADP-ribose)polymerase inhibit release of these mediators by preventing mRNA expression indicating that ADP-ribosylation plays a crucial role in the synthesis of these mediators.
A Colao et al.
Clinical endocrinology, 52(4), 437-445 (2000-04-13)
Dopamine agonists are indicated as primary therapy for PRL-secreting pituitary adenomas, while controversial results have been reported in nonfunctioning adenomas (NFA). To evaluate whether the in vivo visualization of dopamine D2 receptor expression detected by pituitary scintigraphy using 123I-methoxybenzamide (123I-IBZM)
N Nemoto et al.
Carcinogenesis, 12(4), 623-629 (1991-04-01)
Regulation of P(1)450 gene expression in mouse hepatocytes from responsive (C57BL/6) and non-responsive (DBA/2) strains in primary culture was investigated with respect to aryl hydrocarbon hydroxylase (AHH) activity and P450 transcript levels. Although significant induction of AHH activity in C57BL/6
G Golderer et al.
The Biochemical journal, 277 ( Pt 3), 607-610 (1991-08-01)
ADP-ribosylation of core histones was investigated in isolated nuclei of Physarum polycephalum. Core histone species differed in the mode of modification. Whereas ADP-ribosylation of H2A and H2B is sensitive to inhibition by 3-methoxybenzamide, as with most other nuclear acceptor proteins
C Dani et al.
Developmental biology, 203(1), 149-162 (1998-11-10)
The propagation of pluripotential mouse embryonic stem (ES) cells is sustained by leukemia inhibitory factor (LIF) or related cytokines that act through a common receptor complex comprising the LIF receptor subunit (LIF-R) and the signal transducer gp130. However, the findings
A S Waldman et al.
Nucleic acids research, 19(21), 5943-5947 (1991-11-11)
We determined the effect of 3-methoxybenzamide (3-MB), a competitive inhibitor of poly(ADP-ribose) polymerase (E.C. 2.4.2.30), on intrachromosomal homologous recombination in mouse Ltk- cells. We used a cell line that contained in its genome two defective Herpes thymidine kinase (tk) genes
Y Ohashi et al.
Journal of bacteriology, 181(4), 1348-1351 (1999-02-11)
3-Methoxybenzamide (3-MBA), which is known to be an inhibitor of ADP-ribosyltransferase, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells. Our genetic analysis of 3-MBA-resistant mutants indicated that the primary target of the drug is
J W Huh et al.
Journal of bacteriology, 178(16), 4935-4941 (1996-08-01)
Endogenous ADP-ribosylation was detected in Bacillus subtilis, as determined in vitro with crude cellular extracts. The ADP-ribosylated protein profile changed during growth in sporulation medium, displaying a temporary appearance of two ADP-ribosylated proteins (36 and 58 kDa) shortly after the
S Hauschildt et al.
The Biochemical journal, 288 ( Pt 1), 255-260 (1992-11-15)
The fibroblast cell line L929 contains a constitutively expressed NO synthase (EC 1.14.29.-) activity, which can be increased about 10-fold by tumour-necrosis factor alpha (TNF-alpha). Activities of the constitutive and the inducible enzymes are tetrahydrobiopterin-independent and can be inhibited by
P E Devaraj et al.
Molecular and cellular biochemistry, 124(2), 175-181 (1993-07-21)
In mouse fibroblasts stimulated from quiescence into proliferation by serum the induction of expression of the c-myc proto-oncogene is strongly stimulated by 3-methoxybenzamide. Similar superinduction effects are seen with related compounds such as 3-aminobenzamide and the acid analogues, 3-anisic acid
M Lechleitner et al.
Lipids, 29(9), 627-633 (1994-09-01)
A recently developed immunosuppressive substance, 2-chloro-2-deoxyadenosine (2-CdA), was reported to inhibit monocyte functions at low concentration. Because macrophages play a key role in the formation of atherosclerotic plaques, it was of interest to study the effect of 2-CdA on cellular
M Jesser et al.
Biochemical and biophysical research communications, 195(2), 558-564 (1993-09-15)
A cytoplasmic poly(ADP-ribose)polymerase (PARP) was purified from mouse plasmacytoma free messenger ribonucleoprotein particles using chromatography on 3-aminobenzamide affigel-10. The purified protein showed one band at 116 kDa on SDS-polyacrylamide gel electrophoresis and shared similar antigenic sites to the nuclear PARP.
C Le Page et al.
Advances in experimental medicine and biology, 419, 203-207 (1997-01-01)
Nitric oxide (NO) is a potent mediator involved in many biological functions including macrophage cytotoxicity and non-specific immunity against parasites, bacteria and viruses. Murine macrophages possess the capacity to express the inducible NO synthase (iNOS) which is not constitutively expressed
H Altmann
Acta biologica Hungarica, 41(1-3), 19-34 (1990-01-01)
Poly(ADP-ribose)-polymerase is an important cellular regulatory enzyme which can change chromatin structure and function. Action mechanisms and activation of the enzyme are described. The synthesis of poly(ADP-ribose) can be modulated by interaction of substances with the DNA binding site of
S Hauschildt et al.
Biochemical and biophysical research communications, 179(2), 865-871 (1991-09-16)
Stimulating bone marrow derived macrophages with LPS results in the induction of NO-synthase as measured by NO2- formation. Inhibitors of poly(ADP-ribose)polymerase, namely nicotinamide, 3-aminobenzamide and 3-methoxybenzamide, prevented NO2- formation in a dose dependent manner. Inhibition was most effective if the
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