• Archives of Pharmacal Research
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• 제25권3호
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• pp.375-380
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• 2002

Cytochrome P4501A2 (CYP1A2) is a member of the cytochrome P450 family of isozymes involved in the phase I drug metabolism of vertebrates. CYP1A2 is responsible for the activation of a number of aromatic amines to mutagenic and carcinogenic forms. Thus, the level of CYP1A2, which varies among different populations, may determine an individual's susceptibility to these chemicals. We have previously reported on the importance of a cis element named PRB (protected region B) in the regulation of human Cytochrome P4501A2 (CYP1A2) gene, which appeared to act as a positive regulatory element. Closer examination of the PRB sequence (-2218 to -2187 bp) revealed a putative AP-1 binding site, TGACTAA, at -2212 bp (Chung and Bresnick, 1997). To elucidate the role of AP-1 in CYP1A2 regulation, we transiently overexpressed c-Jun and c-Fos transcription factors in human hepatoma HepG2 cells, and examined their influence on the CYP1A2 promoter activity by reporter gene assays. Cotransfection of the c-Jun and the c-Fos expression vectors increased the induced transactivation by five to six fold from the CYP1A2 promoter constructs. However, deletion of the PRB element did not affect the degree of activation by the c-Jun and the c-Fos. Therefore, it is unlikely that the c-Jun and the c-Fos activate the CYP1A2 promoter through this AP-1 consensus-like sequence in the PRB region.

• Bulletin of the Korean Chemical Society
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• 제34권11호
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• pp.3233-3238
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• 2013

Two new Cu(II) complexes, $[Cu_2(acpy-mdtc)_2(HBA)(ClO_4)]{\cdot}H_2O$ (1) (acpy-mdtc- = 2-acetylpyridine S-methyldithiocarbamate and $HBA^-$ = benzilic acid anion) and $[Cu_2(acpy-phtsc)_2(HBA)]{\cdot}ClO_4$ (2) (acpy-$phtsc^-$ = 2-acetylpyridine 4-phenyl-3-thiosemicarbazate) have been synthesized and characterized by elemental analysis, infrared spectroscopy, thermogravimetric analysis, and single crystal X-ray diffraction. The X-ray analysis reveals that the structures of 1 and 2 are dinuclear copper(II) complexes bridged by two thiolate sulfur atoms of Schiff base ligand and bidentate bridging $HBA^-$ anion. For 1, each of the two copper atoms has different coordination environments. Cu1 adopts a five-coordinate square-pyramidal with a $N_2OS_2$ donor, while Cu2 exhibits a distorted octahedral geometry in a $N_2O_2S_2$ manner. For 2, two Cu(II) ions all have a five-coordinate square-pyramidal with a $N_2OS_2$ donor. In each complex, the Schiff base ligand is coordinated to copper ions as a tridentate thiol mode.

• Bulletin of the Korean Chemical Society
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• 제18권10호
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• pp.1050-1052
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• 1997

The complexes M(CO)4-1,2-(PPh2)2-1,2-C2B10H10 (M=Cr 2a, Mo 2b, W 2c) have been prepared in good yields from readily available bis-diphenylphosphino-o-carboranyl ligand, closo-1,2-(PPh2)2-1,2-C2B10H10 (1), by direct reaction with Group Ⅵ metal carbonyls. The infrared spectra of the complexes indicate that there is an octahedral disposition of chelate bis-diphenylphosphino-o-carboranyl ligand around the metal atom. The crystal structure of 2a was determined by X-ray diffraction. Complex 2a crystallizes in the monoclinic space group P21/n with cell parameters a = 12.2360(7), b = 17.156(1), c = 16.2040(6) Å, V = 3354.1(3) Å3, and Z =4. Of the reflections measured a total of 2514 unique reflections with F2 > 3σ(F2) was used during subsequent structure refinement. Refinement converged to R1 = 0.066 and R2 = 0.071. Structural studies showed that the chromium atom had a slightly distorted pseudo-octahedral configuration about the metal center with two phosphine groups of o-carborane occupying the equatorial plane cis-orientation to each other. These metal carbonyl complexes are rapidly converted to the corresponding metal carbene complexes, [(CO)3M=C(OCH3)(CH3)]-1,2-(PPh2)2-1,2-C2B10H10 (M= Cr 3a, Mo 3b, W 3c), via alkylation with methyllithium followed by O-methylation with CF3SO3CH3.

• 정보처리학회논문지A
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• 제16A권4호
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• pp.223-226
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• 2009

하이퍼큐브와 많은 면에서 비슷하면서도 절반 정도의 지름을 가지는 등 개선된 망 성질들을 가지는 꼬인 큐브는 병렬처리 시스템의 상호연결망으로 각광 받아 왔다. 짝수인 m 에 대하여 크기가 $2{\times}2^m$인 메쉬가 연장률 1과 확장율 1로, 혹은 크기가 $4{\times}2^m$인 메쉬가 연장율 1과 확장율 2로 꼬인 큐브에 임베딩됨은 최근에 알려졌다 [Lai and Tsai, 2008]. 그러나 양변의 길이가 모두 8 이상인 메쉬가 꼬인 큐브에 연장율 1로 임베딩되는지는 알려진 바가 없다. 본 논문에서는 m 이 짝수일 경우엔 크기 $2^n{\times}2^m$인 메쉬가 꼬인 큐브에 연장율 1, 확장율 $2^{n-1}$ 로 임베딩됨을 보이고 m이 홀수일 경우엔 연장율 1, 확장율 $2^n$로 임베딩됨을 보인다 ($1{\leq}n{\leq}m$).

• BMB Reports
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• 제44권8호
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• pp.553-557
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• 2011

We previously reported that CDK2/Cyclin A can phosphorylate and activate the transcription factor NF-Y. In this study, we investigated a potential regulatory role for NF-Y in the transcription of Cyclin A and other cell cycle regulatory genes. Gel-shift assays demonstrate that NF-Y binds to CCAAT sequences in the Cyclin A promoter, as well as to those in the promoters of cell cycle G2 regulators such as CDC2, Cyclin B and CDC25C. Furthermore, expression of Cyclin A increases NF-Y's affinity for CCAAT sequences in the CDC2 promoter; however, Cyclin A's induction of CDC2 transcription is antagonized by p21, an inhibitor of CDK2/Cyclin A. These results suggest a model wherein NF-Y binds to and activates transcription from the Cyclin A promoter, increasing cellular levels of Cyclin A/CDK2 and potentiating NF-Y's capacity for transcriptional transactivation, and imply a positive feedback loop between NF-Y and Cyclin A/CDK2. Our findings are additionally indicative of a role for Cyclin A in activating Cyclin B/CDK1 through promoting NF-Y dependent transcription of Cyclin B and CDC2; NF-Y mediated crosstalk may therefore help to orchestrate cell-cycle progression.

• 약학회지
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• 제48권4호
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• pp.254-260
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• 2004

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 2,4-difluorophenyl( 2a-5a), 2,5-difluorophenyl(2b-5b), 4-ethylphenyl(2c-5c), 2-hydroxyphenyl(2d-5d) and 2-methylnaphthyl(2e-5e) instead of naphthyl group with hydrogen(3a-3e), methyl(4a-4e), and ethyl(5a-5e) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds( 3a, 4a, 5a, 3d, 4d, 4d, 5d, 3e, and 4e) showed significant anti-fungal activity against T. mentagroPhytes. (E)-N-(3-Phenyl-2-propenyl)-2- hydroxy-benzenemethaneamine( 3d) displayed moderate antifungal activity against all five different fungi.

• 한국결정학회지
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• 제2권1호
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• pp.12-16
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• 1991

p-dimethylaminobenzaldehyde 4-(p-ethoxyphenyl) thiosemicarbazone, C18H22N4OS의, 단위포상수는 단사정계 a=11.802(2), b=31.962(2), c=9.829(2)A, β=100.12(1)˚, V=3694.8A3이며 F(000)=1472, Mr=342.47, 공간군은 P2₁/c, Z=8, Dx=1.246 Mg m-3, Dm=1.17Mg m-3, μ=0.15mm-1이다. T=294 K에서 Mo Ka(λ=0.71073 A)을 사용하여 최종 R값은 0.0856이다. 비대칭단위내의 두개 분자간의 구조상의 큰차이는 C(9)-N(1)-C(6)-C(7)의 비틀림각이 각각 58.8(8)˚와 1(1)˚인것으로, 각 분자는 길이가 각각 2.613(7)과 2.566(7) A인 N(1)-H(10)'N(3) 분자내 수고결합을 하고 있으며 각 분자는 N(2)원자를 정점으로 하여 V-모양을 하고 있다. 독립적인 두 분자는 두개의 분자간 수소 결합 N(2)-H(11)'S'=3.367(5) A과 N(2')-H(11')'S=3.421(4)A으로 연결되어 이중체(dimer)를 형성하고 있으며 그 이중체들은 van der Waals력으로 결합되어 있다.

• Bulletin of the Korean Chemical Society
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• 제20권3호
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• pp.307-313
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• 1999

2,4-Di-(2'-vinyloxyethoxy)benzylidenemalononitrile (la), methyl 2,4-di-(2'-vinyloxyethoxy)benzylidenecyanoacetate (lb), 3,4-di-(2'-vinyloxyethoxy)benzylidene malononitrile (2a), methyl 3,4-di-(2'-vinyloxyethoxy)benzylidenecyanoacetate (2b), 2,5-di-(2'-vinyloxyethoxy)benzylidenemalononitrile (3a), methyl 2,5-di-(2'-vinyloxyethoxy)benzylidenecyanoacetate (3b), 2,3-di-(2'-vinyloxyethoxy)benzylidenemalononitrile (4a), and methyl 2,3-di-(2'-vinyloxyethoxy)benzylidenecyanoacetate (4b) were prepared by the condensation of 2,4-di-(2'-vinyloxyethoxy)benzaldehyde, 3,4-di-(2'-vinyloxyethoxy)benzaldehyde, 2,5-di-(2'-vinyloxyethoxy) benzaldehyde, and 2,3-di-(2'-vinyloxyethoxy)benzaldehyde with malononitrile or methyl cyanoacetate, respectively. Trifunctional divinyl ether monomers 1-4 were polymerized readily with boron trifluoride etherate as a cationic initiator to give optically transparent swelling poly(vinyl ethers) 5-8 havina oxybenzylidenemalononitrile and oxycyanocinnamate, which is presumably effective chromophore for second-order nonlinear optical applications. Polymers 5-8 were not soluble in common organic solvents such as acetone and DMSO due to crosslinking. Polymers 5-8 showed a thermal stability up to 300 ℃ in TGA thermograms, which is acceptable for electrooptic device applications.

• 약학회지
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• 제47권5호
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• pp.293-299
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• 2003

Structure-activity relationship studies of allylamine type of antimycotics were carried out to evaluate the effect of naphthyl and methyl portion of naftifine. Compounds with 4-fluorophenyl(2a-5a), 2-fluorophenyl(2b-5b), 2,4-dichlorophenyl(2c-5c), 2,6-dichlorophenyl(2d-5d), 4-nitrophenyl(2e-5e), and 2,3-dihydro-benzo[1,4]dioxan-6-yl( 2f-5f) instead of naphthyl group with hydrogen(3a-3f), methyl(4a-4f), and ethyl(5a-5f) in the place of methyl in naftifine were synthesized and tested their in vitro anti-fungal activity against five different fungi. Eight compounds(3a, 5a, 3c, 4c, 4d, 5d, 5e, and 4f) showed significant antifungal activity against T. mentagrophytes. (E)-N-Ethyl-(3-phenyl-2-propenyl)-4-nitro-benzenemethaneamine(5e) displayed moderate antifungal activity against all five different fungi.

• BMB Reports
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• 제28권4호
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• pp.331-335
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• 1995

Simian virus 40 (SV40) small-t antigen (small-t) has been known to regulate the activity of a cellular enzyme, protein phosphatase 2A (PP2A), composed of A. B, and C subunits, via binding to the A subunit In the study presented here, the stoichiometry of the binding of small-t to PP2A was determined to be 1: 1. It was also shown that small-t binds to the AC form of PP2A with a higher apparent affinity than it binds to the free A subunit. We also characterized the interaction of PP2A with wild-type and various mutant small-ts. A single-point mutant (Val134Met) and a double-point mutant (Trp147Gly;Leu152 Pro) of small-t exhibited 3-fold and 5-fold lower potencies in inhibiting PP2A activity. respectively. This suggests that the region around amino acids between 134 and 152 of small-t might be important in regulating the enzyme activity of PP2A.