• Title/Summary/Keyword: ligand selectivity

검색결과 73건 처리시간 0.032초

SIRT1 억제에 의한 DR5 발현증강과 c-FLIP 발현저해 작용으로 사람유방암세포 MCF-7의 TRAIL 감수성 증강 (Inhibition of SIRT1 Sensitizes TRAIL-Resistant MCF-7 Cells by Upregulation of DR5 and Inhibition of c-FLIP)

  • 이수훈;김학봉;김미주;이재원;배재호;김동완;강치덕;김선희
    • 생명과학회지
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    • 제22권10호
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    • pp.1277-1285
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    • 2012
  • Tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)은 암세포 선택적으로 작용하므로서 유용한 항암제로 주목 받고 있다. 그러나, TRAIL 에 내성을 나타내는 암세포도 많이 존재한다. 그러므로 TRAIL 내성을 극복할 수 있는 방법을 고안하는 연구는 암 치료 요법에 매우 중요하다. 본 연구에서는 SIRT1 siRNA 또는 SIRT1 inhibitor인 amurensin G를 사람 유방암세포에 처리하면 DR5및 c-Myc의 발현 증강과 c-$FLIP_{L/S}$ 및 Mcl-1 발현 억제를 유도하므로서, TRAIL 에 내성을 나타내는 사람유방암세포 MCF-7 세포의 TRAIL 감수성을 증강시킴을 알 수 있었다. 또한, SIRT1 억제에 의한 caspase 활성화, PARP cleavage 및 Bcl-2 발현감소를 나타내었다. 이러한 연구결과는 SIRT1 저해에 의한 DR5 유도와 함께 c-FLIP 발현 억제가 TRAIL 내성 암세포의 TRAIL 반응성 증강에 유용한 기전으로 사용 될 수 있음을 시사하였다.

Potentially Multidentate Tripodal Amine Catechol Ligands as Chelators for Ga(III) and In(III)

  • Sahoo, Suban K.;Baral, Minati;Bera, Rati Kanta;Kanungo, B. K.
    • Bulletin of the Korean Chemical Society
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    • 제30권9호
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    • pp.1956-1962
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    • 2009
  • The binding abilities of two multidentate tripodal amine catechol ligands, cis,cis-1,3,5-tris[(2,3-dihydroxybenzylamino) aminomethyl]cyclohexane (TMACHCAT, $L^1)\;and\;N^1,N^3,N^5$-tris(2-(2,3-dihydroxybenzylamino) ethyl)cyclohexane-1,3,5-tricarboxamide (CYCOENCAT, $L^2$) with Ga(III) and In(III) have been investigated by potentiometric and spectrophotometric methods in an aqueous medium of 0.1 M KCl at 25 ${\pm}\;1\;{^{\circ}C}.$ The ligands $L^1\;and\;L^2$ formed various monomeric species $MLH_3,\;MLH_2$, MLH and ML (M = $Ga^{+3}\;and\;In^{+3}$) and showed potential to form strong encapsulated tris(catechol) type complexes. The coordination modes, binding ability and selectivity of the ligands towards Ga(III) and In(III) have been discussed with the help of experimental evidences, and supported with molecular modeling calculations.

Synthesis and Selective Recognition of Dihydrogen Phosphate by Urea-Anthraquinone

  • Jeon, Seung-Won;Park, Duck-Hee;Lee, Hyo-Kyoung;Park, Jin-Young;Kang, Sung-Ok;Nam, Kye-Chun
    • Bulletin of the Korean Chemical Society
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    • 제24권10호
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    • pp.1465-1469
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    • 2003
  • A neutral ligand is synthesized and studied for the binding properties with anions by electrochemical methods. The binding of 1,8-bis[(N'-phenylureido)ethyloxy]anthraquinone (BPUA) with $H_2PO_4^-$ makes cathodic shift of its electrochemical potentials and red shift of absorption band. This novel neutral anion receptor BPUA binds anions through hydrogen bonding and show high selectivity with $H_2PO_4^-$ over $CH_3CO_2^-,CI^-,{\;}and{\;}HSO_4^-$. The selecivity of H_2PO_4^-$ over $CH_3CO_2^-,CI^-,{\;}and{\;}HSO_4^-$ may be attributed to the stronger hydrogen bonding with urea moiety and also with anthraquinone moiety of BPUA receptor, and also the higher complementarity of the cavity of BPUA for tetrahedral H_2PO_4^-$.

Tetradiazo(o-carboxy)phenylcalix[4]arene for Determination of Pb2+ Ion

  • Tan, Le Van;Quang, Duong Tuan;Lee, Min-Hee;Kim, Tae-Hyun;Kim, Ha-Suck;Kim, Jong-Seung
    • Bulletin of the Korean Chemical Society
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    • 제28권5호
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    • pp.791-794
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    • 2007
  • A new azocalix[4]arene, 5,14,17,23-tetra[(2-benzoic acid)(azo)phenyl] calix[4]arene (2), has been prepared by hydrolysis of its ester derivative and characterized by 1H NMR, IR, UV-Vis spectroscopy and elemental analysis. Based on UV spectral changes, we found that 2 exhibits Pb2+ ion selectivity. In basic media, Pb2+ forms a 1:1 complex with the ligand. Beer's law is obeyed in the range of 2.0 × 10?6 ? 2.4 × 10?5 mol L?1 of Pb2+. The molar absorptivity (ε ) of 2-Pb2+ complex is 1.89 × 104 L mol?1 cm?1 at 440 nm, and the detection limit is 1.6 × 10?6 mol L?1.

A Carbazole-Attached NO2S2-Macrocycle Exhibiting Hg2+ and Cu2+ Selectivity

  • Lee, Seul-Gi;Kang, Eun-Ju;Lee, Shim Sung
    • Bulletin of the Korean Chemical Society
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    • 제34권5호
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    • pp.1429-1434
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    • 2013
  • A synthesis and cation-induced fluorescent behavior of the carbazole-attached $NO_2S_2$-macrocycle (L) is described and structurally characterized by single crystal X-ray analysis. The photoluminescence spectrum of L in 80% $CH_3CN/CH_2Cl_2$ displays a peak maximum at 431 nm (blue emission). In the metal-induced fluorometric experiment, L showed a drastic chelation-enhanced fluorescence quenching (CHEQ) effect only with $Hg^{2+}$ and $Cu^{2+}$. In ESI-mass study, a 1:1 stoichiometry for complexation of L with $Hg^{2+}$ was confirmed, suggesting the unique sensing behavior of the proposed ligand L due to the selective complexation affinity for $Hg^{2+}$. The observed results indicate that L is a promising turn-off type fluoroionophore for $Hg^{2+}$ and $Cu^{2+}$ detections. Additionally, the $Ag^+$ complex of the precursor macrocycle was prepared and its solid structure was crystallographically characterized.

Interaction of the Post-transition Metal Ions and New Macrocycles in Solution

  • Jung, Oh-Jin
    • Bulletin of the Korean Chemical Society
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    • 제14권6호
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    • pp.687-691
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    • 1993
  • Complexation of $Cd^{2+},\;Pb^{2+}\;and\;Hg^{2+}$ ions with four cryptands were studied by potentiometry and solution calorimetry in various weight percent methanol-aqueous solvent at 25${\circ}$C under $CO_2$free nitrogen atmosphere. The stabilities of the complexes were dependent on the cavity size of macrocycles. The $Hg^{2+}$ ion stability constants are higher than those of $Cd^{2+}\;and\;Pb^{2+}$ ion. All the cryptands formed complexes having 1 : 1 (metal to ligand) mole-ratio except for $Hg^{2+}-L_1$ (cryptand 1,2b: 3,5-benzo-9,14,17-trioxa-1,7-diazabicyclo-(8,5,5) heptadecane) and $Cd^{2+}-L_2$ (cryptand 2,2b: 3,5-benzo-10,13,18,21-tetraoxa-1,7-diazabicyclo (8,5,5) eicosane) complexes. $Hg^{2+}-L_1$ complex was a sandwitch type, and the $Cd^{2+}-L_2$ complex showed two stepwise reactions. Thermodynamic parameters of the $Cd^{2+}-L_2$ complex were $6.08(log\;K_1)$, -7.28 Kcal/mol $({\Delta}H_1)$, and $4.78\;(log\;K_2)$, -4.62 Kcal/mol $({\Delta}H_2)$, respectively, for 1 : 1 and 2: 1 mole-ratio. The sequences of the selectivity were increased in the order of $Hg^{2+}\;>Pb^{2+}\;>Cd^{2+}$ ion for $L_3\;and\;L_4$ macrocycles, and the $L_2$-macrocycle has a selectivity for $Cd^{2+}$ ion relative to $Zn^{2+},\;Ni^{2+},\;Pb^{2+}\;and\;Hg^{2+}$ ions. Thus, it is expected that the $L_2$ can be used as carrier for seperation of the post transition metals by macrocycles-mediated liquid membrane because $L_2$ is not soluble in water, and the difference of stability constants of the metal complexes with $L_2$ are large as compared with the other transition metal complexes. The $^1H\;and\;^{13}C-NMR studies indicated that the nitrogen atoms of cryptands have greater affinity to the post transition metal ions than the oxygen atoms, and that the planarities of the macrocycles were lost by complexation with the metal ions because of the perturbation of ring current of benzene molecule attached to macrocycles and counter-anions.

철-디피리딜-메페남산 삼원착물을 이용한 메페남산의 정량 (Determination of Mefenamic Acid with Fe(II)-Dipyridyl-Mefenamic Acid Ternary Complex as Ion-exchagner)

  • 남수자;문현숙;이미나;정문모;허문희;안문규
    • 분석과학
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    • 제14권1호
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    • pp.59-63
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    • 2001
  • 철-디피리딜-메페남산 삼원착물을 이온교환체로, NPOE(o-nitrophenyl octyl ether)를 가소게, PVC[poly(vinyl chloride)]를 지지체로 사용한 메페남산 이온선택성막 전극을 제작하였다. 디피리딜 화합물은 2,2'-디피리딜, 4,4'-디피리딜 그리고 4,4'-디페닐-2,2'-디피리딜을 이용하였다. 이들 막전극은 pH 8.9의 붕산완충액 중에서 $10^{-5}{\sim}10^{-3}mol/L$ 농도의 메페남산에 대하여 감응전위가 -55.98, -49.47 그리고 -59.35mV/decade를 각각 나타내는 직선성이었다. 방향족 및 지방족 카복실산염의 존재는 전극의 감응에 지장을 주지 않았다.

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Two 3D CdII and ZnII Complexes Based on Flexible Dicarboxylate Ligand and Nitrogen-containing Pillar: Synthesis, Structure, and Luminescent Properties

  • Liu, Liu;Fan, Yan-Hua;Wu, Lan-Zhi;Zhang, Huai-Min;Yang, Li-Rong
    • Bulletin of the Korean Chemical Society
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    • 제34권12호
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    • pp.3749-3754
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    • 2013
  • Two 3D isomorphous and isostructural complexes, namely, $[Zn(BDOA)(bpy)(H_2O)_2]_n$ (1) and $[Cd(BDOA)-(bpy)(H_2O)_2]_n$ (2); (BDOA = Benzene-1,4-dioxyacetic acid, bpy = 4,4'-bipyridine) were synthesized under hydrothermal conditions and characterized by means of elemental analyses, thermogravimetric (TG), infrared spectrometry, and single crystal X-ray diffraction. Complexes 1 and 2 crystallize in the triclinic system, space group P-1 and each metal ion in the complexes are six-coordinated with the same coordination environment. In the as-synthesized complexes, $BDOA^{2-}$ anions link central metal ions to form a 1D zigzag chain $[-BDOA^{2-}-Zn(Cd)-BDOA^{2-}-Zn(Cd)-]_{\infty}$, whereas bpy pillars connect metal ions to generate a 1D linear chain $[-bpy-Zn(Cd)-bpy-Zn(Cd)-]_{\infty}$. Both infinite chains are interweaved into 2D grid-like layers which are further constructed into a 3D open framework, where hydrogen bonds play as the bridges between the adjacent 2D layers. Luminescent properties of complex 1 showed selectivity for $Hg^{2+}$ ion.

Physalin D inhibits RANKL-induced osteoclastogenesis and bone loss via regulating calcium signaling

  • Ding, Ning;Lu, Yanzhu;Cui, Hanmin;Ma, Qinyu;Qiu, Dongxia;Wei, Xueting;Dou, Ce;Cao, Ning
    • BMB Reports
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    • 제53권3호
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    • pp.154-159
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    • 2020
  • We investigated the effects of physalin A, B, D, and F on osteoclastogenesis induced by receptor activator of nuclear factor κB ligand (RANKL). The biological functions of different physalins were first predicted using an in silico bioinformatic tool (BATMAN-TCM). Afterwards, we tested cell viability and cell apoptosis rate to analyze the cytotoxicity of different physalins. We analyzed the inhibitory effects of physalins on RANKL-induced osteoclastogenesis from mouse bone-marrow macrophages (BMMs) using a tartrate-resistant acid phosphatase (TRAP) stain. We found that physalin D has the best selectivity index (SI) among all analyzed physalins. We then confirmed the inhibitory effects of physalin D on osteoclast maturation and function by immunostaining of F-actin and a pit-formation assay. On the molecular level, physalin D attenuated RANKL-evoked intracellular calcium ([Ca(2+)](i)) oscillation by inhibiting phosphorylation of phospholipase Cγ2 (PLCγ2) and thus blocked the downstream activation of Ca2+/calmodulin-dependent protein kinases (CaMK)IV and cAMP-responsive element-binding protein (CREB). An animal study showed that physalin D treatment rescues bone microarchitecture, prevents bone loss, and restores bone strength in a model of rapid bone loss induced by soluble RANKL. Taken together, these results suggest that physalin D inhibits RANKL-induced osteoclastogenesis and bone loss via suppressing the PLCγ2-CaMK-CREB pathway.

황화납 양자점 감지막을 통해 감도가 개선된 수소센서 (Sensitivity enhancement of H2 gas sensor using PbS quantum dots)

  • 김세완;김나리;권진범;김재건;정동건;공성호;정대웅
    • 센서학회지
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    • 제29권6호
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    • pp.388-393
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    • 2020
  • In this study, a PbS quantum dots (QDs)-based H2 gas sensor with a Pd electrode was proposed. QDs have a size of several nanometers, and they can exhibit a high surface area when forming a thin film. In particular, the NH2 present in the ligand of PbS QDs and H2 gas are combined to form NH3+, subsequently the electrical characteristics of the QDs change. In addition to the resistance change owing to the reaction between Pd and H2 gas, the resistance change owing to the reaction between the NH2 of PbS QDs and H2 gas increases the current signal at the sensor output, which can produce a high output signal for the same concentration of H2 gas. Using the XRD and absorbance properties, the synthesis and particle size of the synthesized PbS QDs were analyzed. Using PbS QDs, the sensitivity was significantly improved by 44%. In addition, the proposed H2 gas sensor has high selectivity because it has low reactivity with heterogeneous gases such as C2H2, CO2, and CH4.