• Title/Summary/Keyword: 결합체

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Antiestrogen등 약물이 cytochrome P450와 AEBS에 미치는 효과의 관계

  • 신윤용;정세영
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.100-100
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    • 1993
  • Antiestrogen은 에스트로젠 의존성 유방암 치료에 사용되는 약물로써 표적 세포 내에서 에스트로젠 수용체와 작용하여 세포 증식 억제 작용을 나타내고 동시에 에스트로젠 수용체와는 구분되는 소포체 분획의 antiestrogen specific binding site (AEBS) 와도 결합을 하는 것으로 알려져 있다. 그러나, 아직 이 AEBS의 생리적 또는 약리적 기능은 밝혀져 있지 않다. 따라서 본 실험에서는 AEBS의 기능을 조사하기 위하여 cytochrome P45O III 효소군과 AEBS와의 관계를 자옹 백서를 이용하여 면역 화학 반응 실험 및 경쟁적 결합 반응 실험을 하였고, 그 결과는 다음과 같다. 1) AEBS에 대해서 SKF-525A와 metyrapone은 결합 능력을 나타내었다. 2) 자성쥐에서는 주령이 증가함에 따라 cytochrome P450양이 감소하였다. 3) 자옹성쥐 모두에서 phenobarbital 처치에 의해 cytochrome P450 III 효소양이 증가하였고, AEBS도 증가하였다. 4) 웅성쥐에서는 testosterone에 의하여 AEBS가 증가하였다. 5) 자웅성쥐 모두에 tamoxifen 관류시 cytochrome P450 III 효소양이 증가하였고 estradiol과 병용 관류시에는 tamonifen 단독 관류시보다 감소하였다. 이상의 결과에서 tamoxifen이 cytochrome P450 III을 유도할 수 있는 것으로 사료되며 cytochrome P450 III 효소군과 안티에스트로젠 결합부위와 밀접한 관련이 있는 것으로 생각된다.

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Non-Radiative Dielectric(NRD) Rotman Lens with Gap-Coupled Unidirectional Dielectric Radiator(UDR) (갭 결합된 단향성 유전체 방사체를 적용한 비방사 유전체 로트만 렌즈)

  • 이재곤;이정해
    • The Journal of Korean Institute of Electromagnetic Engineering and Science
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    • v.14 no.12
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    • pp.1269-1275
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    • 2003
  • In this paper, nonradiative dielectric(NRD) rotman lens with a gap-coupled unidirectional dielectric radiator(UDR) has been designed. Gap-coupled UDR is structurally suitable for NRD rotman lens. We have optimized NRD rotman lens for minimizing side-lobe, and calculated design parameters of UDR such as length of resonator and distance of gap using an equivalent circuit model of an evanescent NRD guide. Experimental prototype of UDR is fabricated and measured at the center frequency of 38 GHz. The simulated S-parameter and far-field radiation beam pattern of UDR show good agreements with measured data. Finally, total beam pattern of NRD rotman lens of multi-beam feed has been obtained using a measured pattern of UDR and array factor of NRD rotman lens. The obtained beam pattern shows remarkably suppressed side-lobe.

Molecular Holographic QSAR Analysis on the Bonding Affinity Constants between Nicotin Acetylcholine Receptors and New 3-Benzylidenemyosmine Analogues and Molecular Design (새로운 3-Benzylidenemyosmine 유도체와 Nicotin Acetylcholine 수용체 사이의 결합 친화력 상수에 관한 HQSAR 분석과 분자설계)

  • Jang, Seok-Chan;Sung, Nack-Do
    • Applied Biological Chemistry
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    • v.50 no.2
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    • pp.127-131
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    • 2007
  • The molecular design and holographic (H) quantitative structure-activity relationships (HQSARs) on the binding affinity constants between new 3-benzylidenemyosmine analogues and nicotin acetylcholine receptors (nAChRs) of American cockroach (Periplaneta. americana L.) were studied quantitatively. The optimized HQSAR model (IV-2) for the binding affinity constants was derived from fragment distinction of hydrogene atoms in fragment size, 5${\sim}$8 bin. The statistical results of the HQSAR model (IVI-2) exhibited the best predictability and fitness for the binding affinity constants based on the cross-validated value (q$^2$=0.507) and non cross-validated value (r$^2_{nev.}$=0.944). From the graphical analyses of atomic contribution maps, it was revealed that the binding affinity constants depends upon the anabaseine ring in molecule and the most active compounds were designed by optimized HQSAR model (VI-2).

Effects of Neuroleptics on the Opioid Receptor Binding in the Mouse Striatum (마우스 선조체에서 Opioid 수용체 결합에 대한 Neuroleptics의 영향)

  • Kim, Soo-Kyung;Lee, Seong-Ryong;Park, Chang-Gyo
    • The Korean Journal of Pharmacology
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    • v.30 no.3
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    • pp.291-297
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    • 1994
  • Our purpose was to gain insight into a possible modulatory role for ${\mu},\;{\delta},\;and\;{\kappa}$ opioid receptors by neuroleptics (chlorpromazine, thioridazine, haloperidol, sulpiride, and pimozide) in chronic morphine 5 mg/kg and 20 mg/kg treated mouse striatum. We attempted quantitative receptor assays using highly specific radioligands, $[^3H]\;DAGO\;([D-Ala^2,\;N-Mephe^4,\;Glycol^5]\;enkephalin)$, $[^3H]DPDPE\;([D-Pen^2,\;D-Pen^5]\;enkephalin)$ and $[^3H]\;DPN(diprenorphine)$ to measure the binding affinity in the experimental groups. The decrease of $[^3H]DAGO$ binding was potentiated by sulpiride and pimozide in the chronic morphine treatment (5 mg/kg and 20 mg/kg). The decrease of $[^3H]DPDPE$ binding was inhibited by chlorpromazine, thioridazine, haloperidol, sulpiride, and pimozide in chronic morphine treatment (5 mg/kg and 20 mg/kg). The decrease of $[^3H]\;DPN$ binding was significantly inhibited by chlorpromazine, thioridazine, sulpiride, and pimozide in chronic morphine 20 mg/kg treatment. $[^3H]\;DPN$ binding on the neuroleptics was antagonized by naloxone pretreatment in chronic morphine 20 mg/kg treatment. These findings suggest that neuroleptics influence opposing tonically active on the ${\delta},\;and\;{\kappa}$ opioid receptor compared with ${\mu}$ opioid receptor in the chronic morphine treated mouse striatum.

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A Study on Resonance Frequencies of a Whispering Gallery Mode Dielectric Resonator Considering Electromagnetic Coupling Phenomena with an Excitation Part (여기부와의 전자파 결합 현상을 고려한 위스퍼링 갤러리 모드 유전체 공진기의 공진주파수에 관한 연구)

  • 황재효;민경일;구경완
    • The Journal of Korean Institute of Electromagnetic Engineering and Science
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    • v.9 no.5
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    • pp.603-613
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    • 1998
  • Resonant characteristic of Whispering modes(W. G. mode) on a dielectric disk resonator is influenced by an external circuit that is placed near the disk to excite this type of modes. In order to evaluate this phenomenon, we divide the disk resonator as two parts; a coupling part in which the mode coupling occurs and on uncoupled region. In the coupled part, we regard the part of the disk as a curved waveguide which is loaded with matched circuit, and derive a coupled mode equation for nonparallel dielectric waveguides. From the coupled mode equation, we calculate coupling coefficients and a coupled electromagnetic field. By using the complex coupling coefficients, we can calculate power transfer. We also calculate a resonant frequency in consideration of the mode coupling phenomenon. The calculated resonance frequence is confirmed by experiment for the resonance characteristics. As the results, it is found that the discrepancy between the theoretical and the experimental resonance frequencies is about 1.28% and the discrepancy between theory and experiment of FSR is about 0.6%.

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The Effect of a Potent Oxytocin Antagonist, Antag I, on In Vitro Uterine Contractions in Response to Exogenous Oxytocin and on Uterine Oxytocin Receptor Number and Affinity (옥시토신 길항제, Antag I이 옥신토신 투여에 따른 자궁수축과 자궁의 옥시토신 수용체 수 및 친화력에 미치는 영향)

  • ;C. Warnell;G. Flouret;L. Wilson Jr.
    • Korean Journal of Animal Reproduction
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    • v.18 no.2
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    • pp.95-99
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    • 1994
  • The purpose of the present study was to determine the in vivo effect of oxytocin antagonist-I(Al) on uterine oxytocin receptor number (Rn) and/or binding affinity (Kd) in the estrous rat. Anesthetized rats were given a bolus infusion of control or 5${\mu}\textrm{g}$ of AI and sacri-ficed 0.5 and 4 hours later. The uterine tissue was removed, trimmed and frozen. Membrane oxytocin receptors were isolated after homogenization of uterine tissue and differential ultracentrifugation. The oxytocin receptor assay was performed by saturation with cold oxytocin competion with a high specific activity oxytocin antagonist. Rn and Kds were determined by nonlinear curve fitting methods. No differences(p>0.05) between the AI and control treated animals in either oxytocin receptor number or binding affinity was detected in this study. These data suggest that the major mode of action of AI is via competitive inhibition at the uterine oxytocin receptor and not by altering receptor number or binding affinity.

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Protein Binding Characteristics of Brazilin and Hematoxylin

  • Moon, Chang-Kiu;Lee, Jong-Hwoa;Ha, Bae-Jin
    • Journal of Food Hygiene and Safety
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    • v.7 no.2
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    • pp.77-82
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    • 1992
  • In order to investigate the protein binding characteristics of braD6n and hematoxy6n to bovine semm albumin (BSA), the fluorescence probe method was adopted. Brazilin and hematoxy6n showed strong binding affinity for BSA. It was also confirmed that hematoxy6n was bound to BSA stronger than braDlin. The association constants were decreased by the elevation of concentrations of brazilin and hematoxylin. It might be due to the complex formation of the probe and both compounds or the interaction between the probe-protein complex and both compounds. The bindings between both compounds and BSA were dependent on pH and ionic strength. It seems that electrostatic force as weD as hydrophobic force is involved in the binding of braD6n and bematoxylin to BSA.

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The Scaffolding Protein WAVE1 Associates with Kinesin 1 through the Tetratricopeptide Repeat (TPR) Domain of the Kinesin Light Chain (KLC) (Kinesin Light Chain (KLC)의 Tetratricopeptide Repeat (TPR) 도메인을 통한 Scaffold 단백질 WAVE1과 Kinesin 1의 결합)

  • Jang, Won Hee;Jeong, Young Joo;Urm, Sang-Hwa;Seog, Dae-Hyun
    • Journal of Life Science
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    • v.26 no.8
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    • pp.963-969
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    • 2016
  • Kinesin superfamily proteins (KIFs) are microtubule-dependent molecular motor proteins essential for the intracellular transport of organelles and protein complexes in cells. Kinesin 1 is a member of those KIFs that transport various cargoes, including organelles, synaptic vesicles, neurotransmitter receptors, cell signaling molecules, and mRNAs through interaction between its light chain subunit and the cargoes. Kinesin light chains (KLCs) are non-motor subunits that associate with the kinesin heavy chain (KHC) dimer. KLCs interact with many different binding proteins, but their particular binding proteins have not yet been fully identified. We used the yeast two-hybrid assay to identify proteins that interact with the tetratricopeptide repeat (TPR) domain of KLC1. We found an interaction between the TPR domain of KLC1 and Wiskott-Aldrich syndrome protein family member 1 (WAVE1), a member of the WASP/WAVE family involved in regulation of actin cytoskeleton. WAVE1 bound to the six TPR domain-containing regions of KLC1 and did not interact with KHCs (KIF5A, KIF5B, and KIF5C) in the yeast two-hybrid assay. The carboxyl (C)-terminal verprolin-cofilin-acidic (VCA) domain of WAVE1 is essential for interaction with KLC1. Also, other WAVE isoforms (WAVE2 and WAVE3) interacted with KLC1 in the yeast two-hybrid assay. When co-expressed in HEK-293T cells, WAVE1 co-localized with KLC1 and co-immunoprecipitated with KLC1 and KIF5B. These results suggest that kinesin 1 motor protein may transport WAVE complexes or WAVE-coated cargoes in cells.

The Effect of ${\pi}$ Bonds on the Calculated Dipole Moments for Tetrahedral and Square Planar [M(Ⅱ)$O_2S_2$] Type Complexes [M(II) = Co(II), Ni(II), Cu(II) and Zn(II)] (사면체 및 사각형 [M(II)$O_2S_2$]형태 착물의 쌍극자 모멘트에 대한 ${\pi}$결합의 영향 [M(II) = Co(II), Ni(II), Cu(II) 및 Zn])

  • Sangwoon Ahn;Jin Ha Park;Chang Jin Choi
    • Journal of the Korean Chemical Society
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    • v.26 no.5
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    • pp.265-273
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    • 1982
  • The effect of ${\pi}$ bonds on the calculated dipole moments for square planar and tetrahedral [M(II)$O_2S_2$]] type complexes has been investigated by two different approaches. One is the approximate molecular orbital method based on the assumption that the mixing coefficient CM of the valence basis sets for the central metal ion and the appropriate ligand orbitals is equal for all ${\sigma}$ and ${\pi}$ bonding molecular orbitals. The other is the more refined calculation based on the semiempirical LCAO-MO method. If ${\sigma}$ bonds only are assumed to be formed, the calculated dipole moments for square planar and tetrahedral complexes are lower than those of the experimental values. If the contribution of ${\pi}$ bonds to the calculated dipole moments are fully considered, the calculated dipole moments for both square planar and tetrahedral [M(II)$O_2S_2$]] type complexes are higher than the experimental values. However if ${\pi}$ bonds are assumed to be delocalzed, the calculated dipole moments for tetrahedral [M(II$O_2S_2$]] type complexes fall in the range of the experimental values, but those for square planar complexes deviate from the experimental values. These results suggest that [M(II)$O_2S_2$]] type complexes may have the tetrahedral structure in inert solvent solution. This structure is in agreement with the experimental one. The calculated dipole moments for tetrahedral [M(II)$O_2S_2$]] type complexes indicate that the contribution of ${\pi}$ bonds to the calculated dipole moments may not be neglected.

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The Changing Trace of Emotional state by Memory retrieval and Knowledge Reasoning process (기억회상과 지식추론에 따른 감정 상태 변화의 추이)

  • Shim, JeongYon
    • Journal of the Institute of Electronics and Information Engineers
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    • v.50 no.4
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    • pp.83-88
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    • 2013
  • Many studies adopting brain functions to the engineering systems have been made for recent years as the brain Science has developed. If we investigate the parts which take part in memorizing and emotional process, we can know that Hippocampus of memorizing center and Amygdala of Emotional center closely cooperate each other. Actually Knowledge effects on Emotion and Emotion effects on Knowledge. During the human decision making, emotional factor has much important effects on Decision making process. For implementing more delicate intelligent system, the knowledge base coupled to emotional factor should be designed. Accordingly in this paper starting from the idea of cooperating system between Hippocampus and Amygdala,, we design Knowledge Emotion Binding System and propose Emotional changing mechanism by Memory retrieval and knowledge reasoning process.