• Biomolecules & Therapeutics
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• 제29권4호
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• pp.392-398
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• 2021

In this study, we determined the effect of 24 different synthetic 4-benzylpiperidine carboxamides on the reuptake of serotonin, norepinephrine, and dopamine (DA), and characterized their structure-activity relationship. The compounds with a two-carbon linker inhibited DA reuptake with much higher potency than those with a three-carbon linker. Among the aromatic ring substituents, biphenyl and diphenyl groups played a critical role in determining the selectivity of the 4-benzylpiperidine carboxamides toward the serotonin transporter (SERT) and dopamine transporter (DAT), respectively. Compounds with a 2-naphthyl ring were found to exhibit a higher degree of inhibition on the norepinephrine transporter (NET) and SERT than those with a 1-naphthyl ring. A docking simulation using a triple reuptake inhibitor 8k and a serotonin/norepinephrine reuptake inhibitor 7j showed that the regions spanning transmembrane domain (TM)1, TM3, and TM6 form the ligand binding pocket. The compound 8k bound tightly to the binding pocket of all three monoamine reuptake transporters; however, 7j showed poor docking with DAT. Co-expression of DAT with the dopamine D₂ receptor (D₂R) significantly inhibited DA-induced endocytosis of D₂R probably by reuptaking DA into the cells. Pretreatment of the cells with 8f, which is one of the compounds with good inhibitory activity on DAT, blocked DAT-induced inhibition of D₂R endocytosis. In summary, this study identified critical structural features contributing to the selectivity of a molecule for each of the monoamine transporters, critical residues on the compounds that bound to the transporters, and the functional role of a DA reuptake inhibitor in regulating D₂R function.

• Biomolecules & Therapeutics
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• 제30권2호
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• pp.191-202
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• 2022

Tetrazoles were designed and synthesized as potential inhibitors of triple monoamine neurotransmitters (dopamine, norepinephrine, serotonin) reuptake based on the functional and docking simulation of compound 6 which were performed in a previous study. The compound structure consisted of a tetrazole-linker (n)-piperidine/piperazine-spacer (m)-phenyl ring, with tetrazole attached to two phenyl rings (R1 and R2). Altering the carbon number in the linker (n) from 3 to 4 and in the spacer (m) from 0 to 1 increased the potency of serotonin reuptake inhibition. Depending on the nature of piperidine/piperazine, the substituents at R1 and R2 exerted various effects in determining their inhibitory effects on monoamine reuptake. Docking study showed that the selectivity of tetrazole for different transporters was determined based on multiple interactions with various residues on transporters, including hydrophobic residues on transmembrane domains 1, 3, 6, and 8. Co-expression of dopamine transporter, which lowers dopamine concentration in the biophase by uptaking dopamine into the cells, inhibited the dopamine-induced endoctytosis of dopamine D₂ receptor. When tested for compound 40 and 56, compound 40 which has more potent inhibitory activity on dopamine reuptake more strongly disinhibited the inhibitory activity of dopamine transporter on the endocytosis of dopamine D₂ receptor. Overall, we identified candidate inhibitors of triple monoamine neurotransmitter reuptake and provided a theoretical background for identifying such neurotransmitter modifiers for developing novel therapeutic agents of various neuropsychiatric disorders.

• Advances in materials Research
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• 제13권4호
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• pp.269-283
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• 2024

Biocompositesmade up of starch and jute fibres are biodegradable and environmentally friendly materials for sustainable development. In this study, corn starch has been separately modified with 15% pine rosin and 40% glutaraldehyde, and 30% glycerol is used as a plasticizer. The composites have been prepared for three different volume proportions of matrix and jute fibre such as 60:40, 70:30 and 80:20 by using a hot compression moulding machine. The effects of pine rosin and glutaraldehyde on mechanical properties have been studied. Pine rosin modified starch jute composites have shown higher tensile and flexural properties as compared with glutaraldehyde modified starch jute composite. The highest tensile strength and modulus are found at 60:40 matrix and jute fibre volume proportion of pine rosin modified starch jute composite which are 13.97 MPa and 782.94 MPa respectively. Similar trends were found in flexural strength and modulus for pine rosin modified starch jute composite having matrix to jute fibre proportion 60:40 which are 29.18 MPa and 1107.76 MPa respectively. But, in case of impact strength, glutaraldehyde modified starch jute composite having matrix to jute fibre proportion 80:20 have shown highest impact strength that is 59.05 KJ/m². Starch-jute composite with glutaraldehyde shows 33% more water absorbency as compared to composite having pine rosin as cross linker. Highest FTIR graph indicates that the number of -OH group is much lower in case of pine rosin modified starch than glutatraldehyde modified starch which indicates that bonds formed by pine rosin are much stronger than the bonds formed by glutaraldehyde. The surface morphology of the composite was influenced by pine rosin and glutaraldehyde which is shown in the SEM image.

• Journal of Microbiology and Biotechnology
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• 제17권8호
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• pp.1385-1389
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• 2007

5-Enolpyruvylshikimate-3-phosphate (EPSP) synthase catalyzes the formation of EPSP and inorganic phosphate from shikimate-3-phosphate (S3P) and phosphoenolpyruvate (PEP) in the biosynthesis of aromatic amino acids. To delineate the domain-specific function, we successfully isolated the discontinuous C-terminal domain (residues 1-21, linkers, 240-427) of EPSP synthase (427 residues) by site-directed mutagenesis. The engineered C-terminal domains containing no linker (CTD), or with gly-gly ($CTD^{GG}$) and gly-ser-ser-gly ($CTD^{GSSG}$) linkers were purified and characterized as having distinct native-like secondary and tertiary structures. However, isothermal titration calorimetry (ITC), $^{15}N-HSQC$,\;and\;^{31}P-NMR$ revealed that neither its substrate nor inhibitor binds the isolated domain. The isolated domain maintained structural integrity, but did not function as the half of the full-length protein.

• 통합자연과학논문집
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• 제9권2호
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• pp.86-93
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• 2016

The peptide sequences, GHK(Gly-His-Lys) and KTTKS(Lys-Thr-Thr-Lys-Ser), using a collagen stimulator recently were manipulated at N-terminal as a multifunctional peptide derivative with PEG(polyethyleneglycol) linker connected to gallic acid which presents anti-inflammatory activity. The multifunctional peptide derivatives were obtained in a normal peptide preparation method through SPPS(solid phase peptide synthesis) using Fmoc chemistry and a carboxyl group insertion reaction of PEG-3,4,5-triacetoxy benzoate by using potassium tert-butoxide and ethyl bromoacetate, which was separated by Sephadex DEAE. It gave a good compromise to a cosmetic application for cell cytotoxicity, anti-wrinkle, and anti-inflammation.

• Bulletin of the Korean Chemical Society
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• 제33권9호
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• pp.2991-2998
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• 2012

A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.

• 한국정보과학회 언어공학연구회:학술대회논문집(한글 및 한국어 정보처리)
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• 한국정보과학회언어공학연구회 1995년도 제7회 한글 및 한국어 정보처리 학술대회
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• pp.290-296
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• 1995

본고는 한국어에 나타나는 동사의 연쇄현상(serialization in verbals)에 있어서 단일절(mono-clausal)내에서 소위 복합동사(compound verb)라 불리는 일련의 동사들의 결합 현상을 고찰한다. 연결사(linker/connective)를 매개로 서로 결합하는 동사 연쇄증에는, 일반적으로 동사하나가 하나의 사건을 나타내는데 비해 2개 이상의 동사가 배열됨에도 동시에 일어나 묶여질 수 있는 하나의 사건(single event)을 지칭하는 동사부류가 존재하는데, 이를 통해 동사 결합간 긴밀성을 우선적으로 유추할 수 있고, 역으로 통사적 현상에 의해 그 긴밀성이 확인된다는 점에서 문장 접속의 통어적 구성과는 다른 문법범주 형성을 뒷받침하는 개념적 근거가 된다. 여기에서는, 이러한 연속동사구성(연쇄동사)에 있어 행위성/비대격성을 지니는 동사들간의 연쇄현상을 제약하는 여러 원인들을 검토하고 아울러 이들의 의미적 범주선택을 고려한 거르개로서의 생성여과 규약을 제안한다.

• 한국전기화학회:학술대회논문집
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• 한국전기화학회 2005년도 수소연료전지공동심포지움 2005논문집
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• pp.329-334
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• 2005

In order to find out rational design and synthetic strategies toward efficient hydrogen storage materials, we performed quantum mechanical calculations on a series of the Metal-Organic Frameworks (MOFs) containing functionalized organic linkers. Based on the shape of frontier orbitals and the electrostatic potential map of various MOFs from density functional theory calculations, it was found that the delocalization of electron and asymmetric polarization of the organic linker play an important role in the hydrogen storage capacity of Metal-Organic Frameworks. The prediction of the modeling study could be supported by the hydrogen adsorption experiments using MOF-5 and amine substituted MOF-5, which showed more enhanced hydrogen storage capacity of amine substituted MOF-5 compared with that of MOF-5.

• Bulletin of the Korean Chemical Society
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• 제32권4호
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• pp.1133-1137
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• 2011

Ordered array of gold nanoparticles (Au NPs) over ITO glass was investigated in terms of ITO pretreatment, particle size, and diamines with different chain length. Owing to the indium-tin-oxide (ITO) layer coated on the glass, the substrate surface has a limited number of hydroxyl groups which can produce functionalized amine groups for Au binding, which resulted in the loosely-packed array of Au NPs on the ITO surface. Diamine ligand as a molecular linker was introduced to enhance the lateral binding of adjacent Au NPs immobilized on the amine-functionalized ITO glass, consequently leading to the densely-packed array of Au NPs over the ITO substrate. The molecular bridging effect was strengthened with the increase of chain length of diamines: C-12 > C-8. The packing density of small Au NPs (< 40 nm) was significantly increased with the increase of C-8 diamine, but large Au NPs (> 60 nm) did not produce densely-packed array on the ITO glass even for the dosage of C-12 diamine.

• 한국전기전자재료학회논문지
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• 제26권6호
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• pp.478-481
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• 2013

Diameter controlled carbon nanotubes (CNTs) were grown using surface modified iron nano-particle catalysts with aminpropyltriethoxysilane (APS). Iron nano-particles were synthesized by thermal decomposition of iron pentacarbonyl-oleic acid complex. Subsequently, APS modification was done using the iron nano-particles synthesized. Agglomeration of the iron nano-particles during the CNT growth process was effectively prevented by the surface modification of nano-particles with the APS. APS plays as a linker material between Fe nano-particles and $SiO_2$ substrate resulting in blocking the migration of nano-particles. APS also formed siliceous material covering the iron nano-particles that prevented the agglomeration of iron nano-particles at the early stages of the CNT growth. Therefore we could obtain the diameter controlled CNTs by blocking agglomeration of the iron nano-particles.