• Bulletin of the Korean Chemical Society
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• 제30권6호
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• pp.1325-1330
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• 2009

A general method has been developed for the solid phase synthesis of drug-like 7-aryl-benzo[b][1,4]oxazin-3(4H)- one derivatives 6. The method relies on a novel, microwave irradiation promoted cyclization reaction of the BOMBA resin bound, N-substituted-$\alpha$-(2-chloro-4-bromophenoxy)acetamide 3 that takes place via a Smiles rearrangement. The 7-bromobenzo[1,4]oxazine 4, produced in this process is converted to 7-aryloxazin analogs 5 by utilizing Suzuki coupling with various substituted arylboronic acids. Finally, the target 7-aryl-benzo[b][1,4]oxazin-3(4H)-ones 6 are liberated from the resin by treatment with 5% TFA. The progress of the reactions involved in this preparative route can be monitored by using ATR-FTIR spectroscopy on a single bead. The target compounds, obtained by using this five-step sequence, are produced in high yields and purities.

• Archives of Pharmacal Research
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• 제25권6호
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• pp.801-806
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• 2002

Cyclicpeptides are important targets in peptide synthesis because of their interesting biological properties. Constraining highly flexible linear peptides by cyclization is one of the mostly widely used approaches to define the bioactive conformation of peptides. Cyclic peptides often have increased receptor affinity and metabolic stability over their linear counterparts. We carried out virtual screening experiment via docking in order to understand the interaction between HLE-Human Leukocyte Elastase and ligand peptide and to identify the sequence that can be a target in various ligand peptides. We made cyclic peptides as a target base on Metlle-Phe sequence having affinity for ligand and receptor active site docking. There are three ways to cyclize certain sequences of amino acids such as Met-lie-Phe-Gly-Ile. First is head-to-tail cyclization method, linking between N-terminal and C-terminal. Second method utilizes amino acid side chain such as thiol functional group in Cys, making a thioether bond. The last one includes an application of resin-substituted amino acids in solid phase reaction. Among the three methods, solid phase reaction showed the greatest yield. Macrocyclization of Fmoc-Met-Ile-Phe-Gly-Ile-OBn after cleavage of Fmoc protection in solution phase was carried out to give macrocyclic compound 5 in about 7% yield. In the contrast with solution phase reaction, solid phase reaction for macrocyclization of Met-Ile-Phe-Gly-Ile-Asp-Tentagel in normal concentrated condition gave macrocyclic compound 7 in more than 35% yield.

• 상하수도학회지
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• 제32권6호
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• pp.559-572
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• 2018

The aim of this study was to evaluate pretreatment methods for 27 pharmaceuticals and personal care products (PPCPs) in various sewage samples using a modified quick, easy, cheap, effective, rugged, and safe (QuEChERS) and online solid-phase extraction with LC-MS/MS. Extraction efficiencies of PPCPs in the solid phase under different experimental conditions were evaluated, showing that the highest recoveries were obtained with the addition of sodium sulfate and ethylenediaminetetraacetic acid disodium salt dehydrate in acidified conditions. The recoveries of target compounds ranged from 91 to 117.2% for liquid samples and from 61.3 to 137.2% for solid samples, with a good precision. The methods under development were applied to sewage samples collected in two sewage treatment plants (STPs) to determine PPCPs in liquid and solid phases. Out of 27 PPCPs, more than 19 compounds were detected in liquid samples (i.e., influent and effluent) of two STPs, with concentration ranges of LOQ-33,152 ng/L in influents and LOQ-4,523 ng/L in effluents, respectively. In addition, some PPCPs such as acetylsalicylic acid, ibuprofen, and ofloxacin were detected at high concentrations in activated sludge as well as in excess sludge. This methodology was successfully applied to sewage samples for the determination of the target compounds in STPs.

• 한국추진공학회지
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• 제12권3호
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• pp.1-8
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• 2008

본 연구에서는 고출력 레이저에 의한 고에너지 물질의 점화 현상 모델을 제시하였다. 본 모델에서는 강판에 긴 조사 시간을 가진 펄스 레이저를 조사하여 발생한 어블레이션에 의한 열 확산을 고려하였고, 수 kW의 continuous 레이저를 폭약에 조사하여 폭약이 열에 의하여 점화하는 현상을 실험 결과와 비교를 통해 검증하였다. 여기서는 매우 짧은 조사 시간(femto- 혹은 pico-second)을 가진 펄스 레이저에서 나타나는 전자에 의한 효과는 무시 되었다. 본 연구에 사용된 폭약은 RDX, TATB 그리고 HMX이며, 제시한 모델은 실험 결과와 흡사한 결과를 도출하였다.

• Carbon letters
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• 제15권1호
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• pp.15-24
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• 2014

As a part of the electromagnetic spectrum, microwaves heat materials fast and efficiently via direct energy transfer, while conventional heating methods rely on conduction and convection. To date, the use of microwave heating in the research of carbon-based materials has been mainly limited to liquid solutions. However, more rapid and efficient heating is possible in electron-rich solid materials, because the target materials absorb the energy of microwaves effectively and exclusively. Carbon-based solid materials are suitable for microwave-heating due to the delocalized pi electrons from sp2-hybridized carbon networks. In this perspective review, research on the microwave heating of carbon-based solid materials is extensively investigated. This review includes basic theories of microwave heating, and applications in carbon nanotubes, graphite and other carbon-based materials. Finally, priority issues are discussed for the advanced use of microwave heating, which have been poorly understood so far: heating mechanism, temperature control, and penetration depth.

• The Korean Journal of Physiology and Pharmacology
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• 제27권3호
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• pp.241-256
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• 2023

Although chimeric antigen receptor T cell (CAR-T) is a promising immunotherapy in hematological malignancies, there remain many obstacles to CART cell therapy for solid tumors. Identifying appropriate tumor-associated antigens (TAAs) is especially critical for success. Using a bioinformatics approach, we identified common potential TAAs for CAR-T cell immunotherapy in solid tumors. We used the GEO database as a training dataset to find differentially expressed genes (DEGs) and verified candidates using the TCGA database, obtaining seven common DEGs (HM13, SDC1, MST1R, HMMR, MIF, CD24, and PDIA4). Then, we used MERAV to analyze the expression of six genes in normal tissues to determine the ideal target genes. Finally, we analyzed tumor microenvironment factors. The results of major microenvironment factor analyses showed that MDSCs, CXCL1, CXCL12, CXCL5, CCL2, CCL5, TGF- β, CTLA-4, and IFN-γ were significantly overexpressed in breast cancer. The expression of MST1R was positively correlated with TGF- β, CTLA-4, and IFN-γ. In lung adenocarcinoma, MDSCs, Tregs, CXCL12, CXCL5, CCL2, PD-L1, CTLA-4, and IFN-γ were significantly overexpressed in tumor tissues. The expression of MST1R was positively correlated with TGF- β, CTLA-4, and IFN-γ. In bladder cancer, CXCL12, CCL2, and CXCL5 were significantly overexpressed in tumor tissues. MST1R expression was positively correlated with TGF- β. Our results demonstrate that MST1R has the potential as a new target antigen for treating breast cancer, lung adenocarcinoma, and bladder cancer and may be used as a progression indicator for bladder cancer.

• Nuclear Medicine and Molecular Imaging
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• 제40권2호
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• pp.66-73
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• 2006

Monoclonal antibodies are designed to bind specifically to certain antigen, give therapeutic effect to the target and to be produced in large scale with homogeneity. The monoclonal antibodies conjugated with radionuclide can deliver therapeutic irradiation to the target, and showed successful results in certain malignancies, which is known as radioimmunotherapy. The target-to-background ratio depends on the antigen expression in the target and normal tissues, which is related to the therapeutic efficacy and toxicity in radioimmunotherapy. For the solid tumor beta-ray energy should be high, but lower beta energy is better for the hematological malignancies. I-l31 is widely used in thyroid cancer with low cost and high availability. Labeling monoclonal antibody with I-131 is relatively simple and reproducible. Some preclinical data for the I-131 labeled monoclonal antibodies including acute toxicity and efficacy are available from already published literatures in KIRAMS, physician sponsored clinical trial protocols using Rituximab, KFDA approved anti-CD20 chimeric monoclonal antibody and I-131 were approved by KFDA and currently are ongoing.

• 대한방사선치료학회지
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• 제24권1호
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• pp.31-37
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• 2012

목 적: Total Scalp의 방사선 치료 시 표면선량(surface dose)을 증가시키기 위해 조직보상체(bolus)를 사용한다. 이에 본 저자는 두피(scalp) 전체를 덮는 조직보상체로서 Bolx-II, paraffin wax, solid thermoplastic물질을 각각 적용한 Helmet bolus를 제작하여 유용성을 비교 평가해보고자 한다. 대상 및 방법: Rando 팬톰을 이용하여 두피 고정용구(mask)를 만든 후 전체 두피에 Bolx-II (Action Products, USA), paraffin wax (Densply, USA), solid thermoplastic 물질(Med-Tec, USA)을 0.5 cm 두께로 동일하게 적용한 Helmet bolus를 각각 제작 하였다. 각 Helmet bolus에 대한 물리적 특성을 평가하기 위해 전산화 단층촬영(computed tomography) (GE, Ultra Light Speed16)을 시행 후 방사선치료계획시스템(radiation therapy planning system) (Philips, Pinnacle)을 이용하여 최적의 치료 계획(radiationtherapy plan)을 세웠으며, 각 조직 보상체(bolus)에 대한 밀도 변화(density variation)화를 분석하였다. 선량 분포(dose distribution)평가(evaluation)를 위해 선량체적히스토그램(Dose-Volume Histogram) (DVH)을 이용해 임상표적체적(Clinical Target Volume) (CTV)에 대한 Dose-homogeneity index (DHI, $D_{90}/D_{10}$), Conformity index (CI, $V_{95}/TV$)를, 정상 뇌 조직(Normal brain tissue)에 있어$V_{20}$, $V_{30}$을 각각 구하여 비교 하였다. 또한 총 제작시간을 측정하여 제작과정에서의 효율성을 평가하였고, 열형광선량계 (Thermoluminescent Dosimeter)를 사용하여 실제 치료 시 각 두피의 표면선량을 확인 하였다. 결 과: Bolx-II, paraffin wax, solid thermoplastic 물질에 대한 밀도측정(density measurement) 결과 $0.952{\pm}0.13g/cm^3$, $0.842{\pm}0.17g/cm^3$, $0.908{\pm}0.24g/cm^3$로 Bolx-II의 밀도변화(density variation)가 가장 작았다. Bolx-II, paraffin wax, solid thermoplastic 물질을 적용한 각 Helmet bolus DHI는 0.89, 0.85, 0.77, CI는 0.86, 0.78, 0.74로 Bolx-II가 가장 우수 하였으며, 정상조직에 있어 뇌(braintissue)의 $V_{20}$은 11.50%, 10.80%, 10.07%, $V_{30}$은 7.62%, 7.40%, 7.31%로 나타났다. 제작 시 총 소요 시간은 30분, 120분, 90분 이였으며, Bolx-II를 적용한 Helmet bolus 제작과정이 가장 간단하였다. 열형광선량계(Thermoluminescent Dosimeter) 측정 결과세 Helmet bolus 모두 ${\pm}7%$ 이내의 선량오차를 보였다. 결 론: Total Scalp의 방사선치료 시 Bolx-II를 사용한 Helmet bolus의 적용은 CTV (Clinical Target Volume)에 대한 Homogeneity와 Conformity를 높여 줄 뿐만 아니라 제작시간 및 제작방법이 간단하여 임상 적용 시 유용하리라 생각된다.

• 한국자동차공학회논문집
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• 제22권5호
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• pp.73-83
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• 2014

CFD(computational fluid dynamics) model is developed to simulate direct injection of ammonia gas phase from ammonia transporting materials into the SCR catalyst in the exhaust pipe of the engine with solid SCR. Configurations of one-hole and four-hole nozzle, circumferential type, porous tube type, and the effect of mixer configurations which commonly used in liquid injection of AdBlue are considered for complex geometries. Mal-distribution index related to concentration of ammonia gas, flow uniformity index related to velocity distribution, and pressure drop related to flow resistance are compared for different configurations of complex geometries at the front section of SCR catalyst. These results are used to design the injection system of ammonia gas phase for solid SCR of target vehicle.

• 분석과학
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• 제17권5호
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• pp.388-392
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• 2004

genomics의 정보해석이나 신경전달물질 또는 약의 전달체계에서 아주 중요한 역할을 담당하는 막단백질의 구조연구는 기존의 X-ray나 용액상 핵자기공명분광법으로 수행하기 어려우나 지방질 이분자층이나 여러분자층에서 움직이지 않게 정렬시킨 단백질시료를 이용하여 특이하게 고안된 home-built solid-state NMR probe를 이용하면 구조를 연구할 수 있다. 이 논문에서는 박테리오파지인 pf1의 growth, 분리, 정제 및 pf1에서의 coat protein의 분리, 정제과정과 최종적으로 분리 정제된 pf1의 coat protein의 인산지방질 이분자층에서의 구조를 고체상 핵자기공명 분광법을 이용하여 연구하고자 한다.