• Biomolecules & Therapeutics
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• 제23권6호
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• pp.510-516
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• 2015

In this review, lipid A, from its discovery to recent findings, is presented as a drug target and therapeutic molecule. First, the biosynthetic pathway for lipid A, the Raetz pathway, serves as a good drug target for antibiotic development. Several assay methods used to screen for inhibitors of lipid A synthesis will be presented, and some of the promising lead compounds will be described. Second, utilization of lipid A biosynthetic pathways by various bacterial species can generate modified lipid A molecules with therapeutic value.

• 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.

• BMB Reports
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• 제57권7호
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• pp.324-329
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• 2024

The aim of the present study is to provide a rational background for silencing the V-set and transmembrane domain containing 2 like (VSTM2L) in consort with recognising soluble VSTM2L against cholangiocarcinoma. A therapeutic target against cholangiocarcinoma was selected using iterative patient partitioning (IPP) calculation, and it was verified by in vitro and in silico analyses. VSTM2L was selected as a potential therapeutic target against cholangiocarcinoma. Silencing the VSTM2L expression significantly attenuated the viability and survival of cholangiocarcinoma cells through blockade of the intracellular signalling pathway. In silico analysis showed that VSTM2L affected the positive regulation of cell growth in cholangiocarcinoma. Liptak's z value revealed that the expression of VSTM2L worsened the prognosis of cholangiocarcinoma patients. In addition, soluble VSTM2L was significantly detected in the whole blood of cholangiocarcinoma patients compared with that of healthy donors. Our report reveals that VSTM2L might be the potential therapeutic target and a soluble prognostic biomarker against cholangiocarcinoma.

• Journal of Cancer Prevention
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• 제22권4호
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• pp.203-210
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• 2017

After transcription, RNAs are always associated with RNA binding proteins (RBPs) to perform biological activities. RBPs can interact with target RNAs in sequence- and structure-dependent manner through their unique RNA binding domains. In development and progression of carcinogenesis, RBPs are aberrantly dysregulated in many human cancers with various mechanisms, such as genetic alteration, epigenetic change, noncoding RNA-mediated regulation, and post-translational modifications. Upon deregulation in cancers, RBPs influence every step in the development and progression of cancer, including sustained cell proliferation, evasion of apoptosis, avoiding immune surveillance, inducing angiogenesis, and activating metastasis. To develop therapeutic strategies targeting RBPs, RNA interference-based oligonucleotides or small molecule inhibitors have been screened based on reduced RBP-RNA interaction and changed level of target RNAs. Identification of binding RNAs with high-throughput techniques and integral analysis of multiple datasets will help us develop new therapeutic drugs or prognostic biomarkers for human cancers.

• 한국의학물리학회:학술대회논문집
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• 한국의학물리학회 2006년도 제33회 추계학술대회 발표논문집
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• pp.60-60
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• 2006

• Nuclear Medicine and Molecular Imaging
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• 제40권2호
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• pp.58-65
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• 2006

Since the development of sophisticated molecular carriers such as octereotides for peptide receptor targeting and monoclonal antibodies against various antigens associated with specific tumor types, radionuclide therapy (RNT) employing open sources of therapeutic agents is promising modality for treatment of tumors. furthermore, the emerging of new therapeutic regimes and new approaches for tumor treatment using radionuclide are anticipated in near future. In targeted radiotherapy using peptides and other receptor based tarrier molecules, the use of radionuclide with high specific activity in formulating the radiopharmaceutical is essential in order to deliver sufficient number of radionuclides to the target site without saturating the target. In order to develop effective radiopharmaceuticals for therapeutic applications, it is crucial to carefully consider the choice of appropriate radionuclides as well as the tarrier moiety with suitable pharmacokinetic properties that could result in good in vivo localization and desired excretion. Up to date, only a limited number of radionuclides have been applied in radiopharmaceutical development due to the constraints in compliance with their physical half-life, decay characteristics, cost and availability in therapeutic applications. In this review article, we intend to provide with the improved understanding of the factors of importance of appropriate radionuclide for therapy with respect to their physical properties and therapeutic applications.

• 통합자연과학논문집
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• 제6권1호
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• pp.57-63
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• 2013

Histone deacetylase (HDACs) is an enzyme family that deacetylates histones and non-histones protein. Availability of crystal structure of HDAC8 has been a boosting factor to generate target based inhibitors. Hydroxamic class is the most studied one to generate potent inhibitors. HDAC class I and class II enzymes are emerging as a therapeutic target for cancer, diabetes, inflammation and other diseases. DNA methylation and histone modification are epigenetic mechanism, is important for the regulation of cellular functions. HDACs enzymes play essential role in gene transcription to regulate cell proliferation, migration and death. The aim of this article is to provide a comprehensive overview about structure and function of HDACs enzymes, histone deacetylase inhibitors (HDACi) and HDACs enzymes as a therapeutic target for cancer, inflammation and diabetes.

• 한국의학물리학회지:의학물리
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• 제3권1호
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• pp.53-62
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• 1992

최근 두개부 종양의 방사성물질의 자입과 방사선입체조사에 의한 뇌수술이 개발되어 의료계 에 많은 관심을 끌고 있다. 또한 방사선수술등은 비관혈적인 체외조사이므로 뇌정위수술용 좌표계의 전산화단층촬영을 이용한 표적중심결정이 매우 중요하다. 현재 알려진 방법은 뇌정위수술용좌표계의 전산화단층찰영에 대한 직교성하에서 비교적 정확하게 표적의 위치를 결정하게 되나, 임상현장에서 직교성유지는 실제 어려운 실정이다. 이에 필자들은 임의의 비직교성 스켄하에서 정확한 표적좌표를 얻기위한 알고리즘을 사용하였으며, 표적오차는 평균 0.02$\pm$0.3mm를 보였다.

• BMB Reports
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• 제43권5호
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• pp.349-354
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• 2010

Previously, we reported that overexpression of Opa (Neisseria gonorrhoeae opacity-associated)-interacting protein 5 (OIP5) caused multi-septa formation and growth defects, both of which are considered cancer-related phenotypes. To evaluate OIP5 as a possible cancer therapeutic target, we examined its expression level in 66 colorectal cancer patients. OIP5 was upregulated about 3.7-fold in tumors and over 2-fold in 58 out of 66 colorectal cancer patients. Knockdown of OIP5 expression by small interfering RNA specific to OIP5 (siOIP5) resulted in growth inhibition of colorectal and gastric cancer cell lines. Growth inhibition of SNU638 by siOIP5 caused an increase in sub-G1 DNA content, as measured by flow cytometry, as well as an apoptotic gene expression profile. These results indicate that knockdown of OIP5 may induce apoptosis in cancer cells. Therefore, we suggest that OIP5 might be a potential cancer therapeutic target, although the mechanisms of OIP5-induced carcinogenesis should be elucidated.

• 한국방사선학회논문지
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• 제10권6호
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• pp.469-476
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• 2016

본 논문에서는 움직이는 타깃을 대상으로 처방선량과 치료기법에 따른 흡수선량을 유리선량계를 이용하여 평가하였다. 타깃의 움직임에 따라 조사야에서 벗어나는 정도에 따른 선량을 MCNPX를 이용하여 모의모사하였으며 그 결과 조사야에서 이격하는 거리에 비례하여 감소하는 것으로 나타났다. 처방선량에 따른 흡수선량의 결과는 3D CRT의 경우 저선량에서 IMRT보다 흡수선량이 높은 것으로 나타났으며, 대선량에서는 IMRT가 더 높은 비율을 보였다. 치료기법에 따른 결과는 3D CRT가 가장 우수한 것으로 나타났으며, IMRT의 sliding window방식이 가장 낮은 것으로 나타났다. 본 연구를 통하여 3D CRT가 움직이는 타깃에 가장 높은 선량을 조사할 수 있는 기법으로 평가되었다. 하지만 정상조직의 보호효과와 환자의 상태 등을 고려한 적절한 치료기법의 선택으로 치료효과를 높일 수 있는 노력이 필요할 것이다.