• Title, Summary, Keyword: therapeutic target

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Lipid A as a Drug Target and Therapeutic Molecule

  • Joo, Sang Hoon
    • Biomolecules & Therapeutics
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    • v.23 no.6
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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.

Radioimmunotherapy (I): Development of Radioimmunoconjugates (방사면역치료(I): 방사면역접합체 개발)

  • Choi, Tae-Hyun;Lim, Sang-Moo
    • Nuclear Medicine and Molecular Imaging
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    • v.40 no.2
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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.

RNA Binding Protein as an Emerging Therapeutic Target for Cancer Prevention and Treatment

  • Hong, Suntaek
    • Journal of Cancer Prevention
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    • v.22 no.4
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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.

Histone Deactylase Inhibitors as Novel Target for Cancer, Diabetes, and Inflammation

  • Singh, Parul;Madhavan, Thirumurthy
    • Journal of the Chosun Natural Science
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    • v.6 no.1
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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.

A comprehensive review of the therapeutic and pharmacological effects of ginseng and ginsenosides in central nervous system

  • Kim, Hee Jin;Kim, Pitna;Shin, Chan Young
    • Journal of Ginseng Research
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    • v.37 no.1
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    • pp.8-29
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    • 2013
  • Ginseng is one of the most widely used herbal medicines in human. Central nervous system (CNS) diseases are most widely investigated diseases among all others in respect to the ginseng's therapeutic effects. These include Alzheimer's disease, Parkinson's disease, cerebral ischemia, depression, and many other neurological disorders including neurodevelopmental disorders. Not only the various types of diseases but also the diverse array of target pathways or molecules ginseng exerts its effect on. These range, for example, from neuroprotection to the regulation of synaptic plasticity and from regulation of neuroinflammatory processes to the regulation of neurotransmitter release, too many to mention. In general, ginseng and even a single compound of ginsenoside produce its effects on multiple sites of action, which make it an ideal candidate to develop multi-target drugs. This is most important in CNS diseases where multiple of etiological and pathological targets working together to regulate the final pathophysiology of diseases. In this review, we tried to provide comprehensive information on the pharmacological and therapeutic effects of ginseng and ginsenosides on neurodegenerative and other neurological diseases. Side by side comparison of the therapeutic effects in various neurological disorders may widen our understanding of the therapeutic potential of ginseng in CNS diseases and the possibility to develop not only symptomatic drugs but also disease modifying reagents based on ginseng.

P25: A hidden target for AD therapeutic.

  • Ha, Il-Ho
    • 한국약용작물학회:학술대회논문집
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    • pp.93-105
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    • 2006
  • P25/CDK5 phosphorylates BACE1. 2. P25 is a new target for AD therapeutics. 3. P25 inhibitors should block both $A{\beta}$ pathway and Tau pathway.

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OIP5 is a highly expressed potential therapeutic target for colorectal and gastric cancers

  • Chun, Ho-Kyung;Chung, Kyung-Sook;Kim, Hee-Cheol;Kang, Jung-Eun;Kang, Min-Ah;Kim, Jong-Tae;Choi, Eun-Hwa;Jung, Kyeong-Eun;Kim, Moon-Hee;Song, Eun-Young;Kim, Seon-Young;Won, Mi-Sun;Lee, Hee-Gu
    • BMB Reports
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    • v.43 no.5
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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.

Determination of Target Position with BRW Stereoatic Frame in non-orthogonal CT scans (비직교성 전산화단층촬영에서 뇌정위수술용 좌표계를 이용한 표적위치 결정)

  • Park, Tae-Jin;Kim, Ok-Bae;Son, Eun-Ik
    • Progress in Medical Physics
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    • v.3 no.1
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    • pp.53-62
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    • 1992
  • Stereotactic implantation of intracranial lesions, and the development of stereotactic convergent irradiation, radiosurgery, techniques have to obtain the accurate coordinates of the tumor locations and that of critical organ. Computed tomography(CT) provides relatively precise imformations of tumor localization and surround the normal organs for conventional radiotherapy. This CT image use to extend for stereotactic radiosurgery procedures. Since the convergent irradiation technique in linear accelerator requires the target center coincident with gantry isocenter or radosurgery frame, the target coordinates must be described in accurately. We used the BRW stereotactic system for describing the target position in CT images This algorithm provides the coordinate conversions for orthogonal or non-orthogonal CT scan image. In this experiments, the target positions have shown the small discripancy within :to.3mm uncertanty in several known target positions in the phantom through the provided programs and it compared to that of BRW stereotactic systems.

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Evaluated Absorbed Dose According to Prescribed Dose and Therapeutic Technique in Radiation Therapy (방사선치료 시 처방선량과 치료기법에 따른 흡수선량 평가)

  • Lee, Deuk-hee;Park, Eun-tae;Kim, Jung-hoon;Im, In-chul
    • Journal of the Korean Society of Radiology
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    • v.10 no.6
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    • pp.469-476
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    • 2016
  • In this study, evaluated absorbed dose of moving target using PLD according to prescribed dose and therapeutic technique. First, result of MCNPX when target was deviated from exposure field was reduced dose in proportion to distance. According to prescribed dose, absorbed dose of 3D CRT was better than IMRT in low dose and IMRT was more better in high dose. Absorbed dose of 3D CRT was highest according to therapeutic technique. Therefore, 3D CRT was technique of irradiated highest dose to moving target. But, considered protective effect of normal tissue and patient condition that therapeutic technique was selected to maximized treatment efficiency.