• Journal of Digital Convergence
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• v.17 no.1
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• pp.443-447
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• 2019

Aryl hydrocarbon receptor (AhR) is the master regulator of xenobiotics metabolizing enzymes (XMEs). AhR is activated by aryl hydrocarbons upon binding then goes into the cell nucleus and acts as a transcription factor. Despite the role of AhR in human physiology has been investigated for a long while, it is yet to be understood mainly due to the lack of appropriate chemical agents. Furthermore, it has been reported that AhR is related to a wide range of pathogenesis. In addition, recent studies suggest that the study on the development of AhR antagonist may provide a valid therapeutic agent. Some known antagonists in current use are partially agonistic whereas a pure antagonist is still absent. In this study, two phenyl-ring structures of phenyldiazenylphenylpicolinamide has been modified into various structures and evaluated its impact on the AhR antagonistic activity to elucidate the structure-activity relationship.

• Journal of Life Science
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• v.28 no.4
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• pp.488-495
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• 2018

The p53 gene plays a critical role in the transcriptional regulation of cellular response to stress, DNA damage, hypoxia, and tumor development. Keeping in mind the recently discovered manifold physiological functions of p53, its involvement in the regulation of cancer is not surprising. In about 50% of all human cancers, inactivation of p53's protein function occurs either through mutations in the gene itself or defects in the mechanisms that activate it. This disorder plays a crucial role in tumor evolution by allowing the evasion of a p53-dependent response. Many recent studies have focused on directly targeting p53 mutants by identifying selective, small molecular compounds to deplete them or to restore their tumor-suppressive function. These small molecules should effectively regulate various interactions while maintaining good drug-like properties. Among them, the discovery of the key p53-negative regulator, MDM2, has led to the design of new small molecule inhibitors that block the interaction between p53 and MDM2. Some of these small molecule compounds have now moved from proof-of-concept studies into clinical trials, with prospects for further, more personalized anti-carcinogenic medicines. Here, we review the structural and functional consequences of wild type and mutant p53 as well as the development of therapeutic agents that directly target this gene, and compounds that inhibit the interaction between it and MDM2.

• Journal of Life Science
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• v.33 no.3
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• pp.287-294
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• 2023

Healthy adipose tissue is critical for preventing obesity by maintaining metabolic homeostasis. Adipose tissue plays an important role in energy homeostasis through glucose and lipid metabolism. Depending on nutritional status, adipose tissue expands to store lipids or can be consumed by lipolysis. The role of adipose tissue as an endocrine organ is emerging, and many studies have reported that there are various adipose tissue hormones that communicate with other organs and tissues through metabolic signaling. For example, leptin, a representative peptide hormone secreted from adipose tissues (adipokine), circulates and targets the central nervous system of the brain for appetite regression. Furthermore, adipocytes secrete inflammatory cytokines to target immune cells in adipose tissues. Not surprisingly, adipocytes can secrete fatty acid-derived hormones (lipokine) that bind to their specific receptors for paracrine and endocrine action. To understand organ crosstalk by adipose tissue hor- mones, specific metabolic signaling in adipocytes and other communicating cells should be defined. The dysfunction of metabolic signaling in adipocytes occurs in unhealthy adipose tissue in overweight and obese conditions. Therapy targeting novel adipose metabolic signaling could potentially lead to the development of an effective anti-obesity drug. This review summarizes the latest updates on adipose tissue hormone and metabolic signaling in terms of obesity and metabolic diseases.

• Childhood Kidney Diseases
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• v.15 no.1
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• pp.14-21
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• 2011

Although left Left ventricular hypertrophy (LVH) is not only an adaptive response of the heart to increased cardiac workload in hypertension, it surelybut also is the most potent risk factor of overt cardiovascular complications such as coronary heart disease, heart failure, arrhythmia and stroke in the hypertensive population. Also it has become generally accepted that subclinical cardiovascular disease begins in childhood and LVH is the most readily assessed marker for that. As LVH can be seen in children and adolescents with even mild blood pressure elevation with the reported prevalence of 10 to 47%, aggressive antihypertensive treatment is critical in preventing the development of hypertensive heart disease in that those cases.

• Journal of Pharmaceutical Investigation
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• v.13 no.4
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• pp.153-172
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• 1983

The use of carrier systems for the delivery of drugs to areas in the body in need of pharmacological intervention is now the subject of intense research in many laboratories. Because of its obvious advantages (e.g. protection of drugs from hostile environments, facilitated target penetration and avoidance of side effects), drug delivery is expected to ease the pressure and expense of new drug development by making better use of drugs in existence. Generally, carrier-mediated delivery has been envisaged either as direct transport of drugs to a biological target by a carrier that will associate with it selectively, or as release of drugs from a carrier circulating in the blood or immobilized in tissues, at rates compatible with optimal action. One system that has attracted considerable attention is the use of liposomes as carriers of pharmacologically active agents. 154 references were reviewed with special emphasis on the targeting of drugs by use of liposomes in this respect. Recent advances in the other carrier systems and in methods for the preparation of liposomes were also reviewed briefly.

• Nuclear Medicine and Molecular Imaging
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• v.42 no.5
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• pp.337-346
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• 2008

Applications of nanotechnology in the medical field have provided the fundamentals of tremendous improvement in precise diagnosis and customized therapy. Recent advances in nanomedicine have led to establish a new concept of theragnosis, which utilizes nanomedicines as a therapeutic and diagnostic tool at the same time. The development of high affinity nanoparticles with large surface area and functional groups multiplies diagnostic and therapeutic capacities. Considering the specific conditions related to the disease of individual patient, customized therapy requires the identification of disease target at the cellular and molecular level for reducing side effects and enhancing therapeutic efficiency. Well-designed nanoparticles can minimize unnecessary exposure of cytotoxic drugs and maximize targeted localization of administrated drugs. This review will focus on major pharmaceutical nanomaterials and nanoparticles as key components of designing and surface engineering for targeted theragnostic drug development.

• Proceedings of the Korean Information Science Society Conference
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• 2007.10b
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• pp.17-21
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• 2007

Drug discovery is a long process with a low rate of successful new therapeutic discovery regardless of the advances in information technologies. Identification of candidate proteins is an essential step for the drug discovery and it usually requires considerable time and efforts in the drug discovery. The drug discovery is not a logical, but a fortuitous process. Nevertheless, considerable amount of information on drugs are accumulated in UniProt, NCBI, or DrugBank. As a result, it has become possible to try to devise new computational methods classifying drug target candidates extracting the common features of known drug target proteins. In this paper, we devise a method for drug target protein classification by using weighted feature summation and Support Vector Machine. According to our evaluation, the method is revealed to show moderate accuracy $85{\sim}90%$. This indicates that if the devised method is used appropriately, it can contribute in reducing the time and cost of the drug discovery process, particularly in identifying new drug target proteins.

• Journal of Digestive Cancer Research
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• v.6 no.1
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• pp.16-24
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• 2018

Gastric cancer is not a single, uniform disease, but rather heterogeneous in nature. It is generally not possible to cure patients with inoperable advanced or metastatic stomach cancer. In the absence of chemotherapy, the median survival time is 3 to 6 months. Therefore, several studies have confirmed the superiority of chemotherapy to the best supportive treatment, in terms of improving the quality of life and prolonging life. Various chemotherapies have been used in the past to treat advanced gastric cancer. Recently, various target therapies and immunotherapy have been introduced. However, compared to other malignancies, the quality of life and life expectancy remain relatively poor in patients with gastric cancer. We expect to overcome these difficulties in the future, with better elucidation of the molecular biology of gastric cancer.

• Journal of Food Hygiene and Safety
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• v.36 no.5
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• pp.363-375
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• 2021

Trends in the developing era to discover and design peptide-based treatments throughout an epidemic infection scenario such as COVID-19 could progress into a more efficient and low-cost therapeutic environment. However, the weakening of proteolysis is one downside of natural peptide drugs. But, peptidomimetics may help resolve this issue. In this review, peptide and peptide-based drug discovery were summarized to target one key entry mechanism of severe coronavirus pulmonary emboli syndrome (SARS-CoV-2), which encompasses the association of the host angiotensin-converting enzyme-2 (ACE2) receptor and viral spike (S) protein. Furthermore, the benefits of proteins, peptides and other possible actions that have been studied for COVID-19 through new peptide-based treatments are discussed in the review. Lastly, an overview of the peptide-based drug therapy environment is comprised of an evolutionary viewpoint, structural properties, operational thresholds, and an explanation of the therapeutic area.

• Journal of Life Science
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• v.33 no.9
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• pp.754-765
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• 2023

Exosomes are a type of extracellular vesicle containing proteins and messenger and microRNAs; they are secreted by all cell types. Once released, exosomes are selectively taken up by other cells adjacent or at a distance, releasing their contents and reprogramming the target cells. Since exosomes are natural vesicles produced by cells as small sizes, it is generally accepted that exosomes have a non-toxic nature and non-immunogenic behaviors. Recently, exosomes have elicited scientific attention as drug delivery vehicles to the central nervous system. The central nervous system has a blood-brain barrier that makes it difficult for drugs to penetrate. Thus, the blood-brain barrier has been a major obstacle to the development of drugs for treating neurodegenerative diseases. However, accumulating evidence suggests that exosomes can cross the blood-brain barrier primarily through transcytosis. Consequently, exosomes are expected to become a new delivery vehicle that can cross the blood-brain barrier and deliver drugs into the brain parenchyma. In addition, since different types of exosomes are secreted depending on the cell type and disease state, exosomes can also be utilized as biomarkers for the diagnosis of diseases in the central nervous system. In this review, we summarized recent research trends on exosomes, including clinical trials as biomarkers and treatment options for diseases in the central nervous system.