• Title/Summary/Keyword: pharmaceutical innovation

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FAP Inhibitors as Novel Small Molecules for Cancer Imaging using Radionuclide

  • Anvar Mirzaei;Jung-Joon Min;Dong-Yeon Kim
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.9 no.1
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    • pp.49-55
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    • 2023
  • Tumors are encircled by various non-cancerous cell types in the extracellular matrix, including fibroblasts, endothelial cells, immune cells, and cytokines. Fibroblasts are the most critical cells in the tumor stroma and play an important role in tumor development, which has been highlighted in some epithelial cancers. Many studies have shown a tight connection between cancerous cells and fibroblasts in the last decade. Regulatory factors secreted into the tumor environment by special fibroblast cells, cancer-associated fibroblasts (CAFs), play an important role in tumor and vessel development, metastasis, and therapy resistance. This review addresses the development of FAP inhibitors, emphasizing the first, second, and latest generations. First-generation inhibitors exhibit low selectivity and chemical stability, encouraging researchers to develop new scaffolds based on preclinical and clinical data. Second-generation enzymes such as UAMC-1110 demonstrated enhanced FAP binding and better selectivity. Targeted treatment and diagnostic imaging have become possible by further developing radionuclide-labeled fibroblast activation protein inhibitors (FAPIs). Although all three FAPIs (01, 02, and 04) showed excellent preclinical and clinical findings. The final optimization of these FAPI scaffolds resulted in FAPI-46 with the highest tumor-to-background ratio and better binding affinity.

Current Status of Bioinformatics on Bio-databases and it Tools (바이오데이터베이스와 도구를 활용한 바이오인포매틱스의 동향)

  • Im, Dal-Hyuk;Jeon, Sue-Kyoung;Park, Wan-Kyu;Lee, Young-Joo
    • Journal of Pharmaceutical Investigation
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    • v.34 no.1
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    • pp.73-79
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    • 2004
  • The union of information-technology and biology presents great possibilities to both applications of bio-information and development of science and technology. Also, meaningful analysis of bio-information brings about a new innovation in the field of bio-market with the advent and growth of bioinformatics. Hence, bioinformatics is the most import aspect for establishing a science-technology-oriented society in the $21^{st}$ century. This article provides trends in current state of bioinformatics. Technological development of bioinformatics for the rapid growth of bio-industry means that using bioinformatics, a biologist can process and store enormous amount of data such as current Human Genome Project and future data in the field of biology. We have manly looked at the tends of bio-information, databases and mining tools that are generally used, and strategies and directions for the future.

A Study on the Relationship between International Patenting and Export Performance (국제 특허 활동과 수출 성과 간의 관계에 대한 연구)

  • Mun, Hee-Jin;Choe, Soon-Kyoo
    • Korea Trade Review
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    • v.42 no.3
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    • pp.49-74
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    • 2017
  • Drawing on the organizational learning theory, we argue that international patenting allows firms to assess the potential value of their innovation in host countries and find out latent local competitors. The information obtained from international patenting enables firms to make refined innovations that facilitate export performance. However, structural inertia and old knowledge can impede learning from international patenting. Thus, we expect larger firms and older firms to display greater reluctance to use the knowledge obtained from international patenting. Our empirical analysis of Korean pharmaceutical companies from 1998 to 2010 shows that international patent application increases export intensity but firm size and age weaken the positive effect of international patenting on export performance.

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Newly identified maltol derivatives in Korean Red Ginseng and their biological influence as antioxidant and anti-inflammatory agents

  • Jeong Hun Cho;Myoung Chong Song;Yonghee Lee;Seung-Taek Noh;Dae-Ok Kim;Chan-Su Rha
    • Journal of Ginseng Research
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    • v.47 no.4
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    • pp.593-603
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    • 2023
  • Background: Korean Red Ginseng is a major source of bioactive substances such as ginsenosides. Efficacy of red ginseng extract (RGE), which contains not only saponins but also various non-saponins, has long been studied. In the water-soluble component-rich fraction of RGE (WS), a byproduct generated in the process of extracting saponins from the RGE, we identified previously unidentified molecules and confirmed their efficacy. Methods: The RGE was prepared and used to produce WS, whose components were isolated sequentially according to their water affinity. The new compounds from WS were fractionized and structurally analyzed using nuclear magnetic resonance spectroscopy. Physiological applicability was evaluated by verifying the antioxidant and anti-inflammatory efficacies of these compounds in vitro. Results: High-performance liquid chromatography confirmed that the obtained WS comprised 11 phenolic acid and flavonoid substances. Among four major compounds from fractions 1-4 (F1-4) of WS, two compounds from F3 and F4 were newly identified in red ginseng. The analysis results show that these compound molecules are member of the maltol-structure-based glucopyranose series, and F1 and F4 are particularly effective for decreasing oxidative stress levels and inhibiting nitric oxide secretion, interleukin (IL)-1β and IL-6, and tumor necrosis factor-α. Conclusion: Our findings suggest that a few newly identified maltol derivatives, such as red ginseng-derived non-saponin in the WS, exhibit antioxidant and anti-inflammatory effects, making them viable candidates for application to pharmaceutical, cosmetic, and functional food materials.

An Analysis of the Productivity Changes of Korean Pharmaceutical Industry Using Bootstrapped Malmquist Index (Bootstrapped Malmquist 지수를 이용한 국내 의약품산업의 생산성 변화 요인 분석에 관한 연구)

  • So, Soon-Hu
    • Management & Information Systems Review
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    • v.35 no.4
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    • pp.141-153
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    • 2016
  • This study estimates the productivity change of pharmaceutical industry and decompose the change into technical efficiency change and technological change to explore ways to improve the productive efficiency. Unlike most previous studies, this study employs the non-radial and non-oriented slacks-based Malmquist productivity index which can deals directly with the input excesses and output shortfalls. In addition a smoothed bootstrap method is applied to estimate statistical confidence intervals for the Malmquist Index and its components. For the empirical analysis a balanced panel data set is constructed covering ten years over the period from 2005 to 2014. The input variables used in this study are number of workers, tangible assets and major production cost. The gross production is selected as a main output variable. The empirical results suggest that the productivity of pharmaceutical industry has decreased due mainly to decline in the technological progress rather than improvements in technical efficiency. An analysis result shows that the scale efficiency outweighs the pure efficiency in determining the technical efficiency of pharmaceutical industry. Therefore, in order to enhance the competitiveness of domestic pharmaceutical industry, it is important to continue supporting policies to promote the technology innovation capability through efficient R&D investment and industry reform strategy.

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Steroidal Saponins from Paris polyphylla Suppress Adhesion, Migration and Invasion of Human Lung Cancer A549 Cells Via Down-Regulating MMP-2 and MMP-9

  • He, Hao;Zheng, Lei;Sun, Yan-Ping;Zhang, Guang-Wei;Yue, Zheng-Gang
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.24
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    • pp.10911-10916
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    • 2015
  • Background: Tumor metastases are the main reasons for oncotherapy failure. Paris polyphylla (Chinese name: Chonglou) has traditionally been used for its anti-cancer actions. In this article, we focus on the regulation of human lung cancer A549 cell metastases and invasion by Paris polyphylla steroidal saponins (PPSS). Materials and Methods: Cell viability was evaluated in A549 cells by MTT assay. Effects of PPSS on invasion and migration were investigated by wound-healing and matrigel invasion chamber assays. Adhesion to type IV collagen and laminin was evaluated by MTT assay. Expression and protease activity of two matrix metalloproteinases (MMPs), MMP-2 and MMP-9, were analyzed by Western blotting and gelatin zymography, respectively. Results: PPSS exerted growth inhibitory effects on A549 cells, and effectively inhibited A549 cell adhesion, migration and invasion in a concentration-dependent manner. Western blotting and gelatin zymography analysis revealed that PPSS inhibited the expression and secretion of MMP-2 and MMP-9 in A549 cells. Conclusions: PPSS has the potential to suppress the migration, adhesion and invasion of A549 cells. PPSS could be a potential candidate for interventions against lung cancer metastases.

Repeated Neonatal Propofol Administration Induces Sex-Dependent Long-Term Impairments on Spatial and Recognition Memory in Rats

  • Gonzales, Edson Luck T.;Yang, Sung Min;Choi, Chang Soon;Mabunga, Darine Froy N.;Kim, Hee Jin;Cheong, Jae Hoon;Ryu, Jong Hoon;Koo, Bon-Nyeo;Shin, Chan Young
    • Biomolecules & Therapeutics
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    • v.23 no.3
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    • pp.251-260
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    • 2015
  • Propofol is an anesthetic agent that gained wide use because of its fast induction of anesthesia and rapid recovery post-anesthesia. However, previous studies have reported immediate neurodegeneration and long-term impairment in spatial learning and memory from repeated neonatal propofol administration in animals. Yet, none of those studies has explored the sex-specific long-term physical changes and behavioral alterations such as social (sociability and social preference), emotional (anxiety), and other cognitive functions (spatial working, recognition, and avoidance memory) after neonatal propofol treatment. Seven-day-old Wistar-Kyoto (WKY) rats underwent repeated daily intraperitoneal injections of propofol or normal saline for 7 days. Starting fourth week of age and onwards, rats were subjected to behavior tests including open-field, elevated-plus-maze, Y-maze, 3-chamber social interaction, novel-object-recognition, passive-avoidance, and rotarod. Rats were sacrificed at 9 weeks and hippocampal protein expressions were analyzed by Western blot. Results revealed long-term body weight gain alterations in the growing rats and sex-specific impairments in spatial (female) and recognition (male) learning and memory paradigms. A markedly decreased expression of hippocampal NMDA receptor GluN1 subunit in female- and increased expression of AMPA GluR1 subunit protein expression in male rats were also found. Other aspects of behaviors such as locomotor activity and coordination, anxiety, sociability, social preference and avoidance learning and memory were not generally affected. These results suggest that neonatal repeated propofol administration disrupts normal growth and some aspects of neurodevelopment in rats in a sex-specific manner.

Oxidative stress impairs the meat quality of broiler by damaging mitochondrial function, affecting calcium metabolism and leading to ferroptosis

  • Chen, Zuodong;Xing, Tong;Li, Jiaolong;Zhang, Lin;Jiang, Yun;Gao, Feng
    • Animal Bioscience
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    • v.35 no.10
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    • pp.1616-1627
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    • 2022
  • Objective: This work was conducted to investigate the effects of oxidative stress on meat quality, mitochondrial function, calcium metabolism and ferroptosis of broilers. Methods: In this study, a total of 144 one-day-old male Ross 308 chicks were divided into 3 groups (control group, saline group, and hydrogen peroxide [H2O2] group) with 6 replicates of 8 broilers each. The study lasted for 42 d. The broilers in the saline and H2O2 groups were intraperitoneally injected with 0.75% saline and 10.0% H2O2 on the 16th and 37th day of the experimental period respectively, the injection volumes were 1.0 mL/kg of broiler body weight. On the 42nd day of the experimental period, two chicks were randomly selected from each cage, a total of thirty-six chicks were stunned by electric shock and slaughtered to collect breast muscle samples. Results: The H2O2 exposure reduced pH value, increased drip loss and shear force of breast meat (p<0.05), impaired the ultrastructure and function of mitochondria. The H2O2 exposure damaged the antioxidant system in mitochondria, excessive reactive oxygen species carbonylation modified calcium channels on mitochondria, which impaired the activities of key enzymes on calcium channel, resulted in the increased calcium concentration in cytoplasm and mitochondria (p<0.05). In addition, the H2O2 exposure increased the iron content and lipid peroxidation (p<0.05), which induced ferroptosis. Conclusion: Oxidative stress could impair meat quality by causing mitochondrial dysfunction, resulting in calcium metabolism disorder and ferroptosis.

Antibody Engineering for the Development of Therapeutic Antibodies

  • Kim, Sang Jick;Park, Youngwoo;Hong, Hyo Jeong
    • Molecules and Cells
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    • v.20 no.1
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    • pp.17-29
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    • 2005
  • Therapeutic antibodies represent one of the fastest growing areas of the pharmaceutical industry. There are currently 19 monoclonal antibodies in the market that have been approved by the FDA and over 150 in clinical developments. Driven by innovation and technological developments, therapeutic antibodies are the second largest biopharmaceutical product category after vaccines. Antibodies have been engineered by a variety of methods to suit a particular therapeutic use. This review describes the structural and functional characteristics of antibody and the antibody engineering for the generation and optimization of therapeutic antibodies.

A Study on the Effects of Forms of R&D Strategy on Corporate Financial Performance (R&D 전략의 형태가 기업 재무성과에 미치는 영향에 관한 연구)

  • Mun, Hee-Jin;Lee, Joo-Sung
    • Journal of the Korean Operations Research and Management Science Society
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    • v.35 no.1
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    • pp.67-81
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    • 2010
  • In Schumpeterian competition, superior profit arises from successful innovation created by firm's R&D strategy. Such R&D strategy diverges as time passes. This study examines empirically the effects of diverged forms of R&D strategy such as technological assets, technological diversity, and technological similarity on firm performance in Korean pharmaceutical industry. With the financial and patent data of 96 firms for 14 years from 1994 to 2007, we measured variables. And then we performed panel analysis with 3 years lag between dependent variable and other variables. The result shows that firm performance increases as technological asset and technological diversification increase. But technological similarity positively affects on firm performance in opposition to our hypothesis. We interpret and discuss these results and highlight the theoretical and practical implications of our findings.