• Title/Summary/Keyword: peptide inhibitor

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Overexpression of GFP-AFP Chimera Protein using Recombinant Escherichia coli and Analysis of Anti-freezing Characteristics (재조합 대장균을 이용한 GFP-AFP Chimera 단백질 과량발현 및 특성 파악연구)

  • Ko, Ji-Seun;Hong, Soon Ho
    • KSBB Journal
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    • v.28 no.5
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    • pp.310-314
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    • 2013
  • Antifreeze peptide from Myoxocephalus octodecemspinosus was overexpressed and purified in Escherichia coli. Green fluorescence protein-AFP chimera was constructed by integrating gfp and afp genes. Produced GFP-AFP chimera protein was purified using polyhistidine tag which was inserted at C-terminus. By addition of GFP-AFP chimera protein, freezing point of elution buffer was decreased from $-13^{\circ}C$ to $-20^{\circ}C$. This result suggested that GFP-AFP chimera can be considered as a potential candidate of novel inhibitor for gas hydrates.

Morbidly Obese Patients Treated Obesity and Metabolic Diseases Using Naltrexone/Bupropion Extended Release and Other Drugs of Various Mechanisms (날트렉손/부프로피온 복합제 및 여러 기전의 약물을 이용하여 비만과 동반 대사질환을 치료한 고도비만환자)

  • Cho, Soo Hyun
    • Archives of Obesity and Metabolism
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    • v.1 no.2
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    • pp.83-88
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    • 2022
  • Obesity increases the risk of developing metabolic diseases such as hypertension, type 2 diabetes, hyperlipidemia, and cardiovascular diseases, as well as some cancers. To prevent the occurrence of these diseases and death, it is essential to manage obesity. Though there are several treatments for obesity, lifestyle interventions, such as diet and exercise, and drug therapy are most widely used in clinical practice. Among the anti-obesity drugs available, the weight loss effect of naltrexone/bupropion has been well-proven. We present a case study in which naltrexone/bupropion, a glucagon-like peptide-1 agonist, and a sodium-glucose transporter 2 inhibitor showed significant weight loss and improved metabolic parameters. Additionally, the management of type 2 diabetes and hypertension, which are common diseases in patients with obesity, was also included.

Production and Separation of Angiotension Converting Enzyme Inhibitor during Natto Fermentation (납두 발효과정 중 Angiotensin Converting Enzyme 저해물질의 생성 및 분리)

  • Cho, Young-Je;Cha, Woen-Suep;Bok, Su-Kyung;Kim, Myung-Uk;Chun, Sung-Sook;Choi, Ung-Kyu;Kim, Soon-Hee;Park, Kyung-Sook
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.29 no.4
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    • pp.737-742
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    • 2000
  • As functionality investigation of a soybean fermentation food, a angiotensin converting enzyme inhibitory peptide was separated during natto fermentation by Bacillus natto and inhibitory effect was investigated. After incubation at each 2$0^{\circ}C$, 3$0^{\circ}C$, 4$0^{\circ}C$, 5$0^{\circ}C$, 6$0^{\circ}C$ for the 0~72 hr, protein content, protease activity and angiotensin converting enzyme inhibition were determined. The protein content and protease activity were increased and reached maximum at 60 hr fermentation with 4$0^{\circ}C$ and decreased after the 60 hr fermentation during natto fermentation. The optimum condition for angiotensin converting enzyme inhibitors was appeared at fermentation for 60 hr at 4$0^{\circ}C$. Crude extract of natto was partially purified by Amicon membrane YM-3 and Sephadex G-10, G-25 gel filtration, stepwise. The inhibitory rate was increased in a concentration dependent manner, espcially the most potent activity about 74.74% at 1.0 mg peptide content. The most prominent amino acid of the peptide from natto was alanine, followed by phenylalnine, histidine.

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Selective Inhibition of Bicyclic Tetrapeptide Histone Deacetylase Inhibitor on HDAC4 and K562 Leukemia Cell

  • Li, Xiao-Hui;Huang, Mei-Ling;Wang, Shi-Miao;Wang, Qing
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.12
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    • pp.7095-7100
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    • 2013
  • Histone deacetylase (HDAC) inhibitors of cyclic peptide have been proved to be the most complex but the most stable and relative efficient inhibitors because of their large cap region. In this paper, a series of studies were carried out to evaluate the efficacy of synthetic bicyclic tetrapeptide inhibitors 1-5 containing hydroxamic acid referring molecular docking, anti-proliferation, morphology and apoptosis. Docking analysis, together with enzyme inhibitory results, verified the selective capability of inhibitor 4 to HDAC4, which might closely related to haematological tumorigenesis, with Phe227, Asp115, Pro32, His198 and Ser114 participating into hydrophobic interactions and Van der Waals force which was familiar with former study. Moreover, inhibitor 4 inhibited K562 cell line at the $IC_{50}$ value of 1.22 ${\mu}M$ which was 51-67 times more efficient than that for U937 and HL60 cell lines. Inhibitor 4 exhibited the cell cycle-arrested capability to leukemia at S phase or G2/M phase as well as apoptosis-induced ability in different degrees. Finally, we considered that bicyclic tetrapeptide inhibitors were promising inhibitors used in cancer treatment and inhibitor 4 could prevent K562 cell line well from proliferation, arrest cell cycle and induce K562 towards apoptosis to achieve the goals of reversing cancer cells which could become a potential leukemia therapeutic agent in the future.

Roles of Opioid Receptor Subtype in the Spinal Antinociception of Selective Cyclooxygenase 2 Inhibitor

  • Choi, Cheol-Hun;Kim, Woong-Mo;Lee, Hyung-Gon;Jeong, Cheol-Won;Kim, Chang-Mo;Lee, Seong-Heon;Yoon, Myung-Ha
    • The Korean Journal of Pain
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    • v.23 no.4
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    • pp.236-241
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    • 2010
  • Background: Selective inhibitors of cycloosygenase (COX)-2 are commonly used analgesics in various pain conditions. Although their actions are largely thought to be mediated by the blockade of prostaglandin (PG) biosynthesis, evidences suggesting endogenous opioid peptide link in spinal antinociception of COX inhibitor have been reported. We investigated the roles of opioid receptor subtypes in the spinal antionociception of selective COX-2 inhibitor. Methods: To examine the antionociception of a selective COX-2 inhibitor, DUP-697 was delivered through an intrathecal catheter, 10 minutes before the formalin test in male Sprague-Dawley rats. Then, the effect of intrathecal pretreatment with CTOP, naltrindole and GNTI, which are ${\mu}$, $\delta$, and k opioid receptor antagonist, respectively, on the analgesia induced by DUP-697 was assessed. Results: Intrathecal DUP-697 reduced the flinching response evoked by formalin injection during phase 1 and 2 Naltrindole and GNTI attenuated the antinociceptive effect of intrathecal DUP-697 during both phases of the formalin test, CTOP reversed the antinociception of DUP-697 during phase 2, but not during phase 1, Conclusions: Intrathecal DUP-697, a selective COX-2 inhibitor, effectively relieved inflammatory pain in rats. The $\delta$ and $\kappa$ opioid receptors are involved in the activity of COX-2 inhibitor on the facilitated state as well as acute pain at the spinal level, whereas the ${\mu}$ opioid receptor is related only to facilitated pain.

Effect of Samryungbaikchul-san on Astrocyte Activation and Apoptosis in Mouse Model of Alzheimer Disease (삼령백출산(蔘笭白朮散)이 Alzheimer's Disease 동물모델의 Astrocyte 활성화 및 Apoptosis에 미치는 영향)

  • Lee, Sang-Ryong
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.23 no.2
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    • pp.374-380
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    • 2009
  • Samryungbaikchul-san(SRBCS) has been used in oriental medicine for the treatments of gastrointestinal and neurological disorders. Here, potential protective function of SRBCS was investigated in neural tissues in Alzheimer's disease(AD) mouse model. In primary cultured cells from the spinal cord of newborn rats, treatment of ${\beta}$-amyloid peptide elevated cell counts positive to glial fibrillary acidic protein(GFAP) or caspase 3 immunoreactivity, but the co-treatment of SRBCS reduced positive cell counts. In vivo administration of scopolamine, an inhibitor of muscarinic receptor, resulted in increases in the number of glial fibrillary acidic protein(GFAP) and caspase 3-positive cells in hippocampal subfields, which was then decreased by the treatment of SRBCS or acetylcholinesterase inhibitor galathamine. The present data suggest that SRBCS may play a protective role in damaged neural tissues caused by scopolamine treatments in mice.

ACE inhibitory activity of Peptide from krill(Euphausia superba) Hydrolysate

  • Kim, Dong-Soo;Kim, Young-Myoung;Park, Douck-Choun;Do, Jeong-Ryong
    • Proceedings of the Korean Society of Fisheries Technology Conference
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    • 2001.10a
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    • pp.183-184
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    • 2001
  • Angiotensin I converting enzyme (ACE) in renin-angiotensin system is a cause of essential hypertension, which covers most hypertension, one of the major adult diseases. Thus, the inhibition of ACE would be indispensable for the prevention and cure of hypertension. Therefore, a lot of studies on the ACE inhibitor have been conducted. Peptides from the protein hydrolysate have been reported as an remarkable inhibitor. Especially, various ACE inhibitory peptides were isolated and identified from marine products for their utilization as value added products. (omitted)

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Protective Effect of Celecoxib, a Selective Cyclooxygenase-2 Inhibitor, Against Beta-Amyloid-Induced Apoptosis: Possible Involvement of Proinflammatory Signals in Beta-Amyloid-Mediated Cell Death

  • Jang, Jung-Hee;Surh, Young-Joon
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2003.10b
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    • pp.139-140
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    • 2003
  • Inflammatory as well as oxidative tissue damage has been implicated in pathophysiology of Alzheimer's disease (AD), and non-steroidal anti-inflammatory drugs have been reported to have beneficial effects in the treatment or prevention of AD. In the present study, we investigated the effect of celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, on inflammatory cell death induced by beta-amyloid, a neurotoxic peptide associated with senile plaques formed in the brains of patients with AD.(omitted)

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Purification and Characterization of Angiotensin I-Converting Enzyme Inhibitors from Sinapis alba L.

  • Yuk, Jin-Su;Lim, Young-Hee;Cho, Hong-Yon
    • Preventive Nutrition and Food Science
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    • v.5 no.2
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    • pp.75-80
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    • 2000
  • To separate ACE inhibitors from edible plants, spices, and herbs, 285 extracts of 95 sources were screened for ACE inhibitory activity. The extract of Sinapis alba L. had the most potent ACE inhibitory activity. Mustard seeds were crushed homogeneously and extracted with hexane and water successively. Lyophilized water extract was fractionated with $H_2O$:butanol(1:1). The ACE inhibitor was purified from butanol fraction by methanol precipi-tation, gel filtration, HPLC, and FPLC with Superdex peptide HQ 10/30 column. The active fraction has been purified to homogeneity, which was proven by gel filtration using FPLC system. The yield was 0.02%. The com-pound has a molecular weight of about 640. The compound competitively inhibited ACE activity and the $IC_{50}$ value was 79$\mu\textrm{g}$/ml. The purified compound showed uterus contraction activity in isolated rat uterus.

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Discovery of Novel Transcription Factor Inhibitors Using a Pyrazole-based Small Molecule Library

  • Ha, Hyung-Ho;Kim, B.Moon
    • Bulletin of the Korean Chemical Society
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    • v.29 no.2
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    • pp.323-327
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    • 2008
  • A focused library of pyrazole-based compounds was constructed towards novel transcription factor inhibitors. Complementary hydrogen bonding interaction with b-sheet peptide structures was the basis for the design of 5-amino-3-pyrazole carboxamide scaffold. From the preliminary inhibition assay against several transcription factors, compounds 7e and 8g were identified as novel lead compounds against HIF-1a and NF-AT transcription factors, respectively.