• Title/Summary/Keyword: Protein drugs

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Characteristics of protein from red crab (Chionoecetes japonicus) shell by commercial proteases (효소적 가수분해에 의한 홍게껍질 단백질의 특성)

  • Noh, Kyung-Hee;Min, Kwan-Hee;Seo, Bo-Young;Kim, So-Hee;Seo, Young-Wan;Song, Young-Sun
    • Journal of Nutrition and Health
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    • v.45 no.5
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    • pp.429-436
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    • 2012
  • This study was performed to examine the characteristics of protein of red crab (Chionoecetes japonicus) shell powder hydrolyzed by commercial proteases. Red crab shell was digested by commercial proteases, such as Protamex (P), Neutrase (N), Flavourzyme (F), Alcalase (A), Protease M (PM) and Protease A (PA). Protein yield analyzed by Biuret assay, absorbance at 280 nm and brix revealed that PA was the enzyme having the highest proteolytic activity. SDS PAGE showed that molecular weight of proteins produced by protease treatments was various and below 150 kDa. Combinational treatment of proteases (PA + P, PA + PM, PA + F, PA + A) was tried whether these increase protein hydrolysis from red crab shell powder compared to a PA single treatment. Soluble protein content was similar, but amino acid concentration by combinational treatments was higher than PA single treatment [PA + P 247.4 mg/g > PA + F (206.4 mg/g) > PA + A (133.4 mg/g) > PA + PM (59.1 mg/g) > PA (54.9 mg/g)]. Amino acid composition by combinational treatments was slightly different. Most abundant essential amino acids were phenylalanine, glycine, alanine, and leucine, whereas tyrosine and cystine were not detected.

Immunopotentiating Activity of Water Extracts of Some Crude Drugs (수종 생약 수침 엑기스의 면역증강 작용에 관한 연구)

  • Kim, Mi-Sook;Lee, Na-Gyong;Lee, Jae-Hyun;Byun, Soon-Jung;Kim, Young-Choong
    • Korean Journal of Pharmacognosy
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    • v.19 no.3
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    • pp.193-200
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    • 1988
  • Immunopotentiating activity of water extract of Lycii Fructus, Rubus Fructus, Torilis Fructus, Schizandrae Fructus and Cuscutae Semen were investigated using mouse fed with normal diet and protein deficient diet. Body weight, ratio of spleen or thymus to body weight, number of total peritoneal exudate cell, content of total serum protein and albumin content were decreased in the mouse fed with protein deficient diets as compared to the mouse fed with normal diet. Regardless of the nutritional condition, the supplement of the water extract of Lycii, Rubus Torilis, Schizandrae Fructus or Cuscutae Semen increased the ratio of spleen to body weight. The increment of this ratio was significant by the supplement of water extracts of Lycii and Torilis Fructus in mouse fed with protein deficient diet. The supplement of water extracts of Torilis Fructus to the mouse fed with protein deficient diet increased the content of total serum protein and albumin content significantly. Similar results were obtained with Lycii, Rubus, Schizandrae Fructus and Cuscutae Similar. The electrophorogram shows the difference in the concentration of some serum protein constituents between the mouse fed with normal diet and protein deficient diet.

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Inhibition of protein tyrosine phosphatase non-receptor type 2 by PTP inhibitor XIX: Its role as a multiphosphatase inhibitor

  • Le, Hien Thi Thu;Cho, Young-Chang;Cho, Sayeon
    • BMB Reports
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    • v.50 no.6
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    • pp.329-334
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    • 2017
  • Protein tyrosine phosphatases (PTPs) play crucial roles in signal transduction and their functional alteration has been detected in many diseases. PTP inhibitors have been developed as therapeutic drugs for diseases that are related to the activity of PTPs. In this study, PTP inhibitor XIX, an inhibitor of CD45 and PTEN, was investigated whether it inhibits other PTPs. Protein tyrosine phosphatase non-receptor type 2 (PTPN2) was selectively inhibited by the inhibitor in a competitive manner. Drug affinity responsive target stability (DARTS) analysis showed that the inhibitor induces conformational changes in PTPN2. Phosphorylation levels of signal transducer and activator of transcription 3 (STAT3) at Tyr-705, a crucial site for STAT3 activation and target site of PTPN2, decreased upon exposure to the inhibitor. Our results suggest that PTP inhibitor XIX might be considered as an effective regulator of PTPN2 for treating diseases related to PTPN2.

Precise assembly and regulation of 26S proteasome and correlation between proteasome dysfunction and neurodegenerative diseases

  • Im, Eunju;Chung, Kwang Chul
    • BMB Reports
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    • v.49 no.9
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    • pp.459-473
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    • 2016
  • Neurodegenerative diseases (NDs) often involve the formation of abnormal and toxic protein aggregates, which are thought to be the primary factor in ND occurrence and progression. Aged neurons exhibit marked increases in aggregated protein levels, which can lead to increased cell death in specific brain regions. As no specific drugs/therapies for treating the symptoms or/and progression of NDs are available, obtaining a complete understanding of the mechanism underlying the formation of protein aggregates is needed for designing a novel and efficient removal strategy. Intracellular proteolysis generally involves either the lysosomal or ubiquitin-proteasome system. In this review, we focus on the structure and assembly of the proteasome, proteasome-mediated protein degradation, and the multiple dynamic regulatory mechanisms governing proteasome activity. We also discuss the plausibility of the correlation between changes in proteasome activity and the occurrence of NDs.

Antiapoptotic Fusion Protein Delivery Systems

  • Tan, Cheau Yih;Kim, Yong-Hee
    • Macromolecular Research
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    • v.16 no.6
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    • pp.481-488
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    • 2008
  • Apoptosis is a natural cell suicide mechanism to maintain homeostasis. However, many of the diseases encountered today are caused by aberrant apoptosis where excessive apoptosis leads to neurodegenerative disorders, ischemic heart disease, autoimmune disorders, infectious diseases, etc. A variety of antiapoptotic agents have been reported to interfere with the apoptosis pathway. These agents can be potential drug candidates for the treatment or prevention of diseases caused by dysregulated apoptosis. Obviously, world-wide pharmaceutical and biotechnology companies are gearing up to develop antiapoptotic drugs with some products being commercially available. Polymeric drug delivery systems are essential to their success. Recent R&D efforts have focused on the chemical or bioconjugation of antiapoptotic proteins with the protein transduction domain (PTD) for higher cellular uptake with antibodies for specific targeting as well as with polymers to enhance the protein stability and prolonged effect with success observed both in vivo and in vitro. All these different fusion antiapoptotic proteins provide promising results for the treatment of dysregulated apoptosis diseases.

Study on the Protein Binding of Anti-cancer Agent, 2"-O-benzoylcinnamaldehyde, using Ultrafilteration and Flurescence Spectrometry

  • Ren , Shan;Kim, Dae-Duk;Lee, Chi-Ho
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.242.3-243
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    • 2003
  • The compound of 2"-O-benzoylcinnamaldehyde(CB-ph) is a derivative of 2"-hydroxycinnamaldehyde whcih is a methanol extract of cinnamomum cassia blume. It"s a new anti-cancer agent which has been showed to inhibit the growth of various tumor cells in vitro and in vivo. In order to investigate the effective drug concentration and bio-distribution of CB-ph, the plasma protein binding was studied. In this study, the degree of the binding of Cb-ph to various serum proteins, the binding parameters, the binding site of CB-ph in human serum albumin, and the effect of some extensive protein-binding drugs on the protein binding of CB-ph in human serum ablumin were investigated respectively by ultrafilteration and fluorescence spectrometry. (omitted)

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CoMFA and CoMSIA Study on Angiotensin-Converting Enzyme (ACE) Inhibitors: a Molecular Design of Potential Hypertensive Drugs

  • San Juan, Amor A.;Cho, Seung-Joo
    • Proceedings of the Korean Society for Bioinformatics Conference
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    • 2005.09a
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    • pp.249-255
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    • 2005
  • Angiotensin-converting enzyme (ACE) is primarily responsible for human hypertension. Current ACE drugs show serious cough and angiodema health problems due to the un-specific activity of the drug to ACE protein. The availability of ACE crystal structure (1UZF) provided the plausible biological orientation of inhibitors to ACE active site (C-domain). Three-dimensional quantitative structure-activity relationship (3D-QSAR) models have been constructed using the comparative molecula. field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) for a series of 28 ACE inhibitors. Alignment for CoMFA obtained by docking ligands to 1UZF protein using FlexX program showed better statistical model as compared to superposition of corresponding atoms. The statistical parameters indicate reasonable models for both CoMFA (q$^2$ = 0.530, r$^2$ = 0.998) and CoMSIA (q$^2$= 0.518, r$^2$ = 0.990). The 3D-QSAR analyses provide valuable information for the design of ACE inhibitors with potent activity towards C-domain of ACE. The group substitutions involving the phenyl ring and carbon chain at the propionyl and sulfonyl moieties of captopril are essential for specific activity to ACE.

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Inhibitory Effects of Water Extract from Rice Bran Due to cAMP-dependent Phosphorylation of VASP ($Ser^{157}$) on ADP-induced Platelet Aggregation

  • Kim, Hyun-Hong;Hong, Jeong Hwa;Ingkasupart, Pajaree;Lee, Dong-Ha;Park, Hwa-Jin
    • Biomedical Science Letters
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    • v.20 no.3
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    • pp.129-138
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    • 2014
  • In this study, we investigated the effect of water extract from rice bran (RB) on ADP ($20{\mu}M$)-stimulated platelet aggregation. RB dose-dependently inhibited ADP-induced platelet aggregation, and its $IC_{50}$ value was $224.0{\mu}g/mL$, which was increased by adenylate cyclase inhibitor SQ22536 and cAMP-dependent protein kinase (A-kinase) inhibitor Rp-8-Br-cAMPS. RB elevated the phosphorylation of VASP ($Ser^{157}$) which was also inhibited by SQ22536 and Rp-8-Br-cAMPS. It is thought that RB-elevated cAMP contributed to the phosphorylation of VASP ($Ser^{157}$) to inhibit ADP-induced platelet aggregation. Therefore, we demonstrate that RB has an antiplatelet effect via cAMP-dependent phosphorylation of VASP ($Ser^{157}$), and RB may have preventive or therapeutic potential for platelet aggregation-mediated diseases, such as thrombosis, myocardial infarction, atherosclerosis, and ischemic cerebrovascular disease.

Effects of Oriental Medicinal Drugs on Axonal Regeneration in the Spinal Cord Neurons

  • An Joung-Jo;NamGung Uk;Seo In-Chan;Kim Yoon-Sik
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.19 no.6
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    • pp.1640-1646
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    • 2005
  • An oriental medicinal drugs Jahageo (JHG, Hominis placenta) were examined to determine its effects on the responsiveness of central nervous system neurons after injury. We found that JHG was involved in neurite outgrowth of DRG sensory axons. JHG treatment also increased expression of axonal growth-associated protein GAP-43 in DRG sensory neurons after sciatic nerve injury and in the injured spinal cord. JHG treatment during the spinal cord injury increased induction levels of cell division cycle 2 (Cdc2) protein in DRG as well as in the spinal cord. Histochemical investigation showed that induced Cdc2 in the injured spinal cord was found in non-neuronal cells. These results suggest that JHG regulates activities of non-neuronal cells such as oligodendrocyte and astrocyte in responses to spinal cord injury and protects neuronal responsiveness after axonal damage.

Functional Expression of Choline Transporter-Like Protein 1 in LNCaP Prostate Cancer Cells: A Novel Molecular Target

  • Saiki, Iwao;Yara, Miki;Yamanaka, Tsuyoshi;Uchino, Hiroyuki;Inazu, Masato
    • Biomolecules & Therapeutics
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    • v.28 no.2
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    • pp.195-201
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    • 2020
  • Prostate cancer is one of the most common cancers in men. Choline PET or PET/CT has been used to visualize prostate cancer, and high levels of choline accumulation have been observed in tumors. However, the uptake system for choline and the functional expression of choline transporters in prostate cancer are not completely understood. In this study, the molecular and functional aspects of choline uptake were investigated in the LNCaP prostate cancer cell line along with the correlations between choline uptake and cell viability in drug-treated cells. Choline transporter-like protein 1 (CTL1) and CTL2 mRNA were highly expressed in LNCaP cells. CTL1 and CTL2 were located in the plasma membrane and mitochondria, respectively. [3H]Choline uptake was mediated by a single Na+-independent, intermediate-affinity transport system in the LNCaP cells. The anticancer drugs, flutamide and bicalutamide, inhibited cell viability and [3H]choline uptake in a concentration-dependent manner. The correlations between the effects of these drugs on cell viability and [3H]choline uptake were significant. Caspase-3/7 activity was significantly increased by both flutamide and bicalutamide. Furthermore, these drugs decreased CTL1 expression in the prostate cancer cell line. These results suggest that CTL1 is functionally expressed in prostate cancer cells and are also involved in abnormal proliferation. Identification of this CTL1-mediated choline transport system in prostate cancer cells provides a potential new therapeutic target for the treatment of this disease.