• Title/Summary/Keyword: Selective activation

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NEW SELECTIVE AND POTENT INHIBITORS OF HUMAN CYTOCHROM P450 1A FAMILY ENZYMES

  • F. Peter Guengerich;Chun, Young-Jin;Kim, Sanghee;Kim, Donghak;Lee, Sang-Kwang;Dong, Mi-Sook;Ueng, Yune-Fang
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.37-38
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    • 2001
  • The cytochrome P450 (P450) 1 family (1A1, 1A2, 1B1) is involved in the activation of many pro-carcinogens. Previously we characterized a number of synthetic bi- and polycyclic hydrocarbon acetylenes as selective-mechanism-based inhibitors of recombinent P450s 1A1, 1A2, 1B1 (Shimada et al., Chem. Res. Toxicol., 11, 1048-1056, 1998). We reported that the drug oltipraz is a mechanism-based indicator of P450 1A2 (Lagouet et al. Chem. Res. Toxicol., 13, 245-252, 2000).(omitted)

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PARTIAL OXIDATION OF PROPANE ON NAFION SUPPORTED CATALYTIC MEMBRANE

  • F. Frusteri;C. Espro;F. Arena;F. Arena;E. Passalacqua;A.Patti;A. Parmaliana
    • Proceedings of the Membrane Society of Korea Conference
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    • 1999.07a
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    • pp.55-58
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    • 1999
  • Nafion supported catalytic membranes were found to be active, stable and selective in th partial oxidation of propane to oxygenates with H2O2 under mild condition. Addition of Fe2+ in liquid phase enhances the reaction rate. Reaction proceeds according to a radical mechanism based on th electrophilic activation of propane on superacid sites and subsequent reaction of the activated paraffin with OH radicals. The use of a catalytic membrane, which allow separation of the intermediate products from the liquid phase containing the oxidant, was found to be effective to perform selective partial oxidation of propane with high yields to oxygenated products.

Consideration of the Exercise position for Facilitating Gluteus Medius Maximally in Normal Adults

  • Park, Sung Jin;Park, Ji Won;Kwon, Yonghyun
    • The Journal of Korean Physical Therapy
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    • v.31 no.1
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    • pp.62-66
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    • 2019
  • Purpose: This study examined the most efficient exercise position to activate the gluteus medius (GM) and tensor fascia latae (TFL) in hip abduction in side-lying (HA-SL), clam in side-lying (CL-SL), and sling bridging in side-lying (SB-SL), which are the most representative GM exercises. Methods: Twenty-four healthy male adults aged from 20 to 40 years, whose body mass index was under 25, participated in this experiment. While all participants conducted three different positions with a counterbalanced manner, such as in AB, CL, and BR, activation of the GM and TFL was measured using 8-channel wireless EMG. Exercise was performed for 10 seconds three times in total with a five minute-break session. Results: Significant differences in GM and TFL activation were observed among the three positions (p<0.05). The highest activation of 60.69 was observed in BR followed in order by 46.03 and 12.92 in HA-SL and CL, respectively. TFL activation in HA-SL was 42.01, followed in order by 35.98 and 14.01 in BR and CL, respectively. On the other hand, there was no significant difference in TFL muscle activation between BR and HA-SL. Conclusion: These findings suggest that both BR and HA-SL in GM can be done selectively. CL has remarkably low muscle activation in GM and TFL, which makes it less valuable in GM and TFL exercise. In conclusion, selective BR and HA-SL exercise should be applied to maximally and effectively activate the GM.

Ankle Sprain Affects Lower Leg Muscle Activation on Vertical Landing, Half Point, and Gait in Female Ballet Students

  • Kim, Heejaeng
    • The Journal of Korean Physical Therapy
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    • v.31 no.2
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    • pp.129-133
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    • 2019
  • Purpose: This study aimed to investigate effect of ankle instability on peripheral muscle activation among female ballet dancers to provide information on the development of prevention programs for ankle injury rehabilitation. Methods: 32 female ballet dancers were randomly divided into two groups: experience ankle sprain group (n=16, age, $20.7{\pm}0.8years$, BMI $18.6{\pm}1.2kg/m2$) and non-experience ankle sprain group (n=16, $age=21.0{\pm}0.8years$, BMI $19.6{\pm}2.0kg/m2$). Activation of the peroneus longus, tibialis anterior muscle, and gastrocnemius during vertical landing, half pointe, and gait between the two groups were measured. Body composition analyzer was used to examine skeletal muscle mass and body fat mass. Results: A total of 32 patients were included. In the experience ankle sprain group (n=16: left sprain 14, right sprain 2), average ankle sprain injury occurred 7.5 months before the study. The average age of the dancers in the experience ankle sprain group and non-experience ankle sprain group was $20.7{\pm}0.8$ and $21.0{\pm}0.8years$, major period was $64.5{\pm}23.8$ and $71.6{\pm}25.8months$, BMI was $18.6{\pm}1.2$ and $19.5{\pm}2.0kg/m2$, respectively. No significant differences were found on body composition between the two groups (p>0.05). The experience ankle sprain group showed significantly lower tibialis anterior and peroneus longus muscle activation (p<0.5), while gastrocnemius muscle activation appeared to be significantly higher (p<0.05) during landing, half pointe, and normal gait. Conclusion: Ankle sprain can cause a decline in peripheral muscle activation and coordination, which increased the risk for repetitive ankle sprain in the future. Moreover, ankle peripheral muscle selective strength training, coordination program development, and application need to be considered to prevent ankle sprain.

Selective Activation of Mitogen-Activated Protein (MAP) Kinase During the Progression of Renal Disease

  • Park, Sang-Joon;Jeong, Kyu-Shik;Jeong, Tae-Sook;Bok, Song-Hae;Lee, Cha-Soo
    • Proceedings of the Korean Society of Veterinary Pathology Conference
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    • 2000.09a
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    • pp.19-19
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    • 2000
  • Most renal diseases progress by consecutive cell responses such as hypertrophy, hyperplsia, proliferation, defferentiation, sclerosis, fibrosis and other cellular degenerative process. These cellular responses are mediated by the activation of various mitogens such as vasoconstrictors, growth factors, hormone, genotoxins and cytokines through mechanical, hemodynamic, immunological injury as well as metabolic abnormality. (omitted)

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Specific Binding and Catalytic Activation of the MAPK-MKP Complex

  • Kim, Myeongbin;Ryu, Seong Eon
    • Biodesign
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    • v.6 no.4
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    • pp.79-83
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    • 2018
  • Mitogen-activated protein kinases (MAPKs) are one of the most important enzymes in various cellular activities, and the MAPK signaling pathway is implicated in many disorders. MAPK phosphatases (MKPs) are regulators that contain a MAPK-binding domain (MBD) for MAPK recognition, and a catalytic domain (CD), for dephosphorylation and inactivation of MAPKs. Due to their crucial role in regulating the MAPK pathway, MKPs are regarded as a potential drug target in various diseases. Attempts have also been made to regulate the MAPK pathway by reducing the MKP activity. For drug development, it is important to understand the key features of MAPK-MKP complex formation. This review summarizes the studies on MAPK-MKP complexes, mainly focusing on their selective recognition and catalytic activation.

Differential involovement of JNK in apicidin-induced apoptosis.

  • Kim, Ji-Ae;Cho, Eun-jung;Lee, Hoi-Young;Hong , Sung-Youl;Lee, Hyang-Woo;Han, Jeung-Whan
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.323.2-323.2
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    • 2002
  • We previously reported that apicidin induces apoptosis through selective induction of Fas/Fas ligand. resulting in the release of cytochrome C from mitochondria to the cytosol and subsequent activation of caspase-9 and \ulcorner However. we observed that apicidin did not induce the apoptosis in a specific cell line. such as HeLa. which was characterized by nuclear DNA fragmentation. On the basis of these facts, we tested whether JNK activation is involved in cell death induced by apicidin. (omitted)

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Enhanced Anti-tumor Reactivity of Cytotoxic T Lymphocytes Expressing PD-1 Decoy

  • Jae Hun Shin;Hyung Bae Park;Kyungho Choi
    • IMMUNE NETWORK
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    • v.16 no.2
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    • pp.134-139
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    • 2016
  • Programmed death-1 (PD-1) is a strong negative regulator of T lymphocytes in tumor-microenvironment. By engaging PD-1 ligand (PD-L1) on tumor cells, PD-1 on T cell surface inhibits anti-tumor reactivity of tumor-infiltrating T cells. Systemic blockade of PD-1 function using blocking antibodies has shown significant therapeutic efficacy in clinical trials. However, approximately 10 to 15% of treated patients exhibited serious autoimmune responses due to the activation of self-reactive lymphocytes. To achieve selective activation of tumor-specific T cells, we generated T cells expressing a dominant-negative deletion mutant of PD-1 (PD-1 decoy) via retroviral transduction. PD-1 decoy increased IFN-γ secretion of antigen-specific T cells in response to tumor cells expressing the cognate antigen. Adoptive transfer of PD-1 decoy-expressing T cells into tumor-bearing mice potentiated T cell-mediated tumor regression. Thus, T cell-specific blockade of PD-1 could be a useful strategy for enhancing both efficacy and safety of anti-tumor T cell therapy.

Inhibition of liver fibrosis by sensitization of human hepatic stellate cells by combined treatment with galtanin and TARIL

  • Dong-Oh Moon
    • Journal of Applied Biological Chemistry
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    • v.66
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    • pp.138-143
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    • 2023
  • Liver fibrosis is caused by metabolic problems such as cholestasis, genetic problems, or viral infections. Inhibiting hepatic stellate cell (HSC) activation or inducing selective apoptosis of activated HSCs is used as a treatment strategy for liver fibrosis. It has been reported that when HSCs are activated, their apoptosis sensitivity to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is enhanced because the expression of death receptor 5 is elevated. Finding a natural compound that can enhance the apoptotic effect of TRAIL on HSCs is a necessary strategy for liver fibrosis treatment. It was confirmed here that mangosteen-derived gartanin increased the effect of TRAIL-induced apoptosis by increasing the expression of DR5 in a p38-dependent manner in the hepatic stellate cell line LX-2. Combined treatment with gartanin and TRAIL accelerated DNA cleavage through caspase-3 activation and enhanced antifibrotic effects in LX-2 cells.

Synthesis and Biological Activity of Benzoxazole Containing Thiazolidinedione Derivatives

  • Jeon, Ra-Ok;Park, So-Yeon
    • Archives of Pharmacal Research
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    • v.27 no.11
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    • pp.1099-1105
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    • 2004
  • The peroxisome proliferator-activated receptors (PPARs) are a primary regulator of lipid metabolism. Potency for activation of PPAR$\gamma$, one of a subfamily of PPARs, particularly mirrors glucose lowering activity. We prepared thiazolidinediones featuring benzoxazole moiety for subtype selective PPAR$\gamma$ activators. 5-[4-[2-(Benzoxazol-2-yl-alkylamino)ethoxy]benzyl]thiazolidine-2,4-diones have been prepared by Mitsunobu reaction of benzoxazolylalkylaminoethanol 8 and hydroxybenzylthiazolidinedione 6 and their activities were evaluated. Most compounds tested were identified as potent PPAR$\gamma$ agonists.