• Title/Summary/Keyword: HT approaches

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3D Structure Prediction of Human 5-Hydroxytryptamine Receptor 7 (5-HT7R)

  • Madhavan, Thirumurthy
    • Journal of Integrative Natural Science
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    • v.11 no.2
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    • pp.87-92
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    • 2018
  • 5-Hydroxytryptamine receptor 7 ($5-HT_7R$) is one of G-Protein coupled receptors, which is found to be involved in the pathophysiology of various neurological disorders including depression, sleep disorders, memory deficiency and neuropathic pain. After activation of $5-HT_7R$ by serotonin, it activates the production of the intracellular signaling molecule cyclic AMP. The availability of 3D structure of the receptor would enhance the development of new drugs. Hence, in the present study, homology modelling of human 5-hydroxytryptamine receptor 7 ($5-HT_7R$) was performed using comparative modelling (Easy Modeller) and threading (I-TASSER) approaches. The generated models were validated using Ramachandran plot and ERRAT plot and the best models were selected based on the validation results. The 3D model developed here could be useful for identifying crucial residues and further docking study.

The Effect of Vitamin B-2 and (or) Vitamin B-6 Deficiency on Hematologic Profile in Rats (Vitamin B-2와 (또는 ) Vitamin B-6 결핍이 흰쥐의 Hematologic Profile에 미치는 영향)

  • 유정열
    • Journal of Nutrition and Health
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    • v.22 no.3
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    • pp.167-174
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    • 1989
  • The purpose of this study was to determine if vitamin B-2 and vitamin B-6 deficiency affects hematologic profile in vivo. Rats were fed a vitamin B-2 deficient (-B2) diet or a vitamin B-6 deficient (- B6) diet or a combined vitamin B-2 and vitamin B-6 deficient (-B2-B6) diet or a control diet for 6 weeks. Hematocrit (Ht), hemoglobin (Hb), plasma iron (PI), transferrin saturation (TS) and liver iron concentration (LI) were compared. In -B2 rats vs. control rats, PI, TS and LI were significantly lower but Ht and Hb were not. In - B6 rats vs. control, Ht and Hb were significanty lower but LI was higher. The -B2-B6 rats had intermediate effects in Hb, PI, TS and LI and a decrease in Ht. The repletion with a contro diet for 2 weeks resulted in significant improvements in hematologic indices and LI in both - B2 rats and - B6 rats. This study suggests that the intakes of vitamin B-2 and vitamin B-6 are important for preventive and therap\ulcornereutic approaches to improve the hematologic status in nutritionally anemic groups.

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Production and Characterization of Porcine Cell Lines Overexpressing Human H-Transferase (사람 H-Transferase 유전자 과발현 형질전환 체세포주 확립 및 검증)

  • Lee, Sang-Mi;Park, Hyo-Young;Kim, Hey-Min;Moon, Seung-Ju;Kang, Man-Jong
    • Reproductive and Developmental Biology
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    • v.31 no.3
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    • pp.187-191
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    • 2007
  • This study was canted out to develop cell lines overexpressing human H-transferase (HT). One of the approaches to prevent hyperacute rejection in xenotransplantation might be the expression of human HT in porcine cells. In this study, we cloned human HT gene from HepG2 cells using RT-PCR to establish HT-overexpressing vector. The full-length cDNA of human HT was inserted into the 3' end of CMV promoter for construction of the overexpression vector pRc/CMV-hHT. Using ietPEI DNA transfection reagent, the vector was introduced into porcine ear skin fibroblasts from newborn piglets. Transfected cells were selected by treatment of $300{\mu}g/ml$ G418 for 12 days. After antibiotic selection, survived colonies with approximately 5mm in diameter were picked and analysed for transgene human HT by PCR. The colonies proven to be human HT transfectants were analysed by RT-PCR to determine their expressions or human HT. In all colonies tested, human HT mRNA was detected. This result demonstrates the establishment of porcine cell lines overexpressing human HT, and these cell lines may be used for the development of transgenic pigs for xenotransplantation.

Roles of Monoamine Neurotransmitters in Regulation of Hypothalamic PITUITITARY-ADRENAL AXIS(HPA) (III) - Role of 5-hydroxytryptamine in Controlling the Stress-Induced Elevation of Corticosterone in Rat - (시상하부-뇌하수체-부신계 조절에 대한 Monoamine 신경전달물질의 역할에 관한 연구(III)-뇌 5-hydroxytyptamine(Serotonin)이 Stress 시 Corticosteroid 변동에 미치는 영향)

  • Suh, Yoo-Hun;Lim, Jung-Kyoo;Park, Chan-Woong
    • The Korean Journal of Pharmacology
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    • v.19 no.2
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    • pp.45-55
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    • 1983
  • A role for brain serotonin(5-HT) in regulation of the HPA axis has been suggested but remains contoversial and poorly defined. The present experiments were designed to check kinetic parameters of 5-HT turnover in rat hypothalamus and remainder brain areas before and after stress and to test whether using various different pharmacologic approaches to stimulate or eliminate the control serotonergic system have any consistent effect on the stress-induced activation of HPA system. Steady state brain serotonin and 5-HIAA concentrations during 1 min ether stress were significantly elevated without significant rise in the levels of plasma corticosterone, which highly increased 2 minutes after stress. This suggests that the increase in serotonergic neuron activity precede that in HPA activity. Furthermore, during 1 ruin-ether stress or 30 min immobilization stress there is a marked increase in hypothalamic and remainder brain serotonin (5-HT) turnover or synthesis rates assessed by both the pargline/5-HT method and pargyline/5-HIAA method. The stress-induced corticosterone levels were increased by serotonin precursors and serotonin agonist in a dose-related fashion. The stress- induced corticosterone levels were highly elevated by L-tryptophan (100 mg/kg) and Potentiated by monoamine oxidase inhibitor, pargyline or serotonin agonist, 5-MeoDMT. The stress-induced elevation of corticosterone and 5-HT levels in rat brain were not significantly decreased by the administration of 5-HT synthesis inhibitor, PCPA and 5-HT neurotoxin, 5,7-DHT. However, the stress-induced elevation of corticosterone and 5-HT levels were decreased by the destruction of midline raphe nuclei. There was a strong positive correlation between plasma corticosterone and 5-HT concentrations changed by drugs which mainly manipulating 5-HT system in the hyhothalamus and in the remainder of the brain. In conclusion, our present data stongly suggest that 5-HT is an important key neurotransmitter involved in the stress-induced activation of the HPA system.

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Aprepitant in the Prevention of Vomiting Induced by Moderately and Highly Emetogenic Chemotherapy

  • Wang, Shi-Yong;Yang, Zhen-Jun;Zhang, Zhe;Zhang, Hui
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.23
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    • pp.10045-10051
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    • 2015
  • Chemotherapy is a major therapeutic approach for malignant neoplasms; however, due to the most common adverse events of nausea and vomiting, scheduled chemotherapeutic programs may be impeded or even interrupted, which severely impairs the efficacy. Aprepitants, 5-HT3 antagonists and dexamethasone are primary drugs used to prevent chemotherapy-induced nausea and vomiting (CINV). These drugs have excellent efficacy for control of acute vomiting but are relatively ineffective for delayed vomiting. Aprepitant may remedy this deficiency. Substance P was discovered in the 1930s and its association with vomiting was confirmed in the 1950s. This was followed by a period of non-peptide neurokinin-1 (NK-1) receptor antagonist synthesis and investigation in preclinical studies and clinical trials (phases I, II and III). The FDA granted permission for the clinical chemotherapeutic use of aprepitant in 2003. At present, the combined use of aprepitant, 5-HT3 antagonists and dexamethasone satisfactorily controls vomiting but not nausea. Therefore, new therapeutic approaches and drugs are still needed.

CoMSIA 3D-QSAR Analysis of 3,4-Dihydroquinazoline Derivatives Against Human Colon Cancer HT-29 Cells

  • Kwon, Gi Hyun;Cho, Sehyeon;Lee, Jinsung;Sohn, Joo Mi;Byun, Joon Seok;Lee, Kyung-Tae;Lee, Jae Yeol
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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    • pp.3181-3187
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    • 2014
  • A series of 3,4-dihydroquinazoline derivatives with anti-cancer activities against human colon cancer HT-29 cell were subjected to three-dimensional quantitative structure-activity relationship (3D-QSAR) studies using the comparative molecular similarity indices analysis (CoMSIA) approaches. The most potent compound, BK10001 was used to align the molecules. As a result, the best prediction was obtained with CoMSIA combined electrostatic, hydrophobic, and hydrogen-bond acceptor fields ($q^2=0.648$, $r^2=0.882$). This model was validated by an external test set of six compounds giving satisfactory predictive $r^2$ values of 0.879. This model would guide the design of potent 3,4-dihydroquinazoline derivatives as anti-cancer agent for the treatment of human colon cancer.

Angle Invariant and Noise Robust Barcode Detection System (기울기와 노이즈에 강인한 바코드 검출 시스템)

  • Park, Dongjin;Jun, Kyungkoo
    • Journal of KIISE
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    • v.42 no.7
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    • pp.868-877
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    • 2015
  • The barcode area extraction from images has been extensively studied, and existing methods exploit frequency characteristics or depend on the Hough transform (HT). However, the slantedness of the images and noise affects the performance of these approaches. Moreover, it is difficult to deal with the case where an image contains multiple barcodes. We therefore propose a barcode detection algorithm that is robust under such unfavorable conditions. The pre-processing step implements a probabilistic Hough transform to determine the areas that contain barcodes with a high probability, regardless of the slantedness, noise, and the number of instances. Then, a frequency component analysis extracts the barcodes. We successfully implemented the proposed system and performed a series of barcode extraction tests.

Free vibration of an annular sandwich plate with CNTRC facesheets and FG porous cores using Ritz method

  • Emdadi, Mohsen;Mohammadimehr, Mehdi;Navi, Borhan Rousta
    • Advances in nano research
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    • v.7 no.2
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    • pp.109-123
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    • 2019
  • In this article, the free vibration analysis of annular sandwich plates with various functionally graded (FG) porous cores and carbon nanotubes reinforced composite (CNTRC) facesheets is investigated based on modified couple stress theory (MCST) and first order shear deformation theories (FSDT). The annular sandwich plate is composed of two face layers and a functionally graded porous core layer which contains different porosity distributions. Various approaches such as extended mixture rule (EMR), Eshelby-Mori-Tanaka (E-M-T), and Halpin-Tsai (H-T) are used to determine the effective material properties of microcomposite circular sandwich plate. The governing equations of motion are extracted by using Hamilton's principle and FSDT. A Ritz method has been utilized to calculate the natural frequency of an annular sandwich plate. The effects of material length scale parameters, boundary conditions, aspect and inner-outer radius ratios, FG porous distributions, pore compressibility and volume fractions of CNTs are considered. The results are obtained by Ritz solutions that can be served as benchmark data to validate their numerical and analytical methods in the future work and also in solid-state physics, materials science, and micro-electro-mechanical devices.

Ab-initio DFT Modeling of Alkanethiols as Carbon Steel Corrosion Inhibitors (탄소강 부식 억제제로서 알칸 티올의 Ab-initio DFT 모델링)

  • Lgaz, Hassane;Lee, Han-Seung
    • Proceedings of the Korean Institute of Building Construction Conference
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    • 2021.05a
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    • pp.91-92
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    • 2021
  • In the present work, we simulated and explained the bonding of three alkanethiols - hexanethiol (HT), decanethiol (DT), and 11-mercaptoundecanoic acid (MDA) - with Fe(110) surface and Fe2 clusters using Density Functional Theory (DFT) to probe the corrosion inhibition mechanisms. The interaction energies computed from periodic DFT calculations successfully predicted the experimental inhibition performance. We have found strong covalent bond formation between S(thiol) and Fe-atoms in both approaches, further confirmed by the projected density of states and electron density difference. Besides, natural bond orbital (NBO) charge distribution showed that DT had stronger electron-donation and back-donation synergic interactions with Fe-atoms.

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Biological and Genetic Prediction Factors Associated with Suicidal Behavior (자살 행동과 연관된 생물학적, 유전적 예측인자)

  • Kim, Yong-Ku
    • Korean Journal of Biological Psychiatry
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    • v.12 no.1
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    • pp.3-12
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    • 2005
  • Most suicides(about 90%) occur in the context of psychiatric disorders. Prediction of suicide risk in patients with mental illness is very important in preventing suicide attempts. However, current approaches to predict suicidality are based on clinical history and have low specificity and biological markers are not yet included. Many studies have explored the association between different biological parameters and suicidality. Studies of cerebro-spinal fluid(CSF) demonstrated that 5-HIAA and HVA levels were lower in patients with a history of suicide. Platelet serotonin transporter and the 5-HT2 serotonin receptor have also been studied in relation to violence and suicide. Depressive patients with greater suicidal tendency had significantly lower cholesterol concentrations but some researchers failed to find the correlation. DST non-supression is reported to predict suicidality in major depression. Several studies demonstrated a relationship between intron 7 polymorphism of tryptophan hydroxylase and suicidal behavior. Since suicide is not occurred in a single disease, the systematic and comprehensive study in large samples with various diagnoses is necessary to find the biological and genetic predictors of suicidal behavior.

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