• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
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• pp.185-185
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• 2001

The CD95 (Fas, APO-1) is known to play a key role as a transmembrane cell surface receptor that mediates apoptosis of many cell types through binding with Fas ligand or cross-linking to agonistic anti-Fas antibody. Activation of CD95 provokes a potent and rapid responses in a variety of cell types by unknown mechanism.(omitted)

• Archives of Pharmacal Research
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• 제28권2호
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• pp.142-150
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• 2005

The synthesis and structure-activity relationships of a novel series of substituted quercetins that activates peroxisome proliferator-activated receptor gamma ($PPAR{\gamma}$) are reported. The $PPAR{\gamma}$ agonistic activity of the most potent compound in this series is comparable to that of the thiazolidinedione-based antidiabetic drugs currently in clinical use.

• Bulletin of the Korean Chemical Society
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• 제31권6호
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• pp.1501-1505
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• 2010

We report design and synthesis of the novel TRPV1 ligands through a rational approach. Simplified analogues of 12(S)-HPETE showing TRPV1 agonistic effect are disclosed. Biological evaluation revealed that substitution of functional groups without any change in conformation converted agonist into antagonist. Our work provided key information with regard to TRPV1 agonist/antagonist switching.

• 한국지능정보시스템학회:학술대회논문집
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• 한국지능정보시스템학회 2005년도 춘계학술대회
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• pp.169-185
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• 2005

신경계의 뉴런 구조는 흥분 뉴런과 억제 뉴런으로 구성되며 각각의 흥분 뉴런과 억제 뉴런은 주동근 뉴런(agonistic neuron)에 의해 활성화되며 길항근 뉴런(antagonist neuron)에 의해 비활성화 된다. 본 논문에서는 인간 신경계의 생리학적 뉴런 구조를 분석하여 퍼지 논리를 이용한 생리학적 퍼지 신경망을 제안한다. 제안된 구조는 주동근 뉴런에 의해 흥분 뉴런이 될 수 있는 뉴런들을 선택하여 흥분시켜 출력층으로 전달하고 나머지 뉴런들을 억제시켜 출력층에 전달시키지 않는다. 신경계를 기반으로 한 제안된 생리학적 퍼지 신경망의 학습구조는 입력층, 학습 데이터의 특징을 분류하는 중간층, 그리고 출력층으로 구성된다. 제안된 퍼지 신경망의 학습 및 인식 성능을 평가하기 위해 정확성이 요구되는 의학의 한 분야인 기관지 편평암 영상인식과 영상 인식의 주요 응용 분야인 차량 번호판 인식에 적용하여 기존의 신경망과 성능을 비교 분석하였다. 실험 결과에서는 제안된 생리학적 퍼지 신경망이 기존의 신경망보다 학습 시간과 수렴성이 개선되었을 뿐만 아니라, 인식에 있어서도 우수한 성능이 있음을 확인하였다.

• Translational and Clinical Pharmacology
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• 제26권3호
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• pp.115-117
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• 2018

This tutorial explains the basic principles of mechanistic ligand-receptor interaction model, which is an operational model of agonism. A growing number of agonist drugs, especially immune oncology drugs, is currently being developed. In this tutorial, time-dependent ordinary differential equation for simple $E_{max}$ operational model of agonism was derived step by step. The differential equation could be applied in a pharmacodynamic modeling software, such as NONMEM, for use in non-steady state experiments, in which experimental data are generated while the interaction between ligand and receptor changes over time. Making the most of the non-steady state experimental data would simplify the experimental processes, and furthermore allow us to identify more detailed kinetics of a potential drug. The operational model of agonism could be useful to predict the optimal dose for agonistic drugs from in vitro and in vivo animal pharmacology experiments at the very early phase of drug development.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.135.2-135.2
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• 2003

Plasma membrane blebs are observed in many types of apoptotic cells, but their processes of formation remain to be clarified. In the present study, we investigated whether there is a relationship between change of intracellular phosphotyrosine levels and biochemical apoptotic events in Jurkat T cells undergoing apoptosis by agonistic anti-Fas antibody. When Jurkat cells were treated with Fas-antibody in the presence or absence of pretreatment with sodium orthovanadate ($Na_3${VO}_4$), a phosphotyrosine phosphatase (PTPase) inhibitor, membrane blebs disappeared in orthovanadate-treated cells. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.350.1-350.1
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• 2002

A series of diaralkylthiourea derivatives was prepared and tested for its antagonistic activity against vanilloid receptor. In this study we explored the possibility of selected compound type (Ⅰ) with tetrahydronaphthyl group as rigid pendant moiety. Our premise for antagonistic activity of molecules was modeled on the capsazepine. the first antagonist for vanilloid receptor. These compounds (Ⅰ) showed less potent antagonistic activity than that of capsazepine. but they were devoid of agonistic activity. (omitted)

• 대한약리학회지
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• 제26권2호
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• pp.167-176
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• 1990

비스테로이드성 항에스트로젠제는 표적기관에서 estrogen 수용체와 상경적으로 결합하므로써 estrogen의 작용을 억제하는 것으로 알려져 있다. 비스테로이드성 항에스트로젠제는 대체로 triphenylethylene계로서 tamoxifen, clomiphene, LYl17018등이 있으며 표적기관에서 estrogen의 작용을 억제하기 때문에 estrogen과 관련된 질환을 치료하는데 이용되어 오고 있다. 본 연구에서는 생후 21-23일된 미성숙 흰쥐를 재료로 항에스트로젠제중 tamoxifen과 LY117018이 자궁세포 성장에 어떠한 영향을 미치며 어떠한 기전으로 estrogen의 작용을 길항하는지를 규명하고자, 항에스트로젠제가 estrogen작용의 중요 지포에 미치는 영향을 비교 관찰하여 다음과 같은 결과를 얻었다. Tamoxifen과 LY117018은 자궁세포에서 estrogen의 영향이 없는 경우에는 estrogen agonist로, estrogen작용하에서는 estrogen antagonist로서 작용하였다. Estrogen 작용의 여러 가지 지표에 대해 tamoxifen이 LY117018보다 agonistic effect는 더 컸으나, antagonistic effect는 LY117018이 더 큰 것으로 나타났다. Estrogen 수용체에 대한 결합능은 LY117018이 estradiol보다는 약간 낮았으나 용량에 비례하여 estrogen 수용체와 결합하였다. 그러나 tamoxifen은 estrogen 수용체에 대한 결합이 아주 낮았다. Estrogen 수용체에 대한 binding affinity는 estradiol(100%), LY117018(77%), tamoxifen(6.3%) 순으로 나타났다. 항에스트로젠제의 생체내 투여는 estrogen 존재 유무에 따라 estrogen 수용체 농도에 agonist 또는 antagonist로 작용하였다. 항에스트로젠제의 단독투여는 progesterone 수용체 생성을 증가시키나, estrogen에 의하여 유도된 progesterone 수용체 생성을 억제하였다. 이상의 결과로 보아, tamoxifen과 LY117018은 estrogen유무에 따라 흰쥐 자궁세포에서 estrogen antagonist로서 뿐만 아니라 agonist로서도 작용함을 알 수 있다. 그러나 estrogen수용체와의 결합능력이 아주 낮은 tamoxifen은, 용량에 비례하여 estrogen수용체에 결합하므로써 작용하는 LY117018과는 다른 기전으로 작용하는 것으로 생각된다.

• Asian-Australasian Journal of Animal Sciences
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• 제24권5호
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• pp.707-712
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• 2011

The objective of the present study was to determine gender-related and month-related behavioral differences in captive alpine musk deer. The study was conducted at Xinglongshan Musk Deer Farm (XMDF) of Xinglongshan National Nature Reserve in Gansu Province of western China. The integrated method of focal sampling and all occurrence recording was utilized to quantify the behavioural patterns of 45 captive alpine musk deer (Moschus sifanicus) during non-mating season (from August $1^{st}$ to October $25^{th}$), and the behavioural durations of 12 behavioural patterns such as standing-gazing were recorded. The behavioural modes were compared to explore the potential differences between females and males, and the monthly behavioural modes for males and females were analyzed. Our results showed that the captive female deer in XMDF could compensate the energy lost in pregnancy, parturition and lactation through improving its ingestive efficiency. In order to be more sensitive to the changing environment, females expressed more standing-gazing (SG: $67.38{\pm}12.69\;s$) and moving (MO; $27.41{\pm}5.02\;s$), but less bedding (BE: $42.32{\pm}11.35\;s$) than male deer (SG: $56.43{\pm}9.19\;s$; MO: $19.23{\pm}4.64\;s$; BE: $96.14{\pm}15.71\;s$). Furthermore, females perform more affinitive interaction (AI: $7.89{\pm}4.81\;s$) but less ano-genital sniffing (AS: $0.24{\pm}0.13\;s$) and agonistic behaviour (CI: $0.57{\pm}0.26\;s$) than males (AI: $1.45{\pm}1.09\;s$; AS: $0.45{\pm}0.29\;s$; CI: $1.42{\pm}0.67\;s$). The females expressed ingestion more in October ($132.31{\pm}27.47\;s$) than in August ($28.80{\pm}18.44\;s$) and September ($45.1{\pm}10.84\;s$), and the males performed Ano-genital sniffing (AS: $1.79{\pm}1.14\;s$) and self-directed behaviour (SD: $12.61{\pm}5.03\;s$) significantly more in October than in August (AS: 0 s; SD: $0.62{\pm}0.17\;s$) and September (AS: $0.02{\pm}0.01\;s$; SD: $0.17{\pm}0.15\;s$). Moreover, male musk deer increased the intension of ano-genital sniffing, agonistic behaviour and tail rubbing behaviour, which were related to sexual activities.

• 한국발생생물학회지:발생과생식
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• 제20권4호
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• pp.315-329
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• 2016

Fas ligand (FasL) and its receptor Fas have been implicated in granulosa cell apoptosis during follicular atresia. Although interferon-gamma (IFN-${\gamma}$) is believed to be involved in the regulation Fas expression in differentiated granulosa or granulosa-luteal cells, the expression of this cytokine and its role in the regulation of the granulosa cell Fas/FasL system and apoptosis during follicular maturation have not been thoroughly investigated. In the present study, we have examined the presence of IFN-${\gamma}$ in ovarian follicles at different stage of development by immunohistochemistry and related their relative intensities with follicular expression of Fas and FasL, and with differences in granulosa cell sensitivity to Fas activation by exogenous agonistic Anti-Fas monoclonal antibody (Fas mAb). Although IFN-${\gamma}$ immunostaining was detectable in oocyte and granulosa cells in antral follicles, most intense immunoreactivity for the cytokine was observed in these cells of preantral follicles. Intense immunoreactivity for IFN-${\gamma}$ was most evident in granulosa cells of atretic early antral follicles where increased Fas and FasL expression and apoptosis were also observed. Whereas low concentrations of IFN-${\gamma}$ (10-100 U/mL) significantly increased Fas expression in undifferentiated granulosa cells (from preantral or very early antral follicles) in vitro, very higher concentrations (${\geq}1,000U/mL$) were required to up-regulate of Fas in differentiated cells isolated from eCG-primed (antral) follicles. Addition of agonistic Fas mAb to cultures of granulosa cells at the two stages of differentiation and pretreated with IFN-${\gamma}$ (100 U/mL) elicited morphological and biochemical apoptotic features which were more prominent in cells not previously exposed to the gonadotropin in vivo. These findings suggested that IFN-${\gamma}$ is an important physiologic intra-ovarian regulator of follicular atresia and plays a pivotal role in regulation of expression of Fas receptor and subsequent apoptotic response in undifferentiated (or poorly differentiated) granulosa cells at an early (penultimate) stage of follicular development.