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aloin金蟲(chóng) (小有名氣)
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1、Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is a derivative of camptothecin. Irinotecan inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex, and causes double-strand DNA breakage and cell death. 2、Decitabine is indicated for treatment of patients with myelodysplastic syndrome (MDS). It is a chemical analogue of cytidine, a nucleoside present in DNA and RNA. Cells in the presence of Decitabine incorporate it into DNA during replication and RNA during transcription. The incorporation of Decitabine into DNA or RNA inhibits methyltransferase thereby causing demethylation in that sequence. This adversely affects the way that cell regulatory proteins are able to bind to the DNA/RNA substrate. 3、Pimecrolimus is a chemical that is used to treat atopic dermatitis (eczema). Atopic dermatitis is a skin condition characterized by redness, itching, scaling and inflammation of the skin. The cause of atopic dermatitis is not known; however, scientists believe that it may be due to activation of the immune system by various environmental or emotional triggers. Scientists do not know exactly how pimecrolimus reduces the manifestations of atopic dermatitis, but pimecrolimus reduces the action of T-cells and mast cells which are part of the immune system and contribute to responses of the immune system. Pimecrolimus prevents the activation of T-cells by blocking the effects of chemicals (cytokines) released by the body that stimulate T-cells. Pimecrolimus also reduces the ability of mast cells to release chemicals that promote inflammation. 4、Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor. 5、Everolimus is a derivative of Rapamycin (sirolimus), and works similarly to Rapamycin as an mTOR (mammalian target of rapamycin) inhibitor. It is currently used as an immunosuppressant to prevent rejection of organ transplants. In a similar fashion to other mTOR inhibitors Everolimus' effect is solely on the mTORC1 protein and not on the mTORC2 protein. |
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jingjing1005
木蟲(chóng) (小有名氣)
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aloin(金幣+95):謝謝 2010-05-26 10:23:19
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1伊立替康是主要用于治療結(jié)直腸癌的酶抑制劑抗腫瘤藥。伊立替康是喜樹(shù)堿的衍生物。伊立替康抑制拓?fù)洚悩?gòu)酶I的活動(dòng)，通過(guò)形成拓?fù)洚悩?gòu)酶I-DNA復(fù)合物阻止DNA單鏈連接成雙鏈DNA，并導(dǎo)致雙鏈DNA斷裂，最終導(dǎo)致細(xì)胞死亡。 2 地西他濱用于治療骨髓增生異常綜合征（MDS）。它是一種胞啶的化學(xué)類似物，存在于在DNA和RNA的核苷酸中。在地西他濱存在時(shí)，細(xì)胞分別通過(guò)復(fù)制過(guò)程和轉(zhuǎn)錄過(guò)程將它整合到DNA和RNA中，從而抑制甲基轉(zhuǎn)移酶的活性，導(dǎo)致該序列脫甲基化。這嚴(yán)重影響了細(xì)胞調(diào)節(jié)蛋白與DNA / RNA基質(zhì)的結(jié)合。 3吡美莫司是一種用于治療特應(yīng)性皮炎（濕疹）的藥物。異位性皮炎通常有皮膚發(fā)紅，發(fā)癢，魚(yú)鱗和發(fā)炎的癥狀。特應(yīng)性皮炎的發(fā)病原因尚不清楚，但科學(xué)家認(rèn)為它可能是由情緒因素或各種環(huán)境因素導(dǎo)致的免疫系激活引起的�？茖W(xué)家并不知道到底吡美莫司是如何緩解特應(yīng)性皮炎的癥狀的，但吡美莫司減少了T細(xì)胞和肥大細(xì)胞的活動(dòng)，這些細(xì)胞是免疫系統(tǒng)的一部分，并在免疫應(yīng)答過(guò)程中起著重要作用。吡美莫司可以阻斷人體分泌的化學(xué)分子（細(xì)胞因子）刺激T細(xì)胞活化的過(guò)程，同時(shí)它還可以抑制肥大細(xì)胞釋放化學(xué)物質(zhì)，從而減輕炎癥癥狀。 4，馱瑞塞爾Temsirolimus是一種mTOR(哺乳動(dòng)物的雷帕霉素作用靶點(diǎn))抑制劑，它可以與一種細(xì)胞內(nèi)蛋白(FKBP一12)相結(jié)合，這種蛋白-藥物結(jié)合物可以抑制mTOR控制細(xì)胞分裂。 mTOR可以磷酸化激活p70S6k和S6核糖體蛋白，mTOR下游區(qū)的磷脂酰肌醇激酶／AKT(PI3K／AKT)信號(hào)轉(zhuǎn)導(dǎo)通路被阻斷后，其活性將受到抑制可以使G期的腫瘤細(xì)胞生長(zhǎng)停滯。采用腎癌細(xì)胞為研究對(duì)象的體外研究表明，馱瑞塞爾可以抑制mTOR的活性并且降低缺氧誘導(dǎo)因子HIF—l、HIF一2a及血管內(nèi)皮生長(zhǎng)因子水平。 5依維莫司是雷帕霉素衍生物（西羅莫司），與雷帕莫司作用相似，是mTOR（雷帕莫司的作用靶點(diǎn)）的抑制劑。目前用作免疫抑制劑，以防止器官移植的排斥反應(yīng)。與其他mTOR抑制劑相比，依維莫司只作用于mTORC1蛋白，而對(duì)mTORC2蛋白沒(méi)有影響。 |
4樓2010-05-26 09:49:40
aloin
金蟲(chóng) (小有名氣)
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- 專業(yè): 天然藥物化學(xué)
2樓2010-05-25 23:15:11
aloin(金幣+5, 翻譯EPI+1):謝謝 2010-05-26 10:22:55
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我只是來(lái)學(xué)習(xí)的，樓主忽略我吧 antineoplastic抗腫瘤的 colorectal cancer大腸癌 camptothecin喜樹(shù)堿 topoisomerase拓?fù)洚悩?gòu)酶 religation重新連接 recombinant重組 DNA strand DNA鏈 myelodysplastic syndrome (MDS)骨髓增生異常綜合征，原名白血病前期preleukemia cytidine胞嘧啶 nucleoside核苷 incorporate合并、摻進(jìn) replication復(fù)制 transcription轉(zhuǎn)錄 methyltransferase甲基轉(zhuǎn)移酶 adversely affects不利影響 regulatory調(diào)節(jié) atopic dermatitis異位性皮膚炎 eczema濕疹 太晚了 都是些藥品簡(jiǎn)介 |
3樓2010-05-26 00:51:30
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