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00:00
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Slide 0
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00:06
2.
HIV-1&-2 (RNA virus)
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01:56
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病毒的蛋白gp41與gp120。gp41是跨膜蛋白,gp120位於表面;gp41和gp120會結合,就長得像棒棒糖一樣。
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08:27
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Antiretroviral agents
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11:57
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Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
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14:13
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Nucleoside reverse transcriptase inhibitors (NRTI)
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15:39
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Mechanism of action of NRTIs
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17:29
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核苷反轉錄酶抑制劑
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18:48
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Mechanism of action of NRTIs
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20:42
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Abacavir
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23:33
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藥物基因體學(Pharmacogenomics):基因和藥物反應的關係。
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25:11
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Mechanism of action of NRTIs
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26:28
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Mechanism of action of NRTIs
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27:27
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Mechanism of action of NRTIs
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28:45
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Mechanism of action of NRTIs
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30:00
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Mechanism of action of NRTIs
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31:17
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Nucleotide reversetranscriptase inhibitors (NtRTI)
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31:21
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Nucleotide reversetranscriptase inhibitors (NtRTI)
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32:10
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Tenofovir disoproxil fumarate
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33:31
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核苷與核苷酸反轉錄酶抑制劑
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35:14
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Non-nucleoside reversetranscriptase inhibitors(NNRTI)
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37:08
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Slide 48
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37:41
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NNRTIs
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39:31
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可直接與反轉錄酶結合,藉由破壞酵素作用部位,阻斷具RNA 依賴性和DNA 依賴性的DNA 聚合酶活性,從而抑制病毒的繁殖。作用機制:inactive反轉錄酶。(抑制Reverse transcriptase) 結合在反轉錄酶活性區附近的疏水區(target at an allosteric “pocket”),引起其催化部位構型上的變化,直接使反轉錄酶被抑制(direct inactivate the enzyme),屬於非競爭的抑制作用。 NNRTIs (非核苷反轉錄酶抑制劑)與 NRTIs 不同之處在
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42:21
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NNRTI
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44:03
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NNRTI
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45:34
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All of them are macromolecules PI competitively binds to the active site HIV protease and prevents it from cleaving the pro-form of viral proteins into the working machinery of the virus. If the HIV protease enzyme does not work, the virus is not infectio
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50:49
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蛋白酶抑制劑 ( Protease inhibitors, PIs)
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53:18
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Slide 55
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53:36
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Darunavir
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54:24
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蛋白酶抑制劑 ( Protease inhibitors)
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55:05
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Protease inhibitors
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57:40
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脂肪營養不良
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58:53
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Protease inhibitors
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58:55
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蛋白酶抑制劑 ( Protease inhibitors)
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58:56
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Protease inhibitors
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58:56
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脂肪營養不良
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1:00:28
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Protease inhibitors
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1:00:45
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脂肪營養不良
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1:00:46
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IndinavirSide effect: Hyperbilirubinemia, nephrolithiasis (腎結石), nausea, diarrhea, headache, blurred vision, serum aminotransferase Metabolic alterations including hyperlipidemia (cholesterol or triglyceride elevations) and hyperglycemiaLopinavirOnly
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1:02:55
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Ritonavir: a potent inhibitor of CYP3A4 as a pharmacologic booster. It is often used to inhibit the enzyme that metabolizes other protease inhibitors. This inhibition leads to higher concentrations of these latter medication.Side effect: asthenia, GI dist
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1:06:36
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Fusion inhibitor
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1:06:54
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病毒的蛋白gp41與gp120。gp41是跨膜蛋白,gp120位於表面;gp41和gp120會結合,就長得像棒棒糖一樣。
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1:06:58
44.
Fusion inhibitor
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1:07:00
45.
病毒的蛋白gp41與gp120。gp41是跨膜蛋白,gp120位於表面;gp41和gp120會結合,就長得像棒棒糖一樣。
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1:07:25
46.
Mechanism of action: binds to the gp41 subunit of the viral envelop glycoprotein, preventing the conformational changes required for the fusion of the viral and cellular membranes→ Enfuvirtide是一個HIV-1 gp41結構重組的抑制劑 (gp41是virus-cell fusion所必須)。 藥物阻斷融合蛋白(fus
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1:08:38
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Viral entry inhibitor
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1:10:36
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Viral entry inhibitor-1
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1:12:49
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Integrase strand transfer inhibitor (INSTIs)
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1:15:55
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雞尾酒療法HAART
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1:18:21
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雞尾酒療法HAART
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1:20:18
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Slide 70