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Delavirdine

地拉韋啶

Mechanism of action:

Delavirdine 屬於非核苷類反轉錄酶抑制劑(non-nucleoside reverse transcriptase inhibitor)。Delavirdine 會與 HIV-1 病毒反轉錄酶的疏水性非活性位點(allosteric site)結合,改變蛋白質構型,使酶活性降低,阻止病毒 RNA 反轉錄為 DNA。僅對 HIV-1 有效。

​Reference(s):

1. Geitmann M et al. (2006). Biosensor-based kinetic characterization of the interaction between HIV-1 reverse transcriptase and non-nucleoside inhibitors. J Med Chem. 


2. Xia Q et al. (2007). Probing nonnucleoside inhibitor-induced active-site distortion in HIV-1 reverse transcriptase by transient kinetic analyses. Protein Sci. 


3. Freimuth WW et al. (1996). Delavirdine mesylate, a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Adv Exp Med Biol.

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