The study and synthesis of N-acetyl-leucyl-leucyl-norleucinal derivatives

碩士 === 國立成功大學 === 臨床藥學研究所 === 90 === 英文摘要 P-glycoprotein (Pgp), the multidrug resistance gene (mdr1) product, reduces the intracellular accumulation of a variety of drugs by pumping drugs out of membranes. Studies have demonstrated that hydrophobic tripeptides N-acetyl- leucyl- leucyl-norleucinal (...

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Bibliographic Details
Main Authors: Chung-Yee Shieh, 謝忠益
Other Authors: Shen-Fang Su
Format: Others
Language:zh-TW
Published: 2002
Online Access:http://ndltd.ncl.edu.tw/handle/y5u4jc
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Summary:碩士 === 國立成功大學 === 臨床藥學研究所 === 90 === 英文摘要 P-glycoprotein (Pgp), the multidrug resistance gene (mdr1) product, reduces the intracellular accumulation of a variety of drugs by pumping drugs out of membranes. Studies have demonstrated that hydrophobic tripeptides N-acetyl- leucyl- leucyl-norleucinal (ALLN), N-acetyl- leucyl-leucyl-methiminal (ALLM) and N-acetyl-leucyl-leucyl-arginal (leupeptin) are Pgp substrates/inhibitors. We would like to synthesize a series of tripeptides (N-acetyl-leu-leu-X ) and to study the interaction between the tripeptides and Pgp. We employ liquid-phase peptide synthesis method to obtain. We synthesize the N-acetyl-leucyl-leucine benzyl、N-acetyl-leucyl-leucine、N-acetyl-leucyl-leucyl-tryptophanol、N-acetyl-leucyl-leucyl-CBZ-lysinol、 N-acetyl-leucyl-leucyl-phenylalaninol.