KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic.
KNI-102, a novel tripeptide HIV protease inhibitor containing allophenylnorstatine as a transition-state mimic.
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KNI-102，一种新型三肽 HIV 蛋白酶抑制剂，含有别苯基去甲他汀作为过渡态模拟物。
DOI：
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发表时间：
1991
影响因子：
1.7
通讯作者：
Y. Kiso
中科院分区：
文献类型：
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作者：
T. Mimoto;J. Imai;Shigeki Tanaka;N. Hattori;S. Kisanuki;K. Akaji;Y. Kiso
含allophenylnorstatine的HIV-1蛋白酶抑制剂[Apns；（2S,3S）-3-氨基-2-羟基-4-苯基丁酸]-Pro （syn非对映体）是一种有效的高选择性过渡态模拟物。Z-Asn-Apns-Pro-NHBut （KNI-102）是唯一具有显著抗HIV活性的三肽，可能是最小尺寸的，可以有效地、选择性地抑制HIV蛋白酶。由于其简单的化学结构和稳定性，使其易于获得，因此对开发代谢稳定的抗艾滋病药物的研究具有重要价值。
HIV-1 protease inhibitors containing allophenylnorstatine [Apns; (2S,3S)-3-amino-2-hydroxy-4-phenylbutyric acid]-Pro (syn diastereomer) as a transition-state mimic were established to be potent and highly selective. Z-Asn-Apns-Pro-NHBut (KNI-102) is the only tripeptide exhibiting substantial anti-HIV activity and may be of minimum size for potent, selective inhibition of HIV protease. Ready availability due to its simple chemical structure and stability should make it valuable for studies of the development of metabolically stable anti-AIDS drugs.