Inhibition of recombinant dipeptidyl peptidase III by synthetic hemorphin-like peptides
Inhibition of recombinant dipeptidyl peptidase III by synthetic hemorphin-like peptides
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DOI：
10.1016/s0196-9781(03)00119-0
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发表时间：
2003-05-01
期刊：
影响因子：
3
通讯作者：
Matsui, N
中科院分区：
文献类型：
--
作者：
Chiba, T;Li, YH;Matsui, N
为了寻找最有效的二肽基肽酶III降解脑啡肽的拮抗剂，我们合成了N端具有脂肪族或芳香族氨基酸的类血吗啡五肽，如VVYPW、LVYPW、IVYPW、YVYPW、FVYPW和WVYPW。在这些五肽中，IVYPW和WVYPW对rDPP III表现出最强的抑制活性。 IVYPW和WVYPW的K-i值分别为0.100+/-0.011和0.126+/-0.015μM（平均值+/-S.E.）。 Ki值的顺序为Ile大于或等于Trp>Phe大于或等于Tyr>Leu>Ala>Val>Ser>Gly。这些肽以非竞争性方式抑制 rDPP III 活性。肽VYPW不抑制rDPP III活性，但该序列对于抑制活性的表达是必需的。 (C) 2003 Elsevier Inc. 保留所有权利。
In order to find the most effective antagonist for dipeptidyl peptidase III degrading enkephalin, we synthesized hemorphin-like pentapeptides with aliphatic or aromatic amino acids at the N-termini, such as VVYPW, LVYPW, IVYPW, YVYPW, FVYPW and WVYPW. Among those pentapeptides, IVYPW and WVYPW showed the strongest inhibitory activity toward rDPP III. The K-i values of IVYPW and WVYPW were 0.100+/-0.011 and 0.126+/-0.015 muM (mean+/-S.E.), respectively. The order of Ki values was Ile greater than or equal to Trp > Phe greater than or equal to Tyr > Leu > Ala > Val > Ser > Gly. rDPP III activity is inhibited in a non-competitive manner by these peptides. The peptide VYPW did not inhibit rDPP III activity, but the sequence is essential for the expression of inhibitory activity. (C) 2003 Elsevier Inc. All rights reserved.