Synthesis and biological evaluation of a novel pyroglutamyl-modified TRH analogue
Synthesis and biological evaluation of a novel pyroglutamyl-modified TRH analogue
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DOI：
10.1016/s0014-827x(02)01232-6
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发表时间：
2002-06-01
期刊：
影响因子：
--
通讯作者：
Spirito, A
中科院分区：
文献类型：
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作者：
Brunetti, L;Cacciatore, I;Spirito, A
TRH 类似物 3 已合成，并通过 H-1 和 C-13 NMR 充分表征，其中掺入 (S)-异噻唑烷-1,1-二氧化物-3-羧酸 (I) 部分代替天然 L-焦谷氨酸 (pGlu) 残基。已经研究了用磺酰胺对应物替代 pGlu 对生物活性的影响。该肽对 I 型焦谷氨酰肽酶（PP I，EC 3.4.19.3）的水解具有显着的稳定性，已显示出可维持体外催乳素释放活性。 (C) 2002 年科学与医学版 Elsevier SAS。版权所有。
The TRH analogue 3, incorporating the (S)-isothiazolidine-1,1-dioxide-3-carboxylic acid (I) moiety in place of the native L-pyroglutamic acid (pGlu) residue, has been synthesized and fully characterized by H-1 and C-13 NMR. The effects of replacing pGlu with its sulphonamido counterpart on biological activity have been investigated. This peptide, which is significantly stabilized towards hydrolysis by pyroglutamyl peptidase type I (PP I, EC 3.4.19.3), has shown to maintain in vitro prolactin-releasing activity. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.