Characterization of the solution conformations of leuprolide acetate.

Characterization of the solution conformations of leuprolide acetate.
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醋酸亮丙瑞林溶液构象的表征。

DOI:
10.1034/j.1399-3011.2002.21006.x
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发表时间:
2002
期刊:
The journal of peptide research : official journal of the American Peptide Society
影响因子:
--
通讯作者:
D. V. Vander Velde
D. V. Vander Velde
中科院分区:
--
文献类型:
--
作者:
J. Meyer;M. Manning;D. V. Vander Velde

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醋酸亮丙瑞林(pGlu-His-Trp-Ser-Tyr-d-Leu-Leu-Arg-Pro-NHEt)是一种高效的LHRH激动剂,具有广泛的临床应用。在不同的溶液条件下,它显示出完全不同的首选构象:两个低人口β-转角在水中,在TFE/水在低pH值的新生螺旋,和高人口β-转角在TFE/水在微酸性pH值。pH值相关的构象变化在TFE/水是由于pK(a)的乙酸盐的counterparts,而不是电离基团的肽。这些构象都与以前的计算预测不完全一致。
Leuprolide acetate (pGlu-His-Trp-Ser-Tyr-d-Leu-Leu-Arg-Pro-NHEt), a potent LHRH agonist in wide clinical use, was characterized conformationally by NMR and circular dichroism. It displayed quite different preferred conformations under different solution conditions: two low population beta-turns in water, a nascent helix in TFE/water at low pH, and a high population beta-turn in TFE/water at slightly acidic pH. The pH-related conformational change in TFE/water is attributed to the pK(a) of the acetate counterion, not to ionizable groups on the peptide. None of these conformations are in exact agreement with previous computational predictions.
DOI: 10.1021/bi9907936
发表时间: 1999-09-21
期刊: BIOCHEMISTRY
影响因子: 2.9
作者:
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通讯作者: White, SH
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发表时间: 1987
期刊: Biochemistry
影响因子: 2.9
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期刊: ENDOCRINE REVIEWS
影响因子: 20.3
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