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抗癌肽H-Arg-D-Trp-NmePhe-D-Trp-Leu-Met-NH2的代谢

Metabolism of the anticancer peptide H-Arg-D-Trp-NmePhe-D-Trp-Leu-Met-NH2.

作者信息

Jones D A, Cummings J, Langdon S P, MacLellan A J, Higgins T, Rozengurt E, Smyth J F

机构信息

Imperial Cancer Research Fund, Medical Oncology Unit, Western General Hospital, Edinburgh, UK.

出版信息

Peptides. 1995;16(5):777-83. doi: 10.1016/0196-9781(95)00048-o.

DOI:10.1016/0196-9781(95)00048-o
PMID:7479315
Abstract

H-Arg-D-Trp-NmePhe-D-Trp-Leu-Met-NH2 (Antagonist G) will be the first broad-spectrum neuropeptide antagonist to enter a phase I clinical trial. Its in vitro and in vivo metabolism has been extensively characterized. The major metabolites were identified and their structures elucidated by mass spectroscopy and amino acid analysis. Metabolism occurred almost exclusively at the C-terminus and was arrested by phenylmethylsulfonylfluoride, a known serine-protease inhibitor. Biological characterization of the metabolites demonstrated that the degradation of Antagonist G produces metabolites that retain neuropeptide antagonist properties.

摘要

H-精氨酸-D-色氨酸-N-甲基苯丙氨酸-D-色氨酸-亮氨酸-甲硫氨酸-氨基（拮抗剂G）将成为首个进入I期临床试验的广谱神经肽拮抗剂。其体外和体内代谢情况已得到广泛研究。通过质谱分析和氨基酸分析鉴定出了主要代谢产物，并阐明了它们的结构。代谢几乎仅发生在C端，且被已知的丝氨酸蛋白酶抑制剂苯甲基磺酰氟所抑制。对代谢产物的生物学特性研究表明，拮抗剂G的降解产生的代谢产物仍保留神经肽拮抗剂特性。

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Metabolism of the broad-spectrum neuropeptide growth factor antagonist: [D-Arg1, D-Phe5, D-Trp7,9, Leu11]-substance P.
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