NDLI: Metabolic stability of long-acting luteinizing hormone-releasing hormone antagonists

Content Provider	Springer Nature Link
Author	Yao, Jin Feng Zhou, Ning Lv, Yu Jian Zhang, Ruifeng Liu, Ke Liang Xue, Ming
Copyright Year	2012
Abstract	Long-acting luteinizing hormone-releasing hormone (LHRH) antagonists designed to be protease resistant consisted of a series of novel decapeptides structurally similar to LHRH. The aim of this study was to evaluate the in vitro metabolic stability of the LHRH decapeptides using pancreatin and homogenates models and identify the metabolites in rat liver homogenate for the purpose of illustrating the metabolic features of the decapeptides. The major metabolites in rat liver homogenate were identified by LC–ESI-MSn. The half-lives of the 11 LHRH decapeptides were from 44 to 330 min in the pancreatin model. The half-lives of the five decapeptides in rat liver, kidney and lung homogenates were between 8 and 462 min. The most stable decapeptides were the LY616 and LY608 peptides with half-lives of 36 min in liver homogenate. Two major cleavage sites were found by analysing the metabolites of the LY618 peptide in rat liver homogenate, between the Pal3-Ser4 and the Leu7-Ilys8 peptide bonds. The major metabolites were produced via cleavages of peptide bonds at these sites, and further metabolic reactions such as hydroxylation, oxidative dechlorination, alcohol dehydration and isopropyl dealkylation were also observed.
Starting Page	1557
Ending Page	1566
Page Count	10
File Format	PDF
ISSN	09394451
Journal	Amino Acids
Volume Number	43
Issue Number	4
e-ISSN	14382199
Language	English
Publisher	Springer Vienna
Publisher Date	2012-02-08
Publisher Place	Vienna
Access Restriction	Subscribed
Subject Keyword	Luteinizing hormone-releasing hormone Antagonists Degradation Kinetics Cleavage site Mass spectrometry Proteomics Life Sciences Neurobiology Biochemistry Biochemical Engineering Analytical Chemistry
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Biochemistry Clinical Biochemistry

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