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Antagonistic peptides of prostaglandin E2 receptor subtype EP4

机译:前列腺素E2受体亚型EP4的拮抗肽

摘要

Antagonistic peptides of prostaglandin E2 receptor subtype EP4 and their use in the treatment or prevention of medical conditions associated with oligouric nephropathy, bone resorption, abnormal intestinal crypt cell proliferation or patency of the ductus arteriosus and the like are provided herein. The antagonistic peptides of the present invention can include the following formula:X-A-private use character ParenopenstRprivate use character ParenclosestnYm wherein “X” is a hydrogen atom or an amine protecting group producing a carbamate or an amide when reacting with the amine; “A” is L-(4,4′)-biphenylalanine or D-(4,4′)-biphenylalanine; “R” is an amino acid selected from the group consisting of threonine, serine, tyrosine, glutamic acid, alanine, leucine and glycine; “Y” is lysine; “n” is an integer ranging from 5 to 7; and “m” is an integer ranging from 0 to 2.
机译:本文提供了前列腺素E 2受体亚型EP 4的拮抗肽及其在治疗或预防与寡尿性肾病,骨吸收,肠隐窝细胞异常增殖或动脉导管通畅等有关的医学病症中的用途。本发明的拮抗肽可以包括下式:<?in-line-formulae description =“ In-line Formulae” end =“ lead”?> XA- <图像alt =“私人使用字符Parenopenst” file =“ US07414029-20080819-PARENOPENST.GIF” he =“ 7.20mm “ id =“ PRIVATE-USE-CHARACTER-00001” imgContent =“ character” imgFormat =“ GIF” wi =“ 8.47mm” /> R “私人使用字符Parenclosest” n Y m <?in-line-formulae description =“ In-line Formulae” end =“ tail”?>其中“ X”是氢原子或与胺反应时产生氨基甲酸酯或酰胺的胺保护基; “ A”是L-(4,4')-联苯丙氨酸或D-(4,4')-联苯丙氨酸; “ R”是选自苏氨酸,丝氨酸,酪氨酸,谷氨酸,丙氨酸,亮氨酸和甘氨酸的氨基酸; “ Y”是赖氨酸; “ n”为5至7的整数; “ m”为0〜2之间的整数。

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