LY-264086(LY-264086) - 药物靶点：COX-2 x LTB4R_专利_临床

概要

基本信息

药物类型

小分子化药

别名

3-[4-[7-carboxy-3-[decyloxy]-9-oxo-9H-xanthene]]propanoic acid

靶点

COX-2 x LTB4R

作用机制

COX-2抑制剂(环氧化酶-2抑制剂)、LTB4R拮抗剂(白三烯B4受体1拮抗剂)

治疗领域

免疫系统疾病呼吸系统疾病皮肤和肌肉骨骼疾病+ [1]

在研适应症-

非在研适应症

哮喘炎症银屑病

原研机构

Eli Lilly & Co.

在研机构-

非在研机构

Eli Lilly & Co.

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 LY-264086 相关的临床结果

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100 项与 LY-264086 相关的转化医学

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100 项与 LY-264086 相关的专利（医药）

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1

项与 LY-264086 相关的文献（医药）

1992-01-01·Receptor

Characterization of the spatial arrangement of the two acid-binding sites on the human neutrophil LTB4 receptor.

Article

作者: Jackson, W T ; Gapinski, D M ; Chaney, M O ; Froelich, L L ; Mallett, B E

A series of lipophilic benzophenone dicarboxylic acids have been shown to be inhibitors of the binding of LTB4 to its receptors on intact human neutrophils (Gapinski et al. (1990). Structure-activity relationships indicated that maximum activity was achieved when an acid group was attached at the meta position of each ring. In this report, the conformation of these inhibitors that binds best to the LTB4 receptor was determined. Inhibition concentration profiles of four rigid xanthone isomers that mimicked the four major conformational states of this type of benzophenone dicarboxylic acid were compared. LY264086, 3-[4-[7-carboxy-3-[decyloxy]-9-oxo-9H-xanthene]]propanoic acid, was the most potent inhibitor. The distance between the two carboxyl groups in this isomer was found to be 9.8 A, implying that the two acid binding sites on the receptor are separated by similar dimensions. Molecular modeling studies with low energy conformers of the xanthone isomers and LTB4 suggested a configuration of the agonist when it is bound to the receptor but did not exclude all other possibilities. These experiments further support the existence of two acid-binding sites on the human neutrophil LTB4 receptor.

100 项与 LY-264086 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
哮喘	药物发现	美国	Eli Lilly & Co.	1995-07-30
炎症	药物发现	美国	Eli Lilly & Co.	1995-07-30
银屑病	药物发现	美国	Eli Lilly & Co.	1995-07-30