DG172(DG172) - 药物靶点：PPARδ_专利_临床

概要

基本信息

药物类型

小分子化药

别名

(Z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile

靶点

PPARδ

作用机制

PPARδ激动剂(过氧化物酶体增殖物激活受体δ激动剂)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Philipps University of Marburg

在研机构

Philipps University of Marburg

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 DG172 相关的临床结果

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100 项与 DG172 相关的转化医学

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100 项与 DG172 相关的专利（医药）

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1

项与 DG172 相关的文献（医药）

2005-06-01·Biochimica et Biophysica Acta (BBA) - Biomembranes

Role of actin in the cAMP-dependent activation of sodium/glucose cotransporter in renal epithelial cells

Article

作者: Kuniaki Takagi ; Hitoshi Harada ; Akira Ikari

We examined whether actin filaments are involved in the cAMP-dependent activation of a high affinity sodium/glucose cotransporter (SGLT1) using epithelial expression systems. The expression of enhanced green fluorescent protein-tagged SGLT1 (EGFP-SGLT1) in Madin-Darby canine kidney (MDCK) cells was revealed by Western blotting and confocal laser microscopy. 8-Br-cAMP, a membrane permeable cAMP analog, enhanced [14C]-alpha-methyl glucopyranoside ([14C]-AMG) uptake. Both basal and 8-Br-cAMP-elicited [14C]-AMG uptakes were inhibited by N-(2{[3-(4-bromophenyl)-2-propenyl]-amino}-ethyl)-5-isoquinolinesulfonamide (H-89), a protein kinase A inhibitor, and cytochalasin D, an actin filament formation inhibitor. Furthermore, cytochalasin D inhibited the distribution of EGFP-SGLT1 at the apical surface. These results suggest that the EGFP-SGLT1 protein is functionally expressed in the apical membrane of MDCK cells, and is up-regulated by a cAMP-dependent pathway requiring intact actin filaments.

100 项与 DG172 相关的药物交易

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