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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [3]

Target

FXR

Mechanism

FXR antagonists(Bile acid receptor FXR antagonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Hyperlipidemias

Inactive Indication-

Originator Organization-

Active Organization

Zydus Lifesciences Ltd.

Inactive Organization-

Drug Highest PhasePhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC21H30O2

InChIKeyYLFRRPUBVUAHSR-SRJGTTDWSA-N

CAS Registry104010-41-5

Ayurveda, the ancient Indian system of health care and medicine, has a well-organized materia medica in which plants form a dominant part. A key illustration of the exploitation of this knowledge toward the development of a modern drug is the isolation and characterization of two antihyperlipidemic compounds, Z-, and E-guggulsterone from the tree Commiphora mukul, the exudate of which has been traditionally used for mitigating lipid disorders. Here, we demonstrate that Z-guggulsterone and an analog, 80-574 currently in clinical trials, act as antagonists of the bile acid receptor (BAR), a member of the intracellular receptor superfamily. These compounds antagonize the activity of BAR in vitro, and in cell culture systems on promoters and endogenous target genes. In biochemical assays, they are able to displace coactivator peptides from the receptor in a dose-dependent manner. The mechanism by which they act as BAR antagonists is likely through their inability to recruit coactivator proteins, failure to release corepressor proteins from unliganded receptor, and ability to compete with BAR agonists to block coactivator recruitment. Our data suggest these compounds may mediate at least some of their effects via the BAR.

100 Deals associated with Centatin

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