Identification of Clausine E as an inhibitor of fat mass and obesity‐associated protein (FTO) demethylase activity

The alkaloids containing a carbazole nucleus are an established class of natural products with wide range of biological activities. A combination of thermodynamic and enzymatic activity studies provides an insight into the recognition of Clausine E by the fat mass and obesity‐associated protein (FTO...

Full description

Saved in:
Bibliographic Details
Published in:Journal of molecular recognition 2019-10, Vol.32 (10), p.e2800-n/a
Main Authors: Wang, Ying, Li, Junya, Han, Xinxin, Wang, Ning, Song, Chuanjun, Wang, Ruiyong, Chang, Junbiao
Format: Article
Language:English
Subjects:
Alkaloids
Binding
Body fat
Carbazole
Carbazoles
Clausine E
Enthalpy
Entropy
Enzymatic activity
fat mass and obesity‐associated protein
fluorescence
Hydroxyl groups
inhibitor
isothermal titration calorimetry
Natural products
Obesity
Proteins
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The alkaloids containing a carbazole nucleus are an established class of natural products with wide range of biological activities. A combination of thermodynamic and enzymatic activity studies provides an insight into the recognition of Clausine E by the fat mass and obesity‐associated protein (FTO). The binding of Clausine E to FTO was driven by positive entropy and negative enthalpy changes. Results also indicated that the hydroxyl group was crucial for the binding of small molecules with FTO. The structural and thermodynamic information provides the basis for the design of more effective inhibitors for FTO demethylase activity. The characteristics of the binding between Clausine E and the fat mass and obesity‐associated protein were investigated by physicochemical and spectroscopic techniques.
ISSN:0952-3499
1099-1352
DOI:10.1002/jmr.2800