Design, Synthesis, and Initial Evaluation of Affinity-Based Small-Molecule Probes for Fluorescent Visualization and Specific Detection of Keap1

Mengchen Lu; Hai-Shan Zhou; Qi-Dong You; Zhengyu Jiang

doi:10.1021/acs.jmedchem.6b00775

Design, Synthesis, and Initial Evaluation of Affinity-Based Small-Molecule Probes for Fluorescent Visualization and Specific Detection of Keap1

J Med Chem. 2016 Aug 11;59(15):7305-10. doi: 10.1021/acs.jmedchem.6b00775. Epub 2016 Jul 22.

Authors

Mengchen Lu¹, Hai-Shan Zhou¹, Qi-Dong You^{1

2}, Zhengyu Jiang^{1

2}

Affiliations

¹ State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization, China Pharmaceutical University , Nanjing 210009, China.
² Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University , Nanjing 210009, China.

PMID: 27409246
DOI: 10.1021/acs.jmedchem.6b00775

Abstract

Keap1 is a pluripotent protein which plays a predominant role in cellular homeostasis and stress responses. Given that the cellular environment is quite dynamic and versatile, further investigation of the function of Keap1 depends on tools for specific and real-time detection of Keap1. Herein, we report the development of functional affinity-based small-molecule probes which can overcome some shortcomings of current methods and be applied in further studying the function of Keap1.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cell Line
Dose-Response Relationship, Drug
Drug Design*
Fluorescent Dyes / chemistry*
Fluorescent Dyes / pharmacology
Humans
Kelch-Like ECH-Associated Protein 1 / analysis*
Kelch-Like ECH-Associated Protein 1 / antagonists & inhibitors
Molecular Structure
Small Molecule Libraries / chemistry*
Small Molecule Libraries / pharmacology
Structure-Activity Relationship

Substances

Fluorescent Dyes
KEAP1 protein, human
Kelch-Like ECH-Associated Protein 1
Small Molecule Libraries