Next Article in Journal
Sequence-Based Analysis of Structural Organization and Composition of the Cultivated Sunflower (Helianthus annuus L.) Genome
Next Article in Special Issue
Advanced Cell Culture Techniques for Cancer Drug Discovery
Previous Article in Journal
Body Size Shifts in Philippine Reef Fishes: Interfamilial Variation in Responses to Protection
Previous Article in Special Issue
In Vitro High Throughput Screening, What Next? Lessons from the Screening for Aurora Kinase Inhibitors
Article Menu

Export Article

Open AccessReview

Screening for Antifibrotic Compounds Using High Throughput System Based on Fluorescence Polarization

College of Medicine, Florida State University, 1115 W. Call St., Tallahassee, FL 32306, USA
Author to whom correspondence should be addressed.
Biology 2014, 3(2), 281-294;
Received: 15 January 2014 / Revised: 28 February 2014 / Accepted: 1 April 2014 / Published: 10 April 2014
(This article belongs to the Special Issue Screening for Biologically Active Compounds)
PDF [931 KB, uploaded 10 April 2014]


Fibroproliferative diseases are one of the leading causes of death worldwide. They are characterized by reactive fibrosis caused by uncontrolled synthesis of type I collagen. There is no cure for fibrosis and development of therapeutics that can inhibit collagen synthesis is urgently needed. Collagen α1(I) mRNA and α2(I) mRNA encode for type I collagen and they have a unique 5' stem-loop structure in their 5' untranslated regions (5'SL). Collagen 5'SL binds protein LARP6 with high affinity and specificity. The interaction between LARP6 and the 5'SL is critical for biosynthesis of type I collagen and development of fibrosis in vivo. Therefore, this interaction represents is an ideal target to develop antifibrotic drugs. A high throughput system to screen for chemical compounds that can dissociate LARP6 from 5'SL has been developed. It is based on fluorescence polarization and can be adapted to screen for inhibitors of other protein-RNA interactions. Screening of 50,000 chemical compounds yielded a lead compound that can inhibit type I collagen synthesis at nanomolar concentrations. The development, characteristics, and critical appraisal of this assay are presented. View Full-Text
Keywords: fibrosis; antifibrotic drugs; RNA binding protein; fluorescence polarization fibrosis; antifibrotic drugs; RNA binding protein; fluorescence polarization

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Share & Cite This Article

MDPI and ACS Style

Stefanovic, B.; Stefanovic, L. Screening for Antifibrotic Compounds Using High Throughput System Based on Fluorescence Polarization. Biology 2014, 3, 281-294.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Biology EISSN 2079-7737 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top