Journal article
Yeast-based screening for inhibitors of RGS proteins
Methods in enzymology, v 389
01 Jan 2004
PMID: 15313572
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
This article provides information on two screening platforms for the identification of regulators of G-protein signaling (RGS) protein modulators. Utilization of the yeast pheromone response pathway enabled the creation of a functional screen for RGS4 modulators. The RGSZ1-focused screen employs advances in yeast two-hybrid screening technologies and targets the protein-protein interface of the RGS domain/Galpha interaction. Moreover, the RGSZ1 screen provides the opportunity to multiplex the screening of two targets of interest, given the development of two different luciferase reporter genes that enabled sequential determination and intraassay controls. The screen formats were validated, implemented, and conducted as automated 384-well, liquid-based, high-throughput small molecule screens. Primary "hits" were confirmed using benchtop 96-well formats of these assays and advanced to in vitro functional evaluation assays. The yeast-based assay platforms provide robust cellular assays that result in the identification of small molecule modulators for both RGS targets. These molecules can serve both as tools with which to probe biological implications of RGS proteins and as potential starting points toward the development of novel modulators of G-protein signaling pathways. Such modulators may show potential for controlling and treating diseases resulting from inappropriate activity of G-protein signaling pathways.
Metrics
Details
- Title
- Yeast-based screening for inhibitors of RGS proteins
- Creators
- Kathleen H YoungYuren WangCorey BenderSeena AjitFernando RamirezAdam GilbertBart W Nieuwenhuijsen
- Publication Details
- Methods in enzymology, v 389
- Publisher
- Elsevier
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- College of Medicine; Pharmacology and Physiology; Drexel University
- Web of Science ID
- WOS:000224271400017
- Scopus ID
- 2-s2.0-4344685294
- Other Identifier
- 991020100200904721
UN Sustainable Development Goals (SDGs)
This publication has contributed to the advancement of the following goals:
InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Web of Science research areas
- Biochemical Research Methods
- Biochemistry & Molecular Biology