Journal article
Identification of ligands targeting RGS proteins high-throughput screening and therapeutic potential
Progress in molecular biology and translational science, Vol.86, pp.335-356
2009
DOI: 10.1016/S1877-1173(09)86011-0
PMID: 20374721
Abstract
Regulator of G protein signaling (RGS) proteins represent unique targets for the modulation of G protein-coupled receptor-mediated signal transduction cascades. Functionally, RGS proteins act to limit the duration of signaling of activated G proteins due to its ability to act as GTPase activating proteins (GAPs). This GAP activity catalyzes the intrinsic GTPase activity of G protein α subunits, such as those in the Gαo, Gαi, and Gαq families. Because of their unique regulatory properties, RGS proteins have emerged as an interesting target for development of both small molecule laboratory tools and potential future therapeutics. In this chapter, the utility of RGS modulators will be briefly reviewed, with a main focus on high-throughput screening methods and progress being made to discover new RGS ligands.
Details
- Title: Subtitle
- Identification of ligands targeting RGS proteins high-throughput screening and therapeutic potential
- Creators
- David L Roman - Division of Medicinal and Natural Products Chemistry, The University of Iowa College of Pharmacy, Iowa City, Iowa 52242, USA
- Resource Type
- Journal article
- Publication Details
- Progress in molecular biology and translational science, Vol.86, pp.335-356
- Publisher
- Netherlands
- DOI
- 10.1016/S1877-1173(09)86011-0
- PMID
- 20374721
- ISSN
- 1877-1173
- eISSN
- 1878-0814
- Language
- English
- Date published
- 2009
- Academic Unit
- Pharmacy; Iowa Neuroscience Institute; Pharmaceutical Sciences and Experimental Therapeutics; Medicinal and Natural Products Chemistry
- Record Identifier
- 9984065387102771
Metrics
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