| Literature DB >> 35773586 |
Pawel Krawinski1, Martin Caffrey2.
Abstract
G protein-coupled receptors (GPCRs) play vital roles in human physiology and pathophysiology. This makes the elucidation of the high-resolution blueprints of these high value membrane proteins of crucial importance for the structure-based design of novel therapeutics. However, the production and crystallization of GPCRs for structure determination comes with many challenges.In this chapter, we provide a comprehensive protocol for expressing and purifying the thromboxane A2 receptor (TPR), an attractive therapeutic target, for use in structure studies. Guidelines for crystallizing the TPR are also included. Together, these procedures provide a template for generating crystal structures of the TPR and indeed other GPCRs in complex with pharmacologically interesting ligands.Entities:
Keywords: Crystal structure determination; G protein-coupled receptor; GPCR crystallization; GPCR expression; GPCR purification; In meso crystallization; Membrane protein; Ramatroban; Thromboxane A2 receptor; X-ray crystallography
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Year: 2022 PMID: 35773586 DOI: 10.1007/978-1-0716-2368-8_13
Source DB: PubMed Journal: Methods Mol Biol ISSN: 1064-3745