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Crystallization of the human cannabinoid type 2 receptor

人大麻素 2 型受体的结晶

基本信息

批准号：
7406679
负责人：
David Salom
金额：
$ 56.72万
依托单位：
POLGENIX, INC.
依托单位国家：
美国
项目类别：
财政年份：
2003
资助国家：
美国
起止时间：
2003-08-01 至 2009-03-31
项目状态：
已结题

来源：
https://reporter.nih.gov/project-details/7406679
关键词：
Abattoirs Absence of pain sensation Accounting Achievement Agonist Amino Acids Anabolism Analgesics Animal Model Anti-Allergic Agents Antibodies Antineoplastic Agents Area Atomic Force Microscopy Automobile Driving Back Bacteriophage T7 Binding Biochemical Biochemistry Biological Bioreactors Bos taurus Bronchodilation Budgets C-terminal CNR2 gene Cannabinoids Cannabis Capsid Proteins Cattle Cell Nucleus Cells Chronic Code Collaborations Column Chromatography Complex Condition Count Crystallization Crystallography Cyclic GMP DNA Data Desire for food Destinations Detergents Development Disease Disruption Doctor of Philosophy Drug Delivery Systems Drug Receptors Drug abuse Dynein ATPase Endoplasmic Reticulum Enhancers Ensure Epitopes Eye Family Figs - dietary G-Protein-Coupled Receptors GTP-Binding Proteins Gene Transfer Techniques Generations Genes Golgi Apparatus Growth Hand Heterogeneity Human Image Immune System Diseases Immunosuppression In Vitro Inflammation Investigation Knock-in Mouse Knock-out Knockout Mice Laboratories Left Letters Ligand Binding Ligands Light Marijuana Marketing Mechanics Mediating Membrane Membrane Proteins Methods Modeling Moods Mus Muscle relaxation phase Neurons Numbers Obesity Ophthalmology Pain Pattern Pharmaceutical Preparations Pharmacologic Substance Phase Photons Photophobia Photoreceptors Physiologic Intraocular Pressure Population Positioning Attribute Preparation Principal Investigator Procedures Process Production Property Proteins Protocols documentation Publishing Relative (related person)Reporting Research Personnel Resolution Reticulum Retina Retinal Degeneration Rhodopsin Rod Outer Segments Role Sales Sampling Scientist Second Messenger Systems Secure Sedation procedure Signal Transduction Site Source Spottings Standards of Weights and Measures Structure Synapses Synaptic Vesicles System Therapeutic Therapeutic Uses Therapeutic immunosuppression Time TimeLine Transgenic Mice Translations Universities Vomiting Washington Western Blotting absorption base cannabinoid receptor density design desire dimer drug discovery drug of abuse experience extracellular genetic manipulation glycosylation human CX3CR1 protein in vivo interest member molecular modeling neuroprotection novel painful neuropathy polypeptide prevent professor programs promoter protein misfolding receptor receptor expression retinal rods rho rod outer segment disc second messenger success therapeutic target three dimensional structure

项目摘要

DESCRIPTION (provided by applicant): The cannabinoid type 2 receptor (CB2R) is a target for the treatment of neurophatic pain and several other disorders. Solving the 3-dimensional structure of CB2R would enable the design of better CB2R-selective drugs. Although 30-50% of all current therapeutic drugs on the market modulate the action of different G protein coupled receptors (GPCRs), rhodopsin is the only GPCR for which the crystal structure is known. The bottleneck for GPCR crystallization has been the difficulty to generate large quantities of high-quality receptor sample needed for crystallography. The aim of this project is the crystallization and structural elucidation of CB2R by taking advantage of a novel, proprietary expression system to generate large amounts of homogeneous CB2R. If successful, the CB2R structure would dramatically empower our current cannabinoid receptor drug discovery effort. Moreover, this structure would represent the first non-rhodopsin template for molecular modeling of Family 1 GPCRs. And, in particular, it would be an excellent template for the modeling of the closely related CB1R, involved in many therapeutic areas including drug abuse, immune disorders, and obesity.

描述（由申请人提供）：大麻素2型受体（CB 2 R）是治疗神经性疼痛和其他几种疾病的靶点。解决CB 2 R的三维结构将使设计更好的CB 2 R选择性药物成为可能。虽然目前市场上所有治疗药物的30-50%调节不同G蛋白偶联受体（GPCR）的作用，但视紫红质是唯一已知晶体结构的GPCR。GPCR结晶的瓶颈一直是难以产生晶体学所需的大量高质量受体样品。该项目的目的是通过利用一种新型的专有表达系统来产生大量的同质CB 2 R，从而对CB 2 R进行结晶和结构解析。如果成功，CB 2 R结构将大大增强我们目前的大麻素受体药物发现工作。此外，该结构将代表用于家族1 GPCR的分子建模的第一个非视紫红质模板。特别是，它将是一个很好的模板，用于建模密切相关的CB 1 R，涉及许多治疗领域，包括药物滥用，免疫紊乱和肥胖。