Project 1 is responsible for achieving the Center‟
s Aim 1 goals;the immediate goal of Aim 1 studies is the structure solution of GPCRs and their co-crystals with ligands. The long range goal is to develop a better understanding of the structure-function relationship in GPCRs. Ultimately enough structures will be determined to provide a fine sampling of the various GPCR sequence families and, thus, enable reliable modeling and predictive docking studies of other close family members. Structures of receptors in complex with different ligands will be essential for developing a better understanding of their binding properties. Ultimately, this newly acquired knowledge can then be used to validate and to generate hypothesis regarding GPCRs mechanisms of action (e.g., in signal processing pathways). These new structures will have an enormous impact on furthering our understanding of a number of diseases and most probably will help accelerate success rates in drug discovery and therapeutics development studies.

Agency
National Institute of Health (NIH)
Institute
National Institute of General Medical Sciences (NIGMS)
Type
Specialized Center--Cooperative Agreements (U54)
Project #
5U54GM094618-04
Application #
8501564
Study Section
Special Emphasis Panel (ZGM1-CBB-3)
Project Start
Project End
Budget Start
2013-07-01
Budget End
2014-06-30
Support Year
4
Fiscal Year
2013
Total Cost
$640,546
Indirect Cost
$278,158
Name
Scripps Research Institute
Department
Type
DUNS #
781613492
City
La Jolla
State
CA
Country
United States
Zip Code
92037
Eddy, Matthew T; Didenko, Tatiana; Stevens, Raymond C et al. (2016) β2-Adrenergic Receptor Conformational Response to Fusion Protein in the Third Intracellular Loop. Structure 24:2190-2197
Rowe, Timothy B; Luo, Zhe-Xi; Ketcham, Richard A et al. (2016) X-ray computed tomography datasets for forensic analysis of vertebrate fossils. Sci Data 3:160040
Ngo, Tony; Kufareva, Irina; Coleman, James L J et al. (2016) Identifying ligands at orphan GPCRs: current status using structure-based approaches. Br J Pharmacol :
Kufareva, Irina; Gustavsson, Martin; Holden, Lauren G et al. (2016) Disulfide Trapping for Modeling and Structure Determination of Receptor: Chemokine Complexes. Methods Enzymol 570:389-420
Yang, Dehua; de Graaf, Chris; Yang, Linlin et al. (2016) Structural Determinants of Binding the Seven-transmembrane Domain of the Glucagon-like Peptide-1 Receptor (GLP-1R). J Biol Chem 291:12991-3004
Zheng, Yi; Qin, Ling; Zacarías, Natalia V Ortiz et al. (2016) Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists. Nature 540:458-461
Zhu, Lan; Weierstall, Uwe; Cherezov, Vadim et al. (2016) Serial Femtosecond Crystallography of Membrane Proteins. Adv Exp Med Biol 922:151-60
White, Thomas A; Barty, Anton; Liu, Wei et al. (2016) Serial femtosecond crystallography datasets from G protein-coupled receptors. Sci Data 3:160057
Batyuk, Alexander; Galli, Lorenzo; Ishchenko, Andrii et al. (2016) Native phasing of x-ray free-electron laser data for a G protein-coupled receptor. Sci Adv 2:e1600292
Leach, Katie; Gregory, Karen J; Kufareva, Irina et al. (2016) Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor. Cell Res 26:574-92

Showing the most recent 10 out of 109 publications