The binding affinity of G protein-coupled receptor (GPCR) ligands is customarily measured by radio-ligand competition experiments. As an alternative approach, ^(19)F nuclear magnetic resonance spectroscopy (^(19)F-NMR) is used for the screening of small-molecule lead compounds in drug discovery; the two methods are complementary in that the measurements are performed with widely different experimental conditions. Here, we used the structure of the A(2A) adenosine receptor (A(2A)AR) complex with...
[ASAP] Adenosine A2A Receptor (A2AAR) Ligand Screening Using the 19F-NMR Probe FPPA
Adenosine A2A Receptor (A2AAR) Ligand Screening Using the 19F-NMR Probe FPPA
Jinfeng Zhang, Dandan Feng, Jianjun Cheng, and Kurt Wu?thrich
https://pubs.acs.org/cms/10.1021/jacs.3c04218/asset/images/medium/ja3c04218_0005.gif
Journal of the American Chemical Society
DOI: 10.1021/jacs.3c04218
nmrlearner
Journal club
0
06-06-2023 09:06 PM
[NMR paper] DeSiphering receptor core-induced and ligand-dependent conformational changes in arrestin via genetic encoded trimethylsilyl 1H-NMR probe.
DeSiphering receptor core-induced and ligand-dependent conformational changes in arrestin via genetic encoded trimethylsilyl 1H-NMR probe.
Related Articles DeSiphering receptor core-induced and ligand-dependent conformational changes in arrestin via genetic encoded trimethylsilyl 1H-NMR probe.
Nat Commun. 2020 Sep 25;11(1):4857
Authors: Liu Q, He QT, Lyu X, Yang F, Zhu ZL, Xiao P, Yang Z, Zhang F, Yang ZY, Wang XY, Sun P, Wang QW, Qu CX, Gong Z, Lin JY, Xu Z, Song SL, Huang SM, Guo SC, Han MJ, Zhu KK, Chen X, Kahsai AW, Xiao KH, Kong W, Li FH, Ruan...
nmrlearner
Journal club
0
09-28-2020 09:16 PM
[NMR paper] Activation of adenosine A2A receptor by lipids from docosahexaenoic acid revealed by NMR.
Activation of adenosine A2A receptor by lipids from docosahexaenoic acid revealed by NMR.
Related Articles Activation of adenosine A2A receptor by lipids from docosahexaenoic acid revealed by NMR.
Sci Adv. 2020 Mar;6(12):eaay8544
Authors: Mizumura T, Kondo K, Kurita M, Kofuku Y, Natsume M, Imai S, Shiraishi Y, Ueda T, Shimada I
Abstract
The lipid composition of the plasma membrane is a key parameter in controlling signal transduction through G protein-coupled receptors (GPCRs). Adenosine A2A receptor (A2AAR) is located in the...
nmrlearner
Journal club
0
03-25-2020 10:28 PM
[NMR paper] Nanodiscs for INPHARMA NMR Characterization of GPCRs: Ligand Binding to the Human A2A Adenosine Receptor.
Nanodiscs for INPHARMA NMR Characterization of GPCRs: Ligand Binding to the Human A2A Adenosine Receptor.
Related Articles Nanodiscs for INPHARMA NMR Characterization of GPCRs: Ligand Binding to the Human A2A Adenosine Receptor.
Angew Chem Int Ed Engl. 2017 Apr 21;:
Authors: Fredriksson K, Lottmann P, Hinz S, Onila I, Shymanets A, Harteneck C, Müller CE, Griesinger C, Exner TE
Abstract
G-protein-coupled-receptors (GPCRs) are of fundamental importance for signal transduction through cell membranes. This makes them important...
nmrlearner
Journal club
0
04-22-2017 10:30 PM
[NMR paper] NMR metabolomics for identification of adenosine A1 receptor binding compounds from Boesenbergia rotunda rhizomes extract.
NMR metabolomics for identification of adenosine A1 receptor binding compounds from Boesenbergia rotunda rhizomes extract.
http://www.bionmr.com//www.ncbi.nlm.nih.gov/corehtml/query/egifs/http:--linkinghub.elsevier.com-ihub-images-PubMedLink.gif Related Articles NMR metabolomics for identification of adenosine A1 receptor binding compounds from Boesenbergia rotunda rhizomes extract.
J Ethnopharmacol. 2013 Oct 28;150(1):95-9
Authors: Yuliana ND, Budijanto S, Verpoorte R, Choi YH
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE:...
nmrlearner
Journal club
0
05-20-2014 11:10 PM
An NMR strategy for fragment-based ligand screening utilizing a paramagnetic lanthanide probe.
An NMR strategy for fragment-based ligand screening utilizing a paramagnetic lanthanide probe.
An NMR strategy for fragment-based ligand screening utilizing a paramagnetic lanthanide probe.
J Biomol NMR. 2011 Sep 17;
Authors: Saio T, Ogura K, Shimizu K, Yokochi M, Burke TR, Inagaki F
Abstract
A nuclear magnetic resonance-based ligand screening strategy utilizing a paramagnetic lanthanide probe is presented. By fixing a paramagnetic lanthanide ion to a target protein, a pseudo-contact shift (PCS) and a paramagnetic relaxation...
nmrlearner
Journal club
0
09-20-2011 03:10 PM
An NMR strategy for fragment-based ligand screening utilizing a paramagnetic lanthanide probe
An NMR strategy for fragment-based ligand screening utilizing a paramagnetic lanthanide probe
Abstract A nuclear magnetic resonance-based ligand screening strategy utilizing a paramagnetic lanthanide probe is presented. By fixing a paramagnetic lanthanide ion to a target protein, a pseudo-contact shift (PCS) and a paramagnetic relaxation enhancement (PRE) can be observed for both the target protein and its bound ligand. Based on PRE and PCS information, the bound ligand is then screened from the compound library and the structure of the ligandâ??protein complex is determined. PRE is an...
Adenosine A2A Receptor (A2AAR) Ligand Screening Using the 19F-NMR Probe FPPA
Linear Mode
