Eddy, Matthew T.’s team published research in Journal of the American Chemical Society in 140 | CAS: 377727-87-2

Eddy, Matthew T. published the artcileExtrinsic Tryptophans as NMR Probes of Allosteric Coupling in Membrane Proteins: Application to the A_2A Adenosine Receptor, HPLC of Formula: 377727-87-2, the publication is Journal of the American Chemical Society (2018), 140(26), 8228-8235, database is CAplus and MEDLINE.

Tryptophan indole ¹⁵N-¹H signals are well separated in NMR spectra of proteins. Assignment of the indole ¹⁵N-¹H signals therefore enables one to obtain site-specific information on complex proteins in supramacromol. systems, even when extensive assignment of backbone ¹⁵N-¹H resonances is challenging. Here the authors exploit the unique indole ¹⁵N-¹H chem. shift by introducing extrinsic tryptophan reporter residues at judiciously chosen locations in a membrane protein for increased coverage of structure and function by NMR. The authors demonstrate this approach with three variants of the human A_2A adenosine receptor (A_2AAR), a class A G protein-coupled receptor, each containing a single extrinsic tryptophan near the receptor intracellular surface, in helix V, VI, or VII, resp. The authors show that the native A_2AAR global protein fold and ligand binding activity are preserved in these A_2AAR variants. The indole ¹⁵N-¹H signals from the extrinsic tryptophan reporter residues show different responses to variable efficacy of drugs bound to the receptor orthosteric cavity, and the indole ¹⁵N-¹H chem. shift of the tryptophan introduced at the intracellular end of helix VI is sensitive to conformational changes resulting from interactions with a polypeptide from the carboxy terminus of the Gα_S intracellular partner protein. Introducing extrinsic tryptophans into proteins in complex supramol. systems thus opens new avenues for NMR investigations in solution

Journal of the American Chemical Society published new progress about 377727-87-2. 377727-87-2 belongs to triazoles, auxiliary class GPCR/G Protein,Adenosine Receptor, name is 2-(Furan-2-yl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)piperazin-1-yl)ethyl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, and the molecular formula is C25H29N9O3, HPLC of Formula: 377727-87-2.

Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics