Full-length human GLP-1 receptor structure without orthosteric ligands

Structure of full-length human TRPM4

Transient receptor potential melastatin subfamily member 4 (TRPM4) is a widely distributed, calcium-activated, monovalent-selective cation channel. Mutations in human TRPM4 (hTRPM4) result in progressive familial heart block. Here, we report the electron cryomicroscopy structure of hTRPM4 in a closed, Na+-bound, apo state at pH 7.5 to an overall resolution of 3.7 Å. Five partially hydrated sodi...

Single-step purification of full-length human androgen receptor

The full-length human androgen receptor with an N-terminal biotin acceptor peptide tag was overexpressed in Spodoptera frugiperda cells in the presence of 1 microM dihydrotestosterone. Site-specific biotinylation of BAP was achieved in vivo by co-expression of E. coli biotin holoenzyme synthetase. The androgen receptor was purified by single-step affinity chromatography using Streptavidin Mutei...

Approaches to improve the pharmacokinetics of radiolabeled GLP-1 receptor ligands using antagonistic tracers

receptor ligands using antagonistic tracers Svetlana N. Rylova1,2,3, Beatrice Waser4, Luigi Del Pozzo 1,2,3, Roswitha Tönnesmann2, Rosalba Mansi2, Philipp T. Meyer2, Jean Claude Reubi4, Helmut R. Maecke,2 1 German Cancer Consortium (DKTK), Heidelberg, Germany 2 Department of Nuclear Medicine, University Hospital Freiburg, Freiburg, Germany 3 German Cancer Research Center (DKFZ), Heidelberg, Ger...

GLP-1 analogs: satiety without malaise?

DNA Display Selection of Peptide Ligands for a Full-Length Human G Protein-Coupled Receptor on CHO-K1 Cells

The G protein-coupled receptors (GPCRs), which form the largest group of transmembrane proteins involved in signal transduction, are major targets of currently available drugs. Thus, the search for cognate and surrogate peptide ligands for GPCRs is of both basic and therapeutic interest. Here we describe the application of an in vitro DNA display technology to screening libraries of peptide lig...