A Two-Step Strategy to Enhance Activity of Low Potency Peptides

• Published in: PloS one Vol. 9; no. 11; p. e110502
• Main Authors: Doyle, Jamie R., Harwood, Benjamin N., Krishnaji, Subrahmanian Tarakkad, Krishnamurthy, Vijay M., Lin, Wei-En, Fortin, Jean-Philippe, Kumar, Krishna, Kopin, Alan S.
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 12.11.2014; Public Library of Science (PLoS)
• Subjects: Anchoring; Antagonists; Binding sites; Biology and Life Sciences; Cardiology; Chemistry; Cholecystokinin; Fatty acids; G protein-coupled receptors; G proteins; Glycine; Glycine - chemistry; HEK293 Cells; Hormones; Humans; Ligands; Membranes; Modulators; Optimization; Peptides; Peptides - chemistry; Permeability; Pharmaceutical sciences; Pharmacology; Piperidines - chemistry; Plasmids - metabolism; Probes; Protein Structure, Tertiary; Proteins; Prototypes; Receptors; Receptors, G-Protein-Coupled - chemistry; Receptors, Neurokinin-1 - chemistry; Recombinant proteins; Recombinant Proteins - chemistry; Signal Transduction; Signaling; Substance P; Substance P - chemistry; Tetragastrin - chemistry

Novel strategies are needed to expedite the generation and optimization of peptide probes targeting G protein-coupled receptors (GPCRs). We have previously shown that membrane tethered ligands (MTLs), recombinant proteins comprised of a membrane anchor, an extracellular linker, and a peptide ligand...