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Interactions between G protein-coupled receptors and their ligands hold extensive potential for drug discovery. Studying these interactions poses technical problems due to their transient nature and the inherent difficulties when working with G protein-coupled receptors (GPCR) that are only functional in a membrane setting. Here, we describe the use of a furan-based chemical cross-linking methodology to achieve selective covalent coupling between a furan-modified peptide ligand and its native GPCR present on the surface of living cells under normal cell culture conditions. This methodology relies on the oxidation of the furan moiety, which can be achieved by either addition of an external oxidation signal or by the reactive oxygen species produced by the cell. The cross-linked ligand-GPCR complex is subsequently detected by Western blotting based on the biotin label that is incorporated in the peptide ligand.
This article was published in the following journal.
Name: Methods in molecular biology (Clifton, N.J.)
Dimers of furan, 2,3-dihydrofuran, 2,5-dihydrofuran and tetrahydrofuran were investigated with the use of theoretical methods to determine the interactions that keep the molecules together. The QTAIM ...
Multivalency can facilitate complex formation when monovalent receptor ligand interactions are weak. However, enhanced binding of two multivalent binding partners should be avoidable for example when ...
Cross-linking mass spectrometry (XL-MS) has received considerable interest, owing to its potential to investigate protein-protein interactions (PPIs) in an unbiased fashion in complex protein mixtures...
The reaction of Re(CO)(μ-CH)(μ-H) (1) with furan in CHCl at 40 °C yielded two new isomeric dirhenium compounds, Re(CO)(μ-η-2,3-CHO)(μ-H) (2) and Re(CO)(μ-η-3,2-CHO)(μ-H) (3), which contain a ...
G protein-coupled receptors (GPCRs) relay extracellular information across cell membranes through a continuum of conformations that are not always captured in structures. Hence, complementary approach...
To evaluate two different techniques of cross linking: standard epithelium off (CXL epi off) versus trans-epithelial (CXL epi on) cross linking in patient with progressive keratoconus.
the purpose of this study is to compare the efficacy and safety of a new method of corneal cross-linking that uses UV-A irradiation intensity of 9mW/cm2 for 7 minutes to well-known Accele...
To compare 3 year iontophoretic transepithelial corneal cross-linking (I-ON CXL) outcomes with epithelium-off collagen cross-linking (epi-off CXL)in pediatric patients.
This is a compassionate treatment protocol for the use of the UV-X system for corneal collagen cross-linking (CXL) in eyes with progressive keratoconus in patients who have conditions that...
Corneal Cross Linking is new treatment modality for patients with keratoconus. A keratoconus is characterized by progressive bulging and thinning of the eye's cornea. Keratoconus is a pote...
The interactions of particles responsible for their scattering and transformations (decays and reactions). Because of interactions, an isolated particle may decay into other particles. Two particles passing near each other may transform, perhaps into the same particles but with changed momenta (elastic scattering) or into other particles (inelastic scattering). Interactions fall into three groups: strong, electromagnetic, and weak. (From McGraw-Hill Encyclopedia of Science & Technology, 7th ed)
Screening techniques first developed in yeast to identify genes encoding interacting proteins. Variations are used to evaluate interplay between proteins and other molecules. Two-hybrid techniques refer to analysis for protein-protein interactions, one-hybrid for DNA-protein interactions, three-hybrid interactions for RNA-protein interactions or ligand-based interactions. Reverse n-hybrid techniques refer to analysis for mutations or other small molecules that dissociate known interactions.
The field that studies interactions between individuals and the built and natural environment. It includes investigating behaviors that inhibit or foster sustainable, climate-healthy, and nature-enhancing choices.
Enzyme which catalyzes the peptide cross-linking of nascent CELL WALL; PEPTIDOGLYCAN.
One of the protein CROSS-LINKING REAGENTS that is used as a disinfectant for sterilization of heat-sensitive equipment and as a laboratory reagent, especially as a fixative.
Within medicine, nutrition (the study of food and the effect of its components on the body) has many different roles. Appropriate nutrition can help prevent certain diseases, or treat others. In critically ill patients, artificial feeding by tubes need t...
Clinical Approvals Clinical Trials Drug Approvals Drug Delivery Drug Discovery Generics Drugs Prescription Drugs In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which drugs are dis...