Extended x-ray absorption fine structure (EXAFS) spectroscopy was combined with thermodynamic and kinetic approaches to investigate zinc binding to a zinc finger (C2H2) and a tetrathiolate (C4) peptide. Both peptides represent structural zinc sites of proteins and rapidly bind a single zinc ion with picomolar dissociation constants. In competition with EDTA the transfer of peptide-bound zinc io...

Production of cell-targeting vectors in part involves the addition of new targeting ligands to the vector to mediate binding to the cells of interest. For viral vectors, the ideal approach is to genetically engineer new ligands into the capsid proteins of the virus to generate a single agent to mediate therapy. Although this is ideal, this insertion of an exogenous ligand from one structural co...

This study was designed to ascertain whether the extracellular loops of vasopressin/oxytocin receptors bind ligands and, if so, to locate the molecular determinants of this ligand-receptor interaction. Ligand-binding studies were employed using a rat liver V1a vasopressin receptor preparation and both peptide and non-peptide receptor ligands. Synthetic peptides corresponding to defined regions ...

Cu, Zn, and amyloid-β (Aβ) peptides play an important role in the etiology of Alzheimer's disease (AD). Their interaction indeed modifies self-assembly propensity peptide that is at origin deposition insoluble aggregates amyloid plaque, a hallmark found AD brains. Another even more fallout Cu binding to Aβ formation reactive oxygen species (ROS) contributes overall oxidative stress detected due...

The insulin-like growth factor-1 receptor (IGF-1R) is a transmembrane receptor with tyrosine kinase activity. The receptor plays a critical role in cancer. Using monoclonal antibodies (MAbs) against the IGF-1R, typically blocks ligand binding and enhances down-regulation of the cell-surface IGF-1R. Some MAbs such as cixutumumab are under clinical trial investigation. Targeting multiple distinct...

The effectiveness of estrogens in stimulating gene transcription mediated by the estrogen receptor (ER) appears to depend on ER interactions with coactivator proteins. These coactivators bind to ER when it is liganded with an estrogen agonist, but not when it is liganded with an estrogen antagonist. Because estrogen agonists are known to induce a conformation in ER that stabilizes coactivator b...

Background. One of the perspectives anticytokine therapy is development synthetic oligopeptides, which can bind and inhibit activity cytokines. The peptide, a structural analogue cytokine-binding region chemokine receptor, interest as ligand for interaction with interleukin-8 (IL-8). aim research was to evaluate Trp-Asp-Phe-Asp IL-8. Material methods. between peptide cytokine evaluated by chang...

High-throughput structure determination of protein-ligand complexes is central in drug development and structural proteomics. To facilitate such high-throughput structure determination we designed an induced replacement strategy. Crystals of a protein complex bound to a photosensitive ligand are exposed to UV light, inducing the departure of the bound ligand, allowing a new ligand to soak in. W...

Abstract Plant genomes encode hundreds of receptor kinases and peptides, but the number known plant receptor-ligand pairs is limited. We report that Arabidopsis leucine-rich repeat kinase LRR-RK MALE DISCOVERER 1-INTERACTING RECEPTOR LIKE KINASE 2 (MIK2) for SERINE RICH ENDOGENOUS PEPTIDE (SCOOP) phytocytokines. MIK2 necessary sufficient immune responses triggered by multiple SCOOP suggesting t...

Sixteen-amino-acid-long peptides, corresponding to the optimal ligand preferences of the Src homology 3 (SH3) domains of Abl, Cortactin, Crk, p53BP2, and Src, were fused to the N-terminus of Escherichia coli alkaline phosphatase (AP). These secreted fusion proteins have been used as one-step detection probes of peptide ligand-SH3 domain interactions on microtiter plates and membranes. The bindi...