ORF-74, a 7TM receptor oncogene encoded by human herpes virus 8, shows 50% constitutive activity in stimulating phosphatidylinositol turnover and binds a large variety of CXC chemokines. These endogenous ligands cover a full spectrum of pharmacological properties with growth-related oncogene (GRO)-alpha and -gamma functioning as full agonists; GRObeta as a partial agonist; interleukin (IL)-8, n...

A novel methodology is shown enabling the screening of mixtures of compounds for their affinity to a receptor protein. The system presented, dynamic protein-affinity chromatography solid-phase extraction (DPAC-SPE), overcomes the limitations of the existing methods by performing an incubation of the His-tagged protein with a mixture of possible ligands, which are still in their native condition...

Peptides are important affinity ligands for microscopy, biosensing, and targeted delivery. However, because they can have low affinity for their targets, their selection from large naïve libraries can be challenging. When selecting peptidic ligands from display libraries, it is important to: 1) ensure efficient display; 2) maximize the ability to select high affinity ligands; and 3) minimize th...

Searching for new receptors of dendritic cell- and T cell-active chemokines, we used a combination of techniques to interrogate orphan chemokine receptors. We report here on human CCX CKR, previously represented only by noncontiguous expressed sequence tags homologous to bovine PPR1, a putative gustatory receptor. We employed a two-tiered process of ligand assignment, where immobilized chemokin...

Integrins are cell-surface adhesion molecules involved in mediating cell-extracellular matrix interactions. High-resolution structural data are not available for these heterodimeric receptors. In order to generate tools for photoaffinity scanning of the RGD-binding site of human integrin alphaVbeta3. new conformationally constrained ligands were designed. The ligands were based on five differen...

2015 This article provides an overview of the current challenges and trends in bioprocessing, with a focus on recent advances in the affinity purification of the principal classes of biotherapeutics, including monoclonal antibodies, glycoproteins, vaccines and erythropoietin. Affinity chromatography is usually applied during large-scale protein purification; it involves affinity ligands of biol...

BACKGROUND There is a significant need for affinity reagents with high target affinity/specificity that can be developed rapidly and inexpensively. Existing affinity reagent development approaches, including protein mutagenesis, directed evolution, and fragment-based design utilize large libraries and/or require structural information thereby adding time and expense. Until now, no systematic ap...

Combinatorial library screens based on binding affinity may preferentially select ligands with ability for ionic interactions and miss the biologically relevant ligands that bind more weakly with predominantly hydrophobic interactions.

The Front Cover shows the development of a potent ligand for galectin-8 (in light blue), protein produced by endothelial cells and involved in many processes, such as promoting angiogenesis. Starting from 3-lactoylgalactoside pink), best fit to complete “puzzle binding” consisted molecule with cyclohexyl moiety position 3 galactose dichlorothiophenyl group 1. new showed an improved affinity alm...

The value of high affinity-specific reagents in immunology is exemplified by the use of mAbs. Recent in vitro selection methods suggested that oligonucleotides may provide a useful alternative, especially where Abs have been insufficient thus far. We used a systematic evolution of ligands by exponential enrichment (SELEX) procedure to derive high affinity oligonucleotide ligands (aptamers) reco...