HTS development services

ADMEKeywords: ADME, absorption, distribution, metabolism, excretion, pharmacologyADME is an abbreviation in pharmacokinetics and pharmacology for absorption, distribution, metabolism, and excretion, and describes the disposition of a pharmaceutical compound within an organism. The four criteria all influence the drug levels and kinetics of drug exposure to the tissues and hence influence the performance and pharmacological activity of the compound as a drug. With its robust cytotoxicity, metabolite and p-450 assays, AAT Bioquest offer excellent ADME screening for its customers.

Enzyme inhibitorsKeywords: enzymes, inhibition, phosphatases, kinases, proteases, transferases, blocking, drug targetAn enzyme inhibitor is a molecule that binds to an enzyme and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. They are also used in pesticides and other applications. With a large collection of enzyme activity assays AAT Bioquest offer competitive HTS services to screen and identify enzyme inhibitors. We specialize in screening enzyme inhibitors for protein phosphatases, protein kinases, proteases and transferases.

Glucose transporter targetsKeywords: glucose, assay, diabetes, GLUT, SLC2A, insulinGlucose transporters are a wide group of membrane proteins that facilitate the transport of glucose over a plasma membrane. Because glucose is a vital source of energy for all life, these transporters are present in all phyla. The GLUT or SLC2A family are a protein family that is found in most mammalian cells. 14 GLUTS are encoded by human genome. GLUT is a type of uniporter transporter protein. AAT Bioquest has developed the most robust glucose assays that have been used in our HTS services.

GPCR targetsKeywords: GPCR, receptors, signal transduction, cAMP screening, cell membrane, calcium, FLIPRG protein-coupled receptors (GPCRs) which are also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR), constitute a large protein family of receptors, that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses. GPCRs are the largest and most diverse group of membrane receptors in eukaryotes. These cell surface receptors act like an inbox for messages in the form of light energy, peptides, lipids, sugars, and proteins. With its industry-leading calcium and cAMP screening assays and special GPCR cell lines, AAT Bioquest offers a very comprehensive and competitive GPCR screening service.

Ion channelsKeywords: membrane proteins, channels, cell membrane, ionophoric, small molecules, membrane potentialIon channels are pore-forming membrane proteins that allow ions to pass through the channel pore. Their functions include establishing a resting membrane potential, shaping action potentials and other electrical signals by gating the flow of ions across the cell membrane, controlling the flow of ions across secretory and epithelial cells, and regulating cell volume. Ion channels are present in the membranes of all cells. Ion channels are one of the two classes of ionophoric proteins, along with ion transporters (including the sodium-potassium pump, sodium-calcium exchanger, and sodium-glucose transport proteins). With its industry-leading calcium, potassium, chloride, membrane potential screening assays and special ion channel cell lines, AAT Bioquest offers competitive ion channel screening service for sodium, potassium and chloride channels.

Protease targetsKeywords: protease, hydrolysis, digestion, amino acids, enzymes, FRET detection, peptide, oligoProtease (also known as a proteolytic enzyme, peptidase or proteinase) is a type of enzymes that function mainly to help us digest different kinds of proteins. They break down the bonds by a process known as hydrolysis and convert proteins into smaller chains called peptides or even smaller units called amino acids. A variety of proteases are used medically both for their native function (e.g. controlling blood clotting) or for completely artificial functions (e.g. for the targeted degradation of pathogenic proteins). With a large collection of protease activity assays AAT Bioquest offer comprehensive and competitive HTS services to screen and identify protease inhibitors.

Protein kinase inhibitorsKeywords: kinase, inhibition, phosphorylation, cellular pathways, signal transduction, signal amplification, enzymesA protein kinase is a kinase enzyme that modifies other proteins by chemically adding phosphate groups to them (phosphorylation). Phosphorylation usually results in a functional change of the target protein (substrate) by changing enzyme activity, cellular location, or association with other proteins. Kinases are known to regulate the majority of cellular pathways, especially those involved in signal transduction. A protein kinase inhibitor is a type of enzyme inhibitor that blocks the action of one or more protein kinases. With its universal kinase activity assay platform AAT Bioquest offers competitive protein kinase screening service.

Protein phosphatase inhibitorsKeywords: phosphatase, protein modification, dephsophorylation, amino acid residue, enzymesA protein phosphatase is a phosphatase enzyme that removes a phosphate group from the phosphorylated amino acid residue of its substrate protein. Protein phosphorylation is one of the most common forms of reversible protein posttranslational modification. Proteins are phosphorylated predominantly on Ser, Thr and Tyr residues. In contrast, protein phosphatases (PPs) are the primary effectors of dephosphorylation and can be grouped into three main classes based on sequence, structure and catalytic function. The protein pseudophosphatases form part of the larger phosphatase family, and in most cases are thought to be catalytically inert, instead functioning as phosphate-binding proteins, integrators of signalling or subcellular traps. AAT Bioquest offers competitive protein phosphatase inhibitor screening service.