CREBtide, a synthetic 13 amino acid peptide, has been reported as a PKA substrate.
CAT No: R1305
CAS No:149155-45-3
Synonyms/Alias:Crebtide;149155-45-3;Krreilsrrpsyr;DTXSID30164184;DTXCID1086675;DA-62499;G13106;
CREBtide is a synthetic peptide substrate derived from the consensus phosphorylation sequence of the cAMP response element-binding protein (CREB). As a biochemically defined peptide, it serves as a highly specific tool for investigating protein kinase activity, particularly for kinases such as protein kinase A (PKA) and protein kinase B (Akt/PKB), which are known to phosphorylate CREB or related motifs. CREBtide's precise sequence enables researchers to dissect phosphorylation events in vitro, providing a controlled system for studying signal transduction pathways involving CREB and its regulatory kinases. Its functional design and broad compatibility make it an essential reagent in molecular biology, enzymology, and cell signaling research.
Kinase activity assays: CREBtide is widely used as a substrate in quantitative kinase assays designed to measure the enzymatic activity of PKA, Akt, and other kinases that recognize CREB-like motifs. When incubated with these kinases and ATP, the peptide undergoes phosphorylation at the target serine residue, allowing for direct assessment of kinase function. Its defined sequence and high specificity facilitate accurate determination of kinetic parameters, inhibitor screening, and mechanistic studies of kinase-substrate interactions under controlled experimental conditions.
Signal transduction research: As a model substrate, this peptide enables detailed exploration of intracellular signaling pathways that regulate gene transcription via CREB phosphorylation. By serving as a readout for kinase-mediated phosphorylation, it helps elucidate how extracellular signals, such as hormones or growth factors, activate downstream effectors that converge on CREB. Researchers can use the peptide in cell-free systems to isolate and characterize the contributions of specific kinases, phosphatases, and second messengers in the modulation of CREB-dependent signaling cascades.
Inhibitor screening and drug discovery: The use of CREBtide in high-throughput screening platforms allows for the rapid assessment of small molecule inhibitors targeting kinases involved in CREB phosphorylation. By monitoring changes in peptide phosphorylation in the presence of candidate compounds, scientists can identify and characterize potential kinase inhibitors, evaluate selectivity profiles, and optimize lead compounds for further development. The peptide's robustness and reproducibility make it a valuable asset in early-stage drug discovery and pharmacological research.
Phosphorylation detection and quantification: Researchers employ this peptide in conjunction with radiolabeled ATP, phospho-specific antibodies, or mass spectrometry to detect and quantify phosphorylation events with high sensitivity. Its defined sequence ensures that observed phosphorylation is directly attributable to the activity of the kinase of interest, reducing background noise and enhancing assay reliability. Such applications are critical for validating kinase activity, optimizing assay conditions, and benchmarking experimental systems in both basic and applied research.
Enzyme kinetics and mechanistic studies: The peptide serves as an ideal model for dissecting the kinetic properties and mechanistic details of kinase-catalyzed phosphorylation. By varying substrate concentration, ATP levels, or reaction conditions, researchers can determine key parameters such as Km, Vmax, and catalytic efficiency. Insights gained from these studies inform the understanding of enzyme regulation, substrate specificity, and the molecular basis of signal integration in cellular contexts. The availability of a well-characterized peptide substrate like CREBtide thus accelerates progress in enzymology and signal transduction research.
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