Substance P-related peptide which inhibits the binding of G protein to its receptor. Competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
CAT No: R0855
CAS No:143675-79-0
Synonyms/Alias:G Protein Antagonist;143675-79-0;PYR-GLN-D-TRP-PHE-D-TRP-D-TRP-MET-NH2;G-Protein antagonist peptide;(2S)-N-[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2R)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide;pGlu-Gln-D-Trp-Phe-D-Trp-D-Trp-Met-NH2;DTXSID70745572;MFCD03444578;AKOS024456865;DA-53458;FG110327;PD079219;G Protein Antagonist Pyr-Gln-D-Trp-Phe-D-Trp-D-Trp-Met-NH2;5-Oxo-L-prolyl-L-glutaminyl-D-tryptophyl-L-phenylalanyl-D-tryptophyl-D-tryptophyl-L-methioninamide;
G-Protein antagonist peptide is a specialized synthetic peptide designed to modulate G-protein signaling pathways by selectively inhibiting the interaction between G-protein-coupled receptors (GPCRs) and their associated G-proteins. As a biochemical tool, it plays a pivotal role in dissecting the molecular mechanisms underlying cellular signal transduction. Due to the central role of GPCRs in physiological processes such as neurotransmission, hormonal regulation, and sensory perception, this antagonist peptide has become an indispensable reagent for researchers seeking to unravel the complexities of G-protein-mediated signaling events. Its specificity and versatility make it highly relevant for studies aiming to delineate receptor function, downstream effector activation, and the modulation of cellular responses.
Signal Transduction Research: In the context of cellular signaling studies, G-protein antagonist peptides are widely employed to selectively block the interaction between GPCRs and heterotrimeric G-proteins. By competitively inhibiting this coupling, researchers can investigate the direct consequences of G-protein inactivation on downstream effectors such as adenylate cyclase, phospholipase C, and ion channels. This targeted approach enables precise mapping of pathway-specific responses and aids in distinguishing G-protein-dependent from G-protein-independent signaling events, thereby advancing the understanding of receptor pharmacology and intracellular communication.
Receptor Characterization: The antagonist peptide serves as a valuable probe for characterizing the functional properties of GPCRs in various cell types and experimental systems. By selectively disrupting receptor-G-protein interactions, investigators can assess receptor subtype specificity, identify coupling preferences, and elucidate the structural determinants of receptor activation. This application is particularly important in the early stages of drug discovery, where detailed knowledge of receptor behavior informs the development of selective ligands and allosteric modulators.
Peptide-Based Functional Assays: In biochemical and pharmacological assays, G-protein antagonist peptides are utilized to establish negative controls or to validate the specificity of agonist-induced responses. Their inclusion in functional assays allows for the discrimination between direct receptor-mediated effects and secondary signaling cascades. This capability is essential for interpreting complex cellular outcomes and for verifying the mechanistic basis of observed biological activities, particularly in systems where multiple signaling pathways converge.
Neuroscience and Neuropharmacology: Given the prevalence of GPCRs in neuronal tissues, the antagonist peptide is frequently applied in studies examining synaptic transmission, neurotransmitter release, and neuronal excitability. By modulating G-protein activity, researchers can dissect the contributions of specific signaling pathways to neurophysiological processes, synaptic plasticity, and receptor cross-talk. Its use is instrumental in advancing the understanding of central and peripheral nervous system function at the molecular and cellular levels.
Peptide Engineering and Drug Discovery: In the field of peptide engineering, G-protein antagonist peptides provide a foundational scaffold for the design and optimization of novel modulators with enhanced selectivity and potency. Researchers leverage their structure-activity relationships to develop next-generation antagonists or inverse agonists tailored for specific GPCR targets. These efforts support high-throughput screening campaigns, lead compound identification, and the rational design of research tools that facilitate the exploration of GPCR biology and the discovery of innovative therapeutic strategies for a broad range of indications.
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