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Receptor Biology

Peptides exert their biological effects primarily through specific receptor interactions. This section explores the molecular mechanisms governing peptide-receptor recognition, signaling, and regulation.

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GPCR Signaling Mechanisms

G protein-coupled receptor activation, signal transduction cascades (cAMP, IP3, Ca²⁺), biased agonism, and functional selectivity in peptide signaling.

β†’ G protein coupling and second messengers
β†’ Ξ²-arrestin recruitment pathways
β†’ Biased agonism in therapeutic design
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Peptide–Receptor Binding Kinetics

Principles of ligand binding β€” Kd, kon, koff, residence time, and their impact on peptide pharmacological activity and therapeutic duration.

β†’ Radioligand binding assays
β†’ Surface plasmon resonance (SPR)
β†’ Structure-kinetic relationships (SKR)
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Receptor Tyrosine Kinases and Peptide Ligands

RTK family receptors, peptide growth factor signaling, dimerization mechanisms, and therapeutic targeting with peptide agonists and antagonists.

β†’ Insulin and IGF-1 receptor signaling
β†’ Peptide growth factor therapeutics
β†’ Oncogenic RTK inhibition strategies
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Allosteric Modulation of Peptide Receptors

Mechanisms of allosteric modulation, positive and negative allosteric modulators (PAMs/NAMs), cooperativity factors, and therapeutic advantages.

β†’ Orthosteric vs allosteric binding sites
β†’ Cooperativity and probe dependence
β†’ Allosteric peptide drug design
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Receptor Desensitization and Internalization

Mechanisms of homologous and heterologous desensitization, receptor phosphorylation, Ξ²-arrestin-mediated internalization, recycling, and degradation.

β†’ GRK-mediated phosphorylation
β†’ Clathrin-mediated endocytosis
β†’ Therapeutic implications of receptor trafficking