Receptors chinRProten-Coupled Receptor Systems 5HTa serotonin R Cell Surface Multisubunit Ligand-gated lon channels GTP GDP Catalytic Activities: G Proteins: Effectors atawth factor tecentors Defined by Regulated by Cytoplasm a Subunits composition TGFB-rec I adenytyl cycase.Ca.cuments Nat exchange Nucleus regulated by 所subunits: phospholipase CB Figure 2-1.Structural motifs of physiologi and their relationships to signaling pathways. Classification of receptors(by structure and mode of action) 1)lon channel receptors:Include ligand-gated ion channels and voltage-gated ion channels 2)G protein-coupled receptors:Largest cell surface receptor family (or "superfamily").Also termed 7-TM (transmembrane domain)receptors 3)Kinase-linked receptors:These receptors have an extracellular ligand-binding domain and an intracellular kinase domain 4)Nuclear receptors:These receptors are named not just for their locations,but also for their mode of activation
1) Ion channel receptors: Include ligand‐gated ion channels and voltage‐gated ion channels 2) G protein‐coupled receptors: Largest cell surface receptor family (or “superfamily”). Also termed 7‐TM (transmembrane domain) receptors 3) Kinase‐linked receptors: These receptors have an extracellular ligand‐binding domain and an intracellular kinase domain 4) Nuclear receptors: These receptors are named not just for their locations, but also for their mode of activation. Classification of receptors (by structure and mode of action)
Receptor topography and classification Cell surface receptors (shown as enzyme-linked receptor with intrinsic enzymatic activity） 市 3 TRE Nuclear receptors Gene (ligand-dependent transcriptional ↑or↓Gene expression regulators) Receptor topography and classification EGF receptor Nicotinic AchR o(outside) i(inside) Transferrin IAP(CD47). receptor(CD71) and GPCRs S.J.Singer(1990.Ann Rev Cell Biol 6:247)
Nuclear receptors (ligand-dependent transcriptional regulators) Cell surface receptors (shown as enzyme-linked receptor with intrinsic enzymatic activity) Receptor topography and classification (outside) (inside) EGF receptor Transferrin receptor (CD71) IAP (CD47), and GPCRs Nicotinic AchR S.J. Singer (1990, Ann Rev Cell Biol 6:247) Receptor topography and classification
Receptor topography and classification Type V is cell surface molecule anchored to plasma membrane through a glycosyl-phosphatidyl inositol (GPI)anchor.The two examples shown are neural GPI cell adhesion molecules(GPI-CAMs). Other examples include CD16,also called FcyRIll, CD14.which is associated with Toll-like receptor 4 for signaling.and uPA receptor(uPAR,also called CD87). GPIlinkage A Some GPl-linked receptors are capable of trans- membrane signaling.The mechanism has not yet been fully elucidated. GPI linkage B L 品 Receptor-mediated signaling RTK:receptor tyrosine kinase (e.g.,receptors for EGF,PDGF) Shc:proto-oncogene,adaptor Grb2:adaptor protein MEK Sos:Ras exchange factor ERK Ras:Small GTPase Mnk CYTOPLASM Raf,MEK,ERK:kinases Elk-1:transcription factor NUCLEUS Mnk:a MAPKAPK
Type V is cell surface molecule anchored to plasma membrane through a glycosyl-phosphatidyl inositol (GPI) anchor. The two examples shown are neural GPI cell adhesion molecules (GPI-CAMs). Other examples include CD16, also called FcγRIII, CD14, which is associated with Toll-like receptor 4 for signaling, and uPA receptor (uPAR, also called CD87). Some GPI-linked receptors are capable of transmembrane signaling. The mechanism has not yet been fully elucidated. Receptor topography and classification Receptor‐mediated signaling RTK: receptor tyrosine kinase (e.g., receptors for EGF, PDGF) Shc: proto-oncogene, adaptor Grb2: adaptor protein Sos: Ras exchange factor Ras: Small GTPase Raf, MEK, ERK: kinases Elk-1: transcription factor Mnk: a MAPKAPK