2 -Adrenergic catecholamines -Adrenergic catecholamines Adrenocorticotropic hormone (ACTH) Antidiuretic hormone (vasopressin) Calcitonin Chorionic gonadotropin, human (CG) Corticotropin-releasing hormone Follicle-stimulating hormone (FSH) Glucagon Lipotropin (LPH) Luteinizing hormone (LH) Melanocyte-stimulating hormone (MSH) Parathyroid hormone (PTH) Somatostatin Thyroid-stimulating hormone (TSH) B. The second messenger is cGMP Atrial natriuretic factor Nitric oxide C. The second messenger is calcium or phosphatidylinositols (or both) Acetylcholine (muscarinic) 1 -Adrenergic catecholamines Angiotensin II Antidiuretic hormone (vasopressin) Cholecystokinin Gastrin Gonadotropin-releasing hormone Oxytocin Platelet-derived growth factor (PDGF) Substance P Thyrotropin-releasing hormone (TRH) D. The second messenger is a kinase or phosphatase cascade Adiponectin Chorionic somatomammotropin Epidermal growth factor (EGF) Erythropoietin (EPO) Fibroblast growth factor (FGF) Growth hormone (GH) Insulin Insulin-like growth factors I and II Leptin Nerve growth factor (NGF) Platelet-derived growth factor Prolactin TABLE 414 General Features of Hormone Classes Group I Group II Types Steroids, iodothyronines, calcitriol, retinoids Polypeptides, proteins, glycoproteins, catecholamines Solubility Lipophilic Hydrophilic Transport proteins Yes No Plasma half-life Long (hours to days) Short (minutes) Receptor Intracellular Plasma membrane Mediator Receptor-hormone complex cAMP, cGMP, Ca 2+ , metabolites of complex phosphinositols, kinase cascades but closely related functions. For e G- Proteins Guanine nucleotide binding proteins which act as a Transducer between a receptor & an effector
Discovered by Alfred Gilman & Martin Rodbell in 1990
Significance:
Of the top 100 drugs,
26 directed at GPCRs 60 % act through GPCRs 40 % of prescriptions 3rd largest family of genes (865) Present in almost every organ system Structure:
Embedded in the plasma
membrane Lysozyme insert 7 transmembrane -helices
Rhodopsin was first of these
to have its structure confirmed by X-ray crystallography ligand -Adrenergic Receptor PDB 2RH1 Binding Domains
Small molecular ligands
bind to sites within the hydrophobic core formed by
transmembrane helices
Protein and peptide
agonists bind to N terminus & extracellular hydrophilic loops joining the transmembrane domain
G-proteins bind either to
second and third cytoplasmic loop which is largest or to carboxy terminus