Receptors and Drug Action. Receptors: Specific areas of cell membranes (proteins, glycoproteins)* When bound to ligand , positive or negative biological responce . Few ex. of free receptors in cytoplasma. Drugs that do act on receptors:. Drugs that do not act on receptors:.By camden
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Two receptor classes. Receptor tyrosine kinases (RTKs) Ligand induced dimerization Autophosphorylation Substrate phosphorylation Adapter proteins G-Protein coupled receptors (GPCRs) Ligand induced activation Guanine exchange factor (GEF) Second messenger cascade. Nucleotide cyclases.
Receptor-receptor interaction: A critical mechanism for the regulation of neurotransmitter receptor function. Fang Liu MD, PhD Centre for Addiction and Mental Health University of Toronto. Neurotransmitter Receptors:. Ionotropic: ligand-gated ion channels. Open ion channels—4-5 subunits
Título. K 1. Droga + Receptor Droga-Receptor E. K -1. Título. d RC = k 1 . R . C - k -1 . RC. dt. Título. d RC = 0. dt. k 1 . C . R = k -1 . RC. C . R = k -1 = K d. RC k 1. Título.
Receptor Proteins. Receiving and responding to messages. Receptor Proteins Proteins in the cell membrane which receive incoming “messages” Cells communicate with each other by sending specific signal molecules to each other. These molecules bind to specific receptor proteins. . Membrane.
RECEPTOR FAMILIES. By Prof. Omnia Nayel Assoc. Prof. Osama Yousif. ilo s. By the end of this lecture you will be able to :. Classify receptors into their main superfamilies. Recognize their different transduction mechanism. Identify the nature & time frame of their response.
Receptor terminology. Protein-ligand properties: specificity, saturation, affinity, competition Antagonist: binds to receptor site and inhibits Agonist: binds to receptor site and stimulates Down-regulation: levels of messenger receptors Up-regulation: levels of messenger receptors
Receptor Functional Steps. Reception - Respond to some form of energy by absorbing that energy with a membrane protein. Transduction - Translate the absorbed energy into the electrochemical activity of the nervous system.Amplification - Often amplify the original signal.Transmission - Generate a
Receptor/enzymes. Drug Design. Most drugs work on proteins Somehow interfere with a biochemical process Can shut down Can activate. Proteins. Polymers of amino acids that have some function Enzymes Receptors. Protein structure. Function very dependant on structure