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Drug Receptors, Receptor Regulation Mechanisms - Coggle Diagram
Drug Receptors
GPCRs (Most Abundant)
G(s)
Activate Ca channels
Activate adenylyl cyclase
G(i)
Activate K channels
Inhibit adenylyl cyclase
G(o)
Inhibit Ca channels
G(q)
Activate phospholipase C
G(12/13)
Diverse ion transporter interactions
Enzymatic Domain
Receptor Tyrosine Kinases
Adds phosphate to tyrosine residues
Receptor Tyrosine Phosphatases
Removes phosphate from tyrosine residues
Receptor Tyrosine-Associated Kinases
Dimerization activates a tyrosine kinase
Receptor Serine/Threorine Kinases
Adds phosphate to serine or threonine residues
Role in cell growth, differentiation, cancer
Receptor Guanylyl Cyclases
Activate guanylyl cyclase directly
Ion Channels
Ligand-Gated
Voltage Gated
Second Messenger Regulated
Intracellular
Enzymes
Signaling cascades and apoptosis
Transcription Factors
DNA transcription regulation
Structural Proteins
RNA interference and microtubule disruption
Cell-Surface Adhesion
Integrin binding
Function like velcro
Extracellular
Communication between cells
Receptor Regulation Mechanisms
Tachyphylaxis
Repeated administration of a drug results in diminishing effect
Desensitization
Homologous
Decreased response at one receptor
Heterologous
Decreased response coordinated by 2+ receptors
Inactivation
Loss of ability to respond to stimulation by drug
Covalent bonding
Suicide substrate
Refractoriness
Period of time required before initiating another response
Voltage gated sodium channels
Down-Regulation
Repeated interaction at receptor results in removal of receptors from plasma membrane
Via endocytosis