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Organisation of the Body

Quiz yourself by thinking what should be in each of the black spaces below before clicking on it to display the answer.
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Question
Answer
show High affinity for hormone Hormone specific Binding is saturatable  
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Kds   show
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show Conc of hormone that gives 50% response  
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Receptor classes   show
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Ligand gated ion channels   show
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show 5 protein 2 homodimers and 1 extra protein Blocked by cobra toxins Open in response to ACh binding - non-selective cation channel  
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show Glucose enters beta cells and is metabolised to produce ATP This binds to K channels and blocks them Leads to depolarisation and Ca influx Insulin release triggered ATP acts as a hormone  
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G protein coupled receptors   show
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What activates GPCRs   show
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show Around 820 in the human body All have similar structures - hard to design drugs specific to one, so unwanted effects are common  
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show 7 transmembrane regions Extracellular N-terminus Often post translationally glycosylated and phosphorylated to regulate activity  
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show Found in the heart - slow heart rate QNB - antagonist  
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show Get their name from their ability to bind GTP and GDP They exist in an active GTP bound and an inactive GDP bound form Active G proteins bind and activate signalling enzymes causing a specific response Heterotrimeric - alpha, beta and gamma subunits  
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Types of GPCRs   show
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show Inactive - loosly associated with proteins Ligand binds and recruits G proteins GTP exchange causes dissociation of the protein Subunits have different effects GTP hydrolysis causes reassociation  
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Downstream effectors of GPCRs   show
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Adenylate cyclase   show
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show A GPCR agonist Binds to Gs - increased cAMP and PKA Activates CTFR Overactive CTFR causes Cl loss into lumen of gut followed by Na and water Leads to internal dehydration Enkephalin - stimulates Gi to reduce effects  
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show ACTH stimulates Gs - cAMP produced Immediately upregulated cholesterol synthesis by cholesterol ester hydrolase Over a few hours allows uptake of cholesterol by mitochondria  
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show Activated by Gq receptors Cleaves PIP2 into DAG and IP3 DAG activates PKC - phosphorylates proteins IP3 activates store operated calcium ion channels leading to Ca efflux from SR - activation of intracellular proteins  
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show Normal B cells us a Gs pathway to secrete insulin involving GIP and GLP-1 Following chronic hyperglycemia and chronic sulfonylurea treatment they switch to Gq  
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show Channels phosphorylated - less active e.g. G protein gated inwardly rectifying potassium channels in the heart  
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Smooth muscle contraction   show
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show Reaction cascades cause massive signal amplification Proteins made can last a long time, so short activation affects function for longer periods  
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Enzyme linked channels   show
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show Tyrosine kinase receptor Leads to insertion of Glut4 into cell membranes Under fasting conditions no insulin = no glucose uptake as no Glut4 channels in membrane  
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show Control of DNA transcription e.g. steroid hormones and Vit D (for Ca uptake) Takes hours for proteins to be produced  
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show DNA strand contains specific hormone response elements Contains regions for transcriptional regulation, DNA binding and hormone binding  
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What binds to intracellular receptors   show
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show Removal or degradation of the hormone Desensitisation of the receptor Internalisation of the receptor  
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Desensitisation of GPCRs   show
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Resensitisation   show
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show Serves as a connection between glucagon and insulin pathways Insulin drives activation of phosphodiesterase to downregulate the role of glucagon Breaks down cAMP  
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show Receptors taken into the cell by endocytosis Basically receptor mediated endocytosis Dopamine D1 receptors are permanently downregulated due to overuse in addiction - via internalisation and DNA metylation  
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show Failure of ligand binding Failure of signal transduction Constitutively active signal receptor systems Antibodies to receptor  
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show Receptor does not function despite hormone present  
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Activating receptor mutations   show
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Dwarfism   show
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Activating receptor mutations   show
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Physiological response to receptor activation   show
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Types of cell signalling   show
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