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27 Cards in this Set
- Front
- Back
fatty acids are what |
carboxylic acid linked too an aliphatic tail |
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3 chains of fatty acids and explain |
short chain fatty acids- <6 carbon chain medium chain fatty acids- 7-12 carbon chain long chain fatty acids->13 carbon chainfi |
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further classifications of fatty acids |
saturate fatty acids (SFA) monounsaturated (MUFA) polyunsaturated( PUFA) |
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what is arachadonic acid? |
a fatty acid |
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what do FAS HAVE |
GPCR Family |
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how can you get fatty acids |
taken in by diet made in the system |
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explain characteristics of MCFA and SCFA |
Obtained from dietary fat de novo synthesis in the liver essential FA helps synthesis of PUFA |
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what are no esterified free fatty acids |
precursors of signalling molecules ( PGs and LTs) prostalgandins and leukotrienes acts as ligands directly on receptors (FFA GPCRS) |
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explain characteristics of SCFAs |
produced when dietary fiber is fermer microbiota of the gut |
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how do you want to know how FFA Are biologically made |
accumulation OF FFA in the sytstem |
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for FFA1 what is the fatty acids and signalling |
MCFA AND LCFA Gi Gq Gs and arrestin |
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for FFA2 what is the fatty acids and signalling |
SCFA gi gq and arrestin |
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for FFA3 what is the fatty acids and signalling |
SCFA Gi |
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for FFA4 what is the fatty acids and signalling |
SCFA AND MCFA gi gq and arrestin |
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what is arrestin ? |
a non G protein dependant - it is a scaffolding protein |
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explain FFA1 |
originally designated GPR40 crystal structure resolved |
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why is it good having knowledge of regions of ligand binding |
because you can design and develop new drugs |
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what has the highest potency |
LCFA PUFAs |
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what are poor agonists |
trans- unsaturated fatty acids |
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acute LCFA treatment does what |
enhance glucose-dependent insulin secretion |
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chronic LCFA treatment |
lipotoxity and inhibition of insulin secretion leading to signalling bias evoked from different LCFA ligands |
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explain FFA1 agonists crystal structura with TAK875 |
3 potential binding pockets positive allosteric modulation Tak875 a pam of LCFA responses Bias towards activation of specific pathways |
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TAK875 leads to what |
FFA1-> Arr2/3 |
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what happens in arrestin KO MICE |
insulintropic activity reduced |
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LCFAs change into what gq inhibition does what |
FFA1-> G Gq inhibition insulintropic activity ablated |
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how to track FFA1 ligands |
with fluorescent probes for ligand engagement |
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in receptors of FFA2, FFA3, and FFA4 |
FFA2-orthosteric/allosteric agonists FFA3- allosteric agonists FFA4- orthosteric agonist |