Section 4 (Exam 1) Flashcards
A ligand is a ___
signaling molecule involved in the reception stage
A polar ligand is located on the _____an example is_______
receptor on the cell membrane
peptide
A nonpolar ligand is located on the _____ and an example is ____
intracellular receptor
steriod
receptors can have _______ligands (s)
more than one and do different things
ex=epinephrine
name the 5 types of receptors
1) ion channel
2) Receptor Tyrosine Kinase
3) Janus Kinases
4) G-protein coupled receptor
5) Steroid Receptor
Explain what a Ion Channel or Ligand Gated Receptor is
Can be akin to a lock and key format. Once the messenger binds and phosphorylates the receptor, it opens the ion channel attached to it.
Form of facilitated diffusion
can be selectivity filter depending on the size and charge of the ion channel
Explain the Tyrosine Kinase Receptor
1) receptor binds with messenger and receptor phosphorylates its own tyrosine residues (forms a bubble on base of receptor)
2)the bubble is now a docking site for other proteins
3) the bound docking proteins than bind and activate more signaling pathways
Explain the Janus Kinase (JAK) Receptor process
1) ligand binds to receptor and causes a conformational change (changes shape)
2)leads to activation of JAK (forms boob that JAK holds onto)
3) JAK phosphorylates proteins containing Tyrosine
4) JAK kinases phosphorylates different target proteins which increases the synthesis of proteins
What is the difference btw Tyrosine Kinase and JAK
Tyrosine is an independent man and auto-phosphorylates himself
JAK is a protein on the receptor that then phosphorylates
Explain the basic approach to G-protein coupled
1) 7 membrane spanning a-helical region coupled to separate G-protein
2) Ligand binds to receptor which releases GDP from alpha subunit and replaced with GTP
3) alpha subunit than dissascioates from G protein and moves across membrane to effector
4) GTP is replaced with GDP again on the alpha subunit, alpha heads back to beta and gamma. Effector begins its job
Explain the receptor for Steriods
found inside the nucleus (nuclear receptors)
acts as a transcription factor
non-polar steroids head straight into the cell because they are resemble cholesterol?
turns on transcription of genes (long lag time because you’re building new dna
Explain Down Regulation and Up-regulation
UP REGULATION:
lowers percentage of ligands for a bit
increases sensitivity for ligands
ex) low neurotransmitters in damaged muscle tissue, muscle will easily respond to less transmitters
DOWN REGULATION:
high percentage of ligands
reduces cell’s responsiveness (negative feedback)
occurs from receptor internalization (recycling of receptors)
What are some advantages to cells expressing receptors for certain ligands?
more likely for messenger or hormone to be picked up by their specific ligand. Allows the body to do very specific tasks without causing unwanted side effects
Explain the relationship btw binding of ligands to receptors as it relates to structure is a determinant of function.
because of the structure of receptors they can only bind to certain ligands which allows them to only “do their thing” when the body wants them too. Allows for specificity and affinity.
What is a benefit of G-protein coupled receptors
signal amplification (cascade effect)
What are some unique characteristics for Gas Pathway
uses adenylate cyclase as effector
2) amplification =cAMP-> PKA
through catalytic enzymes
3) creb->cre->transcription
cAMP is a ____ _____
second messenger
The effector of GAS is …..
adenylate cyclase (atp-cAMP)
cAMP binds to _____
mothership (PKA) which releases catalytic domains
How do we stop the G alpha s pathway?
hydrolyze GTP-GDP
and Phosphodiesterases (PDEs regulate cAMP)
In intestinal cells, cholera causes _______ ______ of G protein that activates adenylate cyclase (causes opening of Cl-channels)
sustained activation
Cl leaves with Na and H20, leaving the patient dehydrated despite water consumption
15-20 L PER DAY
Define Methylxanthines and give two examples
Also, how does this relate to dogs?
Methylxanthines INHIBIT phosphodiesterases (regulate cAMP) which causes CFTR channels to be constantly open.
ex) caffeine and dark chocolate
Dogs can break down Methylxanthines and have constant cascade effects and constant CFTR openings. This leads to diarrhea and vomiting and kills the patient via dehydration.