Receptors and signaling Flashcards
Example of juxtacrine signaling is
Ephrin
Norepinephrine:
In muscle -
In pancreas -
Contract smooth muscle
Decrease insulin
T/F: Antagonists lower the response of the cell
False. They cause no response(named above is inverse agonist)
Ach … heart but … skeletal muscles
Epinephrine … airways but …skeletal muscles
relaxes, contracts
x2
RTK…
1) Growth factors
2) Autophosphorylation
3) Must dimerize to do so
4) MAPK (important in cancer) pathway
- GRB2(SH2 domain), SOS, RAS(+GTP), RAF-1, MEK, ERK > nucleus for transcription
RGC…
Membrane-bound:
1) ANP, BNP, CNP
2) Single-pass
3) cGMP - PKG
Soluble:
1) NO (activated by Ach, bradykinin, substance P, Ca2+)
- Ca2+ > NO synthase
2) Treat angina pectoris, NT, macrophage/neutrophils destroy invaders
3) Sildenafil(inhibits PDE > increase cGMP and relaxation of vessels), REVATIO(blocks PDE for pulmonary hypertension)
RTK associated…
1) Must dimerize
2) JAK/SRC
3) JAK cross-phosphorylate each other > receptor phosphorylates > STAT > nucleus for transcription
Ser/Thr kinases…
1) TGF-B
2) Ligand binds type II then type II bring type I’s together and phosphorylate.
RTP…
1) CD45 at T, B lymphocytes
2) CD45 dephosphorylated > activates LCK FYN > they phosphorylate other proteins
Tyrosine phosphorylated by… and dephosphorylated by…
TK, Phosphotyrosine phosphatase(PTP)
GPCR…
1) 7 membrane-spanning alpha helices(5-6 bind)
2) alpha and B-Y of G-protein both have effects
3) alpha G has GTPASE activity to shut off
cAMP pathway…
1) Gs of @G activates AC
2) ATP > cAMP(In cortex aldosterone and cortisol secretion, in kidney water retention)
3) PKA
4) PDE = cAMP > AMP
Caffeine, Theophylline inhibits PDE
Epinephrine in fat cells: triglyceride breakdown
Epinephrine in the liver: glycogenolysis/gluconeogenesis
DAG, IP3 pathway…
1) Gq activates PLC
2) PIP2 = IP3 + DAG
3) DAG > PKC
4) IP3 opens Ca2+ channels on ER > PKC
COX:
Lipoxygenase:
Epoxygenase:
Function?
1) Thromboxanes, prostaglandins, prostacyclins
2) 5-HETE, leukotrienes
3) HETE’s, EET’s
Vasoactive, platelet action, modulate ion transport
Blood vessels, inflammation
NSAID’s are… They…Inhibit…
1) non-steroidal anti-inflammatory drugs
2) Relieve pain, fever, inflammation
3) PLA2