Konorev DSA: Drug Targets Flashcards
What does Gs do?
-activates all isoform of AC and Src tyrosine kinase
What doe Gi do?
-inhibits AC but activates tyrosine kinase Src
What does Gq do?
-activates PLC
What happens when we activate a GABA-A receptor?
-inward flux of Cl-….. hyperpolarization
NAch receptor activation
- binds to alpha receptors
- inward Na flux… depolarization
What is a JAK receptor?
-receptor coupled to cytosolic protein kinase
How is JAK receptor different from RTK?
-RTK has intrinsic enzymatic activity
What happens to a GPCR after it gets activated too much?
- gets phosphorylated then B arrestin latches on…… gets internalized (desensitization).
- it reverses back pretty quickly once the ligand leaves
What is an inert binding site?
-the drug binds to it but doesn’t change its function
What do we call the molecule that binds to a receptor?
-the ligand
What is the specific DNA sequence that transcription factors bind to called?
-the response element!
What does DAG activate?
-PKC
True or False, GTP hydrolysis by Beta gamma subunit will terminate the activity of a GPCR.
- False
- GTPase activity is only present in the alpha subunit!
When Active, Gaq results in the increased level of PIP2… is that correct?
- no
- it makes PIP2 turn into IP3 via the activation of PLC!
- so , the concentration of PIP2 will actually decrease
When a boy is using the a B2 adrenergic agonist and it stops working as good, what is the first thing that is happening to the receptor?
- it gets “P”ed first
- then B arrestin binds to it
- then it binds to the coated pit
- gets internalized
What kinds of receptors are growth factors normally?
- RTKs
- so, if there is “GF” anywhere in the name, it’s probs an RTK
What do proteins that contains a SRC homology 2 domain bind to?
- proteins that have a phosphotyrosyl residue
- SH2 binds to P’ed RTK
- SH3 binds SH2… then SOS (which is a GEF) binds to SH3
What is Ras?
-a monomeric GPTase
What is Grb2?
-an adaptor ptn
What is Sos?
a GEF
What chemical messenger passes through the plasma membrane of cells and has receptor molecules in the cytoplasm?
-Testosterone apparently
What is phosphorylated as a result of binding of a cytokine like IL-2 to its receptor?
- STAT protein
- JAK/STAT signaling
- STAT comes over when receptor is activated… magic happens
do voltage gated channels open and close in response to a chemical signal?
-no! VOLTAGE
Binding of a NT to which type of receptor directly leads to a change in distribution of ions between extra and intracellular compartments?
-Ligand-gated ion channels
