mod 6 Flashcards
types of signalling
endocrine (sinalling molecules are hormones)
paracrine: signalling are local mediators (growth factors, NO) produced at low []
autocrine: local mediators, low [], need receptors
neuronal: neurotransmitters
contact-dependent: cell surface and receptor contact
direct: flow of molecular traffic, gap junctions or plasmodesmata
the four types of cell surface receptors
- ion-channel- coupled receptors
- G-protein-coupled receptors
- enzyme-coupled receptors
- nuclear receptor
2 major signal mediators
signalling by phosphorylation (GEF)
&
signalling by GTP-binding (GAP)
what is Kd
the dissociation constant (describes the affinity)
G-protein coupled receptors (GPCRs)
there are 7 transmembrane spanning regions, and more than 800 GPCRs in the human genome, 40-50% of drugs target the GPCR activity
what did reed and Jones discover?
the G protein was identified in 1989
what are the 2 types of G proteins
monomaric and heterotrimeric g-protein
flight or fight
is kinases mediated, cAMP is the secondary messenger which activates a protein kinase called PKA (protein kinase A), results in increased glucose for muscle cells, glucagon or beta adrenergic is the receptor
PKA activation
increased cAMP levels lead to the PKA activity, when binded the subunits fall off allowing catalysis. the PKA can reguate gene expression
inositoltrisphosphate and diacylglycerol
both secondary messengers, initiated by phospholipase C
Calmodulin
involved in Ca signalling, it binds and activated other proteins, can change structure upon calcium binding and can reguate protein targets
Cytosolic domain has what features?
either has protein kinase activity or associates w a protein kinase, are bound often by growth factors
what are the 2 classes of protein kinase receptors
tyrosine kinase receptors and serine/threonin receptor kinases
what is the structure of teh tyrosine kinasses
unbounded, transautophosphorylation activates the receptor
Ras
monomeric GTPase, the SOS is activated by indirect binding ovia GRB2 to the receptor kinase