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MCB Exam 2 - part 3

Agrawls cell receptors

Where will a steroid hormone (including RA, thryroid hormone, corticosteroids) have its receptor? Intracellularly - either in the cytoplasm or nucleus
What does it mean to say that a receptor is saturated? All the receptors are bound by ligaand, and because there is an finite amount of receptors, increasing ligand will not increase effect of ligand
An enzyme that removes acetyl groups on histones is ____. Normally it is bound to _____ in the cytoplasm, but is freed when the hormone _______ passes the cell membrane to bind to the enzyme. The enzyme _____ adds acetly groups to prevent acetylation. HAT; Hsp90; Steroid hormone; HDAC Steroid;
The signaling molecule NO is derived from the amino acid ___and is converted to NO by the enzyme _____ Arginine; NOsynthase
The majority of hydrophilic signaling molecules are ____. Neurotransmiters
A hormone's affinity for a receptor can be measured with the value ____, which is defined as the concentration of chemical needed to achieve ____% occupancy of its receptors. What 2 values does this measure depend on Dissociation constant (Kd); 50%; Kd = K2 (dissociation) / K1 (association) - thus low Kd values indicate high affinity
The 2 main structural types of cell receptors are ____ which activate G proteins on the cytosolic side, and _____ which contain an alpha, beta, and gamma subunit. 7-transmembrane domain receptor; Single domain receptor
In the process of tachyphylaxis (more commonly known as ____) prolonged binding of hormone to receptor causes what to happen? Desensitization (or "Fade Phenomenon"); BARK (g-protein coupled kinase) to phosphorlate the receptor causing it to undergo clatherin-mediated endocytosis to "sequester" the receptor in a vesicle until resensitization occurs
What 2 signaling pathways generally recquire G-protein activation? Which pathway does NOT use G-proteins? Adenylate cyclase and PI turnover; Receptor Tyrosine Kinase
Which subunit (in both heterotrimeric and monomeric G-proteins) binds GTP/GDP and determines if action will be inhibitory or stimulatory? What subunits can also sometimes activate downstream targets? Alpha; Beta
When ____is bound to a G-protein's alpha subunit, alpha is complexed with the beta/gamma subunits and inactive. ____ activates alpha and causes it to dissociate from beta/gamma, while _____ inactivates it. GDP; Nucleotide exchange (for GTP); GTP hydrolysis
Ras is an example of a ______ G-protein. The enzyme ____ turns Ras on by exchanging GDP for GTP. The enzyme ____ turns Ras off by hydrolyzing the GTP to GDP. Monomeric; GEF; GAP
In the adenylate cyclase pathway, hormone binding causes alpha subunit to activate the enzyme _____ which converts ATP into the secondary messenger _____. To turn off the pathway, the enzyme ____ converts the secondary messanger into AMP. Adenylate cyclase; cAMP; cAMPphosphodiesterase
In the adenylate cyclase pathway, cAMP binding activates the enzyme ____. The enzyme moves to the nucleus where it phosphorolates the TF ______ bound to ____promoters. The enzyme ______ regulates PKA by dephosphorolation. PKA; CREBs; CRE; Protein Phosphotase-1
Bronchodilation and Olfactory signal transduction all utilize what signaling pathway? Adenylate cyclase
In photoreceptors, the receptor is_____ which contains a small molecule that detects light called_____. The receptor activates the G-protein ____ which in turn activates a _____. This results in a decrease cGMP causing cGMP-gated ion channels to open. Rhodopsin; Retinal; Transducin; Phosphodiesterase
In the PI turnover pathway, hormone binding activates the enzyme _____ which converts PIP2 into _____ (which activates PKC) and ____ (which binds receptors on the ER membrane to cause and increse in intracellular _____) Phospholipase C (PLC); DAG; IP3; Calcium
After IP3 increases Calcium in the PI turnover pathway, calcium bind a protein to form the ______. This complex, along with PKA, cause muscle contraction and if the repiratory tract this causes ____ Calcium/calmodulin-dependent protein kinase; Bronchoconstriction
Binding of histamine to ____ receptors causes activation of the PI turnover pathway. These receptors are generally found in the ___. Binding of histamine to ____ receptors activates the adenylate cyclawse pathway. These receptor are found in the _____. H1 receptors - airways; H2 receptors - GI tract
In addition to stimulating mm contraction, increases in intracellular calcium also induces _____. What 2 effects does this cause? Arachidonic acid metabolism (breaks down cell membrane lipids to via PLA) - causes pro-inflammatory response (via leukotrines) and vasoconstriction/platlett aggregation (via prostoglandins)
In the tyrosine kinase receptor pathway, ____binding causes the receptor to dimerize and autophosphorolate to expose the ____ domain. 2 enzymes that can bind here are ____ and _____. Growth factor (can also activate the Ras-Raf-MAPK pathway!); SH2 domain; PLC and PI-3 Kinase
PI-3 Kinase (activated in the tyrosine kinase pathway) coverts PIP2 into PIP3. PIP3 binds ____which is phos/activated by ____ bound to PIP2. This causes an increase in TF's used in ____ and inactivates the protein ____ which normally causes apoptosis Akt; PDK1; Translation; FoxO
In the adenylate cyclase pathway, ___ causes an increase in cAMP, ___ causes inhibition of cAMP and activation of phospholipases and phosphodiesterases, ____ cause PIP2 → DAG and IP3 αs; αi; αq
Regulation of the tyrosine kinase pathways is accomplished via 2 proteins: ___ which regulates PI3-kinase, and ___ which regulates Akt. What is the net effect of these 2 regulators? PTEN; PP2A; Increase apoptosis and decrease cell proliferation
Insulin, EGF, and TGF-ß all activate which pathway? Which of the 3 does not follow the typical pathway? Tyrosine kinase pathway; TNF-ß - activates SMADs instead of Ras or Akt
In cytokine signaling, tyrosine kinases (that are NOT part of the receptor), called ___ are activated. The kinase then phosphorolates ____ which dimerizes and moves to the nucleus. This signaling can also activate the __ pathway JAK; STAT; Ras-Raf-MAPK(MEK-ERK) pathway
The only cytokine to not use JAK/STAT pathway is ___. Instead it binds to the receptor ____ to activate ___ to lead to apoptosis or to the receptor ____ to activate ___ pathway to cause cell survival. TNFα; TNFR1; capases; TNFR2 NF-KB
Binding of the cytokine ___ activates JAK1/3 and STAT6 to causes IgE, mucous, chemokine production. Binding of the cytokine ___ causes activation of JAK3, Tyk2, and STAT4 to cause Th0 cells to differentiate into Th1 cells. IL-4; IL-12
Cytokine signaling can be regulated by phosphotases, but the main regulator is ____. In what 2 ways does it inhibit the JAK/STAT pathway? SOCS; binds JAK and inhibits it and it covers the SH2 domain of JAK to prevent binding/activation of STAT
A type of high affinity IgE receptor found on mast and basophil cells is ____. Binding of the receptor by IgE causes dimerization that activates the ___ pathway. What are the 3 main results of activation? FcεRI; JAK/STAT; arachadonic acid metabolism (inflammation), TNF release, and histamine release
The 2 main trasncription factors involved in inflammation is ___ composed of p50-p65 and ___ composed of fos and jun. These TF's are activated by ___ binding. NF-KB; AP-1; cytokine and adhesion molecule
The main inhibitor of NF-KB (p50 + p65) is ___, which gets ub-ed and degraded when cytokines bind. In addition, the ___ and ___ pathways can also activate NF-KB. IKBα; MAPK and PLC pathways
Corticosteroids cross the cell membrane to bind ___ which binds/inactivates NF-Kß. In addition, this hormone increases the inhibitor ___ and inhibits inflammtory genes. GR; IKBα
Created by: c.phill