Term
Macromolecular Target
Clofibrate |
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Definition
Macromolecular Target
Clofibrate = PPAR |
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Term
Macromolecular Target
Lead |
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Definition
Macromolecular Target
Lead = ALAD |
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Term
Macromolecular Target
Pertussis Toxin |
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Definition
Macromolecular Target
Pertussis Toxin = G-protein Gα-i |
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Term
Macromolecular Target
Cholera Toxin |
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Definition
Macromolecular Target
Cholera Toxin = G-protein Gα-s |
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Term
Macromolecular Target
Dioxin/TCDD
Order Sensitivity |
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Definition
Macromolecular Target
Dioxin = Ah Receptor
must bind with AHR/HSP90/ARA9
HIF is competitor
weightloss is correlation not caused by p450 induction
Amino acid Ile 332/ser makes more sensitive,
ILE/ala, Val/ala |
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Term
Macromolecular Target
Botulinum A Toxin |
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Definition
Macromolecular Target
Botulinum A = VAMPS |
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Term
Macromolecular Target
Parathion |
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Definition
Macromolecular Target
Paration = AchE |
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Term
Macromolecular Target
Muscarine |
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Definition
Macromolecular Target
Muscarine = Mucarinic Receptor |
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Term
Macromolecular Target
Nicotine |
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Definition
Macromolecular Target
Nicotine = Nicotinic Receptor |
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Term
Macromolecular Target
Tubocurare |
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Definition
Macromolecular Target
Tubocurare = Nicotinic neuromuscular acetylcholine receptors |
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Term
| G-Protein linked Receptor Sequence |
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Definition
Ligand binds to GPCR causing activation and conformational change
GDP bound to Gαs is replaced by GTP and G-beta and G-gamma dissociates from G-alpha
G-alpha binds to adenylyl cyclase to activate it causing it to catalyze formation of cAMP, raising cAMP levels
cAMP dependant protein kinase causing activation of pka
pka goes into the nucleous, Atp ->ADP activates CREB by phosphorylation
CBP binds to CREB and then binds to cAMP response element causing transcription
G-beta activates phospholipase C which cleaves IP3 from biphosphate and activates Ca2+ channels in ER
Ca2+ activates protein kinase C |
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Term
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Definition
Two Domains:
A = Catalytic Domain
B = Transmembrane/Receptor Domain
Low iron, uses siderophores to sequester and produces toxin. High iron no toxin made
A & B Toxins are cleaved by protease but stay together due to a disulfide bond. The cleaveing activates dip. tox.
binds to HB-EGF and enters cell through endocytosis
The proton pump by V-type ATPase causes acidification 7 to 6 in vacuole resulting insertion into the membrane
A domain is fully cleaved from B domain, A domain crosses the membrane and affects EF2 function by inhibiting the translocation of tRNA from A-site to P-site |
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Term
| Critical Amino Acids in epoxide Hydrolase and why |
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Definition
Y381-OH and Y465-OH hydrogen bond with the O on epoxide faciltates nucleophilic attack by
ASP333-COO- attcks epoxide ring leading to formation of hydroxylacyl intermediate
His523 and ASP495 hydrolyze the intermediate allowing ASP333-COOH to disassociate |
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Term
| Cholinergic neuromuscular junction sequence |
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Definition
Ca2+ enters and binds to SNARE complex (VAMP & SNAP on vesicles) ,opening Ca2+ ion channels
Once bound, the vesicle is docked on presynaptic membrane and releases neurotransmitters. Ach binds to AchR on post synaptic vessicle and triggers transmission of signal flow.
Na+ enters cells and depolarizes, if threshold is reached and action potential triggers.
Sarcolema repolarizes as K+ flows, NA/K pump restores ions.
AcHE cataylzes degradation of Ach in synapse. |
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Term
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Definition
Dioxin binds to AhR,
AhR and Arnt attach to Dioxin repsonse element
CYP1A1 expressed |
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Term
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Definition
Steriod (Rifampicin) binds to PXR, cis-9-retinoic acid binds to RXR
PXR and RXR attach to XREM |
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Term
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Definition
colfibrate binds to PPAR, Cis-9-retinoic acid binds to RXR
PPAR and RXR attach to PPRE
CYP4 expressed |
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Term
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Definition
fatty acids/cholesterol binds to LXR, CXR
LXR and CXR attach to LXRE
CYP1A1 expressed |
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Term
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Definition
Phenobarbital binds to CAR, cis-9-retinoic acid binds to RXR,
CAR and RXR attach to Phenobarbital repsonse element
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Term
| Important Amino Acids in Glutathione |
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Definition
Normally GSH is pH7 then when bound to GST pH 5-6, GSH is not very active but is in presence of GST. Alpha is most predominate
Gsite and binds to GSH, H site is lipophilic and binds to substrate
Y-6 on G site forms the electrophile pocket, its acidic and allowing gsh to be ionized and perform nucleophilic attack on epoxide,
S-209 forms hydrophobic pocket, facilliating Y115
Y-115 acidic h site, forms the substrate pocket, is electron acceptor |
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Term
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Definition
(+)7,8 diol 9,10 epoxide-2 (anti)
(-)7,8 diol 9,10 epoxide-1 (syn)
(+)7,8 diol 9,10 epoxide-1 (syn)
(-)7,8 diol 9,10 epoxide-2 (anti)
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Term
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Definition
| Take regulatory part of gene and attach a reporter gene. Remove parts of regulatory gene and monitor reporter to know which part of gene is important |
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Term
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Definition
mEH - Cis, microsomal epoxide hydrolase, ER metabolism
sEH- Trans, soluble epoxide hydrolase, cytoplasm metabolism |
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Term
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Definition
Cox pathway -> pain
LOX pathway -> Leukotriene = allergies
CYP2 Epoxygenase -> EETs = hypertension adds epoxide to any double bond
CYP4 hydrolase -> Hetes Adds adds an OH to CH3 |
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Term
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Definition
Leukotrine A4 -> LTB4 by hydrolase no acyl group
or A4-> C4 Glutathioe transferase loses glutamic acid
c4-> d4 CGP takes off glycine and becomes acetyl group
d4->e4 acetyl group is transfered becomes amine
e4 -> f4 formation mercapturic acid |
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Term
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Definition
Toxin enters membrane, gets metabolized by P450, goes to UDPGA, UGT->UDP, and then leave cell as toxin-glucuronide,
UDP -> UDPse -> UMP -> Translocase trades cytoplasm UDPGA into ER from UMP to cytoplasm |
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Term
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Definition
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Term
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Definition
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Term
| P-type pumps, f-type pumps, v-type pumps, abc transporter |
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Definition
p = ion pump ATP to pump out
f-type = H+ pump builds ATP and makes acidic
V-type = same as f type but in vacuole
ABC uses 2 ATP to pump molecule out |
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Term
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Definition
| bHLH is DNAbinding with PAS-A, secondary dimerizization is PAS, B is ligand binding, |
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Term
| Clostridium c2 toxin target |
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Definition
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Term
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Definition
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Term
| Tetanus Toxin and botulism toxin mechanism |
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Definition
binds Bot A. binds to SV2, bot. B binds to synaptotagmin, inside vesicle before it buds
buds and retrograde transport into the cell,
acidification inside vesicle due to atpase proton pump
conformation change allowing inserting into membrane
A domain is release in cytoplasm
Bot A. cleaves SNAP-25
Bot B. cleaves synaptobrevin
Tetanus cleaves VAMP
leads to no vesicle docking and no neurotransmitter release |
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Term
Parasympatheic
Sympathetic |
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Definition
Parasympathetic: Long pre, short Post, Ach
Sympathetic: short pre long post,Ach, Ne |
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Term
Muscarinic receptor
Nicotinic receptor |
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Definition
Muscarinic = gprotein receptor
Nicotinic = ligand gated |
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Term
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Definition
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Term
Types of receptors
GABA A & C
GABA-B |
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Definition
Transmitter gated channel = GABA A&C
GPCR - GPCR |
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Term
| Important Amino Acids of ACHE |
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Definition
Peripheral site – allow the substrate to enter, determine affintiy, W279,Y121,F330
Catalytic site - charged residue of Ache, this is required for binding, S200, Hist440, E327 |
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Term
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Definition
| organophoste binds to ACHE, ethylene is removed, permanant addition |
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Term
| GSH reacts with dibromide |
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Definition
GS is - and H is +
GS attacks Br/\/Br -> SG/\/Br- -> GS+ triangle |
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Term
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Definition
HIST 108 extract proton from OH and Sulfate, another OH attacks sulfur in SULT producing and intermediate
-OH on substrate becomes -OSO3 |
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Term
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Definition
Nicotine -UGT-> add Glu onto empty N
Nicotine -CYP2-> add =O on CH2 to the right of N-CH3 -UGT-> to add glu onto emtpy N
Nicotine -CYP2-> add =O on CH2 to the right of N-CH3 -CYP2-> -OH to right of =O -UGT-> -OH to -OGlu |
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Term
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Definition
BAP is 2 on top of 3 rings
P450 add epoxide on bottom left or top left and its either down or up. Epoxide hydrolase makes them OH's the one closest to the bay region matches up/down of epoxide other -OH is opposite. then P450 act on which ever it didn't act on fisrt making another epoxide. Epoxide hydrolase can break and then It can then react with N7 on DNA and then be removed by aicd hydrolysis.
If GST/GSH breaks 2nd you get -oh -SG |
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