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CHEM430 Study Guide - Final Guide: Retinoic Acid Receptor Alpha, Retinoid X Receptor, Thromboxane A2

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Michael Palmer
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-inhibits tubulin polymerization
-binds between alpha and beta tubulin
-inhibits mitosis (makes up mitotic spindle) and promotes apoptosis
-cancer chemotherapy
-inhibits cross linking of bacterial cell wall (same as penicillin but different
-binds terminal of D-alanine dipeptide and inhibits transpeptidase reaction
-works on gram positive bacteria only
-cell surfers osmotic lysis
-resistance took a while to develop, used to treat MRSA
-resistant strains change D-alanine-D-alanine peptide to D-alanine-D-
opossible solution is vancomycin derivative with amidine group
-potassium ionophore – inserts itself in cell membrane and makes
-permeabilizes pro and eukaryotic cells
-experimental (research) not clinical
-protein molecule
-dissolve blood clots in stroke or heart attack
-plasminogen activator cleaves plasminogen to plasmin to dissolve blood
-urokinase can do this too
-sulfonylurea receptor agonist
-GPCR (I think)
-closes Kir channel
-promotes insulin secretion from beta cells
-closing Kir channels increases the membrane potential  calcium-
mediated insulin release
-a sulfanilamide activated through reductive metabolism (prodrug)
-only active in vivo
-antimetabolite of folic acid synthesis
-can be used in humans because we acquire folic acid from the diet
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-cholinergic receptor agonist
-selective agonist for subtype found in motor endplates
-renders muscle unresponsive to presynaptic release to acetylcholine
-muscle relaxation – suppress pain reflexes in spinal cord
-used as adjuvant to system narcosis
Sildenafil (Viagara)
-NO – vasodialation
-NO increases cGMP
-Viagara inhibits PD5 – which converts cGMP to GMP
-Promotes vasorelaxation
-HIV protease inhibitor
-HIV genome is in polypeptide and protease first cleaves itself then other
-Inhibit protease so then other protein components wont be functionl
-inhibits Cox-2 noncovalently
-Cox-2 expressed by inflammatory cells was thought inhibiting only Cox2
and not 1 would be good
-However there were many more heart attacks with these drugs
-Because Cox2 is a vasodialator and cox1 is a vasorestrictor (I think ...
double check?????)
Retinoic Acid
-anticancer agent in premyelocyte leukemia – caused by translocation of
PML and RARA genes – makes PML-RARA and RARA-PML
oPML-RARA is oncoprotein
oRARA is retinoic acid receptor alpha
-Cells differentiate to myelocyte need activation of RARA with retinoid X
receptor (RXR)
-In cancer – PML-RARA will form heterodimers with RXR without retinoic
acid and cause aberrant transcriptional regulation, differentiation does not
occur, so premyelocytes accumulate and proliferate, and there is not
normal blood cell formation
-Treat with excess retinoic acid (to make up for reduced affinity of mutant)
and it can bind
-Also promotes degredation of the protein and RXR can combine with
intact RARA and cell differentiation resumes and premyeolocyte
prolifersation ceases
-thromboxane A2 and its receptor blocked by ramatroban
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