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GPCR Edition – Week 2

GPCR Edition – Week 2. G proteins. IP3/DAG Pathway. GPCR Activation. Second Messengers. GPCR Regulation. Experime-ntal Methods. 100. 100. 100. 100. 100. 100. 200. 200. 200. 200. 200. 200. 300. 300. 300. 300. 300. 300. 400. 400. 400. 400. 400. 400. 500. 500. 500.

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GPCR Edition – Week 2

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  1. GPCR Edition – Week2

  2. G proteins IP3/DAG Pathway GPCR Activation Second Messengers GPCR Regulation Experime-ntal Methods 100 100 100 100 100 100 200 200 200 200 200 200 300 300 300 300 300 300 400 400 400 400 400 400 500 500 500 500 500 500

  3. The heterotrimeric G protein complex is composed of G-alpha, G-beta, and this other G protein G-gamma

  4. These two G proteins subunits remain as heterodimers after G protein complex activation G-beta & G-gamma

  5. Activation of G-alpha leads to exchange of these two nucleotide phosphate molecules GDP & GTP

  6. This class of G-alpha proteins is responsible for activating adenylylcyclase (AC) Gs

  7. Activated G proteins bind to and regulate the function of this general type of proteins involved in second messenger signaling Effector proteins

  8. This membrane-bound enzyme is the effector protein that generates IP3 and DAG Phospholipase C (PLC)

  9. PIP2is enzymatically cut to form IP3 and this molecule Diacylglycerol (DAG)

  10. IP3 will stimulate the release of this cation from particular ion channels in the endoplasmic reticulum Calcium (Ca2+)

  11. This protein kinase requires Ca2+ and DAG to be fully active PKC

  12. This protein changes its conformation upon Ca2+ binding and modulates the activity of many proteins, including NOS and kinases Calmodulin (CaM)

  13. ligands that activate a GPCR are known as this agonists

  14. Ligands binding to the extracellular domains of the GPCR cause conformational changes in these domains Intracellular

  15. GPCRs, unlike light switches, can be fine tuned to have a specific signal depending on the cell type and ligand, much more like this analogy rheostat

  16. This 3-amino acid motif in a GPCR is critical for Gprotein binding and activatioin DRY motif

  17. Activated GPCRscan have their signaling down or off by proteins like beta-arrestin in a process known as this desensitization

  18. Adenylylcyclase uses this molecule as a substrate for cAMP synthesis ATP

  19. Formed by guanylylcyclase and activates PKG Cyclic GMP (cGMP)

  20. cAMP binds to this subunit of PKA to activate the catalytic subunit regulatory

  21. This G-alpha subunit lowers the level of cAMP by inhibiting adenylylcyclase Gi

  22. DAILY DOUBLE This enzyme is responsible for breaking down cyclic nucleotides Phosphodiesterase (PDE)

  23. Phosphates are added to this intracellular domain of an agonist-bound GPCR C-tail/terminus or ICL3

  24. This enzyme phosphorylates active GPCRs GRK

  25. The process of bringing a GPCR off the membrane and into the cell is known as this endocytosis

  26. This protein is responsible for linking a phosphorylatedGPCR to proteins like clathrin and AP-2 (Beta-)arrestin

  27. Clathrin heavy and light chains come together to form this three-pronged quaternary structure triskelion

  28. Ion-exchange, gel-filtration and affinity are all types of this method to purify proteins Column chromatography

  29. The process of introducing a mutation into a specific position within a gene is known as this Site directed mutagenesis

  30. In flow cytometry side scatter measures the overall internal complexity of a cell, while forward scatter measures this Size/shape

  31. This process uses short sequences of ssRNA to prevent the translation of a particular mRNA inside a cell RNA interference (RNAi)

  32. The heisman and national championship Florida QB shown here Tim Tebow

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