Introduction
This scene is of the within the Kappa Opioid Receptor by Group 3.
-"Kappa-Opioid receptors mediate the regulation of pain, respiratory drive, mood"
-"structure reveals important features of the ligand-binding pocket that contribute to the high affinity and subtype selectivity of JDTic for the human kappa-OR"
-consequences of stress as well as depression/anxiety
-hallucinogenic effects
-talk about mu and kappa OR
-intro to kappa-OR subtype selectivity
Overall Structure
-describe the overall size of the molecule: how massive it is, how many alpha helices and beta sheets it contains.
-describe the two different dimmers that form the protien and how and along which alpha helices the dimmers coordinate with each other
-describe how the protein fits in the cell membrane, how much is contained in the membrane.
-describe which parts are conserved and which parts make it a unique molecule like how the sulfide bond near the n-terminus among other feature distinguishes itself from CXCR4
-describe the structure and shape of the binding pocket, discuss how these structural conformations make it unique.
Binding Interactions
Active Site of kappa Opioid Receptors
Common Ligands of Opioid Receptors
Agonists - Mechanisms, Structure, and Effects
Salvinorin A
Morphine
Antagonists - Mechanisms, Structure, and Effects
JDTic
Naloxone
Additional Features
-Show Hydropathy plot displaying opioid receptor as an amphipathic alpha helix
-Show Ramachandran plot displaying different phi and psi angles of receptor with different substrates bound.
- is a long acting antagonist to the k-opioid receptor that binds with high selectivity to only the kappa variant.
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Quiz Question 1
-include some basic structure of , maybe show charge distribution
- Where are the binding sites of the opioid receptor (OR why are the binding sites located here in jmol), and what conformational changes does the protein undergo while binding to ligands? What kinds of functional groups would opioids have that interact with these sites, enabling binding?
Quiz Question 2
What properties would a substrate binding to the active site of the Kappa-opioid receptor probably possess? Explain your reasoning.
See Also
Credits
Introduction - Patrick Harney
Overall Structure - Matthew Long
Drug Binding Site - Brandon Kittredge
Additional Features - Jacob Kellet
Quiz Question 1 - Leah Caffrey
Quiz Question 2 - Bridget Kilkenny
References
