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Voltage-dependent K+ channel beta subunit (W121A) in complex with cortisone 3EB3. By Steven Shikhel. Shaker Family Voltage Dependent Potassium Channels . Denoted Kv1 Shaker Family because the Shaker (Sh) Gene plays a part in the role of the channel
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Voltage-dependent K+ channel beta subunit (W121A) in complex with cortisone 3EB3 By Steven Shikhel
Shaker Family Voltage Dependent Potassium Channels • Denoted Kv1 • Shaker Family because the Shaker (Sh) Gene plays a part in the role of the channel • Shaker channel is voltage dependent and has four subunits which form a pore through which ions flow • Essential for cellular excitability 1QRQ- Beta Subunit
Cortisone 17,21-DIHYDROXYPREGNA-1,4-DIENE-3,11,20-TRIONE PDN
Cortisone • steroid hormone, C21 H26 O5 • increases activity by binding to Kv beta 1 subunits. This is important because loss of function causes hyperexcitability and this is linked with episodic ataxia and atrial fibrillation. • promotes dissociation of Kv beta subunits, dissociation of kv beta 1 should eliminate inactivation and thus promotes cellular excitability. C21 H26 O5
NADPH DIHYDRO-NICOTINAMIDE-ADENINE-DINUNADPH DIHYDRO- NICOTINAMIDE-ADENINE-DINUCLEOTIDE PHOSPHATECLEOTIDE NDPPHOSPHATE NDP
NDP • Nothing specifically was said about NDP as it relates to the beta subunits • Most likely important in function of ion transport and structure since it is located centrally. C21 H30 N7 O17 P3
N-terminus Amine • The N-terminus is start of protein terminated with free amine –NH2 • I first highlighted all amines in yellow and then found an amine on a terminal part and colored it cyan • I believe that the red arrow pointing at cyan color is the N-terminus • N-terminal segment closes channel by N-type inactivation mechanism
The results found of Cortisone has launched a search to find other ligands that will fine tune cellular excitability