Human 5-HT3A -- Lys 277

Species Original Mutated to Mutation
Human Lys 277 (4')

Arg

Gln

Ser

Gly

K277R

K277Q

K277S

K277G

Rat Equivalent Lys 276    
Mouse Equivalent Lys 282 Cys K282C

 

hLys277Arg

Imax (pA) EC50 (uM) nH Vrev (mV) Activation (10-90% rise time, ms) Desensitization (t1/2,s) Conductance (fS)
Wild Type 656 +/- 170 2.34 +/- 0.06 2.87 +/- 0.35 -9.0 +/- 1.6 103 +/- 9 (11) 5.0 +/- 0.5 (12) 390 +/- 15
K277R 569 +/- 89 1.50 +/- 0.08 2.97 +/- 0.18 -6.8 +/- 0.4 106 +/- 15 (7)

26.6 +/- 2.8 (11)

478 +/- 42

 

Gunthorpe MJ, Peters JA, Gill CH, Lambert JJ, Lummis SCR (2000) The 4'Lysine in the Putative Channel Lining Domain Affects Desensitization but not the Single-Channel Conductance of Recombinant Homomeric 5-HT3A Receptors. Journal of Physiology 522(2):187-198

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hLys277Gln

Imax (pA) EC50 (uM) nH Vrev (mV) Activation (10-90% rise time, ms) Desensitization (t1/2,s) Conductance (fS)
Wild Type 656 +/- 170 2.34 +/- 0.06 2.87 +/- 0.35 -9.0 +/- 1.6 103 +/- 9 (11) 5.0 +/- 0.5 (12) 390 +/- 15
K277Q 775 +/- 117 1.47 +/- 0.06 2.77 +/- 0.47 -10.6 +/- 0.9 115 +/- 16 (6)

8.2 +/- 0.8 (11)

441 +/- 35

 

Gunthorpe MJ, Peters JA, Gill CH, Lambert JJ, Lummis SCR (2000) The 4'Lysine in the Putative Channel Lining Domain Affects Desensitization but not the Single-Channel Conductance of Recombinant Homomeric 5-HT3A Receptors. Journal of Physiology 522(2):187-198

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hLys277Ser

Imax (pA) EC50 (uM) nH Vrev (mV) Activation (10-90% rise time, ms) Desensitization (t1/2,s) Conductance (fS)
Wild Type 656 +/- 170 2.34 +/- 0.06 2.87 +/- 0.35 -9.0 +/- 1.6 103 +/- 9 (11) 5.0 +/- 0.5 (12) 390 +/- 15
K277S 979 +/- 364 1.54 +/- 0.04 2.39 +/- 0.34 -8.6 +/- 2.3 99 +/- 10 (6)

11.2 +/- 1.2 (10)

455 +/- 28

 

Gunthorpe MJ, Peters JA, Gill CH, Lambert JJ, Lummis SCR (2000) The 4'Lysine in the Putative Channel Lining Domain Affects Desensitization but not the Single-Channel Conductance of Recombinant Homomeric 5-HT3A Receptors. Journal of Physiology 522(2):187-198

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hLsy277Gly

Imax (pA) EC50 (uM) nH Vrev (mV) Activation (10-90% rise time, ms) Desensitization (t1/2,s) Conductance (fS)
Wild Type 656 +/- 170 2.34 +/- 0.06 2.87 +/- 0.35 -9.0 +/- 1.6 103 +/- 9 (11) 5.0 +/- 0.5 (12) 390 +/- 15
K277G 545 +/- 271 1.39 +/- 0.10 2.73 +/- 0.27 -8.2 +/- 1.9 119 +/- 6(5) 20.3 +/- 2.0 (11) 429 +/- 32

 

Gunthorpe MJ, Peters JA, Gill CH, Lambert JJ, Lummis SCR (2000) The 4'Lysine in the Putative Channel Lining Domain Affects Desensitization but not the Single-Channel Conductance of Recombinant Homomeric 5-HT3A Receptors. Journal of Physiology 522(2):187-198

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mLys282Cys

After the application of 1mM MTSET with 10uM 5-HT, there was no significant change. After the application of 1mM MTSES with 10uM 5-HT, there was no significant change.

 

Reeves DC, Goren EN, Akabas MH, Lummis SCR (2001) Structural and Electrostatic Properties of the 5-HT3 Receptor Pore Revealed by Substituted Cysteine Accessibility Mutagenesis. The Journal of Biological Chemistry 276(45):42035-42042

 

  Wild Type K282C
EC50 1.67 +/- 0.09 1.46 +/- 0.12
Hill Coefficient 2.0 +/- 0.1 2.2 +/- 0.2
Mg Inhibition (before MTSET) -41 +/- 3 -32 +/- 5
Mg Inhibition (after MTSET) -39 +/- 3 -29 +/- 5
Deactivation T50 ratio 0.95 +/- 0.03 1.02 +/- 0.04

 

Panicker S, Cruz H, Arrabit C, Slesinger PA (2002) Evidence for a Centrally Located Gate in the Pore of a Serotonin-Gated Ion Channel. The Journal of Neuroscience 22(5): 1629-1639

 

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