Vm24 Scorpion Toxin: Difference between revisions

Line 10:

Positions <scene name='84/842913/Resi_7-9/1'>7-9</scene> and <scene name='84/842913/Resi_17-20/1'>17-20</scene> are not well defined because they have a reduced number of Nuclear Overhauser effects NOEs [https://pubmed-ncbi-nlm-nih-gov.ezproxy.uvm.edu/22540187/?from_single_result=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.&expanded_search_query=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.] All <scene name='84/842913/All_disulfides/2'>cysteines</scene> and <scene name='84/842913/Ile4/1'>Ile4</scene> are buried entirely, but all other residues are exposed. <scene name='84/842913/Tyr35/1'>Tyr35</scene> and <scene name='84/842913/Cys36/1'>Cys36</scene> are in a very flexible region, which is interesting because they are adjacent to a <scene name='84/842913/Ssbonds_21-36/1'>disulfide bridge</scene>.

==Function==

Vm24 is a potent and selective inhibitor of Kv1.3 potassium channels of human T lymphocytes. In vitro, Kv1.3 current is reduced by approximately 2/3 rds in the presence of 3pM of Vm24

Vm24 is a potent and selective inhibitor of Kv1.3 potassium channels of human T lymphocytes. In vitro, Kv1.3 current is reduced by approximately 2/3 rds in the presence of 3pM of Vm24. The synthetic and natural forms of this protein have nearly identical activity, but the synthetic toxin could be slightly more potent. Kd synthetic =0.5pM and Kd native = 2.9 pM, but this difference is mostly attributed to measurement difficulties at low concentrations [https://pubmed-ncbi-nlm-nih-gov.ezproxy.uvm.edu/22540187/?from_single_result=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.&expanded_search_query=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.]. At a higher concentrations of 100pM, both the synthetic and native peptides reduce Kv1.3 current by 90%.

Vm24 Scorpion Toxin: Difference between revisions

Navigation menu

Page actions

Page actions

Personal tools

Navigation

Search

Tools

@@ Line 10: / Line 10: @@
 Positions <scene name='84/842913/Resi_7-9/1'>7-9</scene> and <scene name='84/842913/Resi_17-20/1'>17-20</scene> are not well defined because they have a reduced number of Nuclear Overhauser effects NOEs [https://pubmed-ncbi-nlm-nih-gov.ezproxy.uvm.edu/22540187/?from_single_result=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.&expanded_search_query=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.] All <scene name='84/842913/All_disulfides/2'>cysteines</scene> and <scene name='84/842913/Ile4/1'>Ile4</scene> are buried entirely, but all other residues are exposed. <scene name='84/842913/Tyr35/1'>Tyr35</scene> and <scene name='84/842913/Cys36/1'>Cys36</scene> are in a very flexible region, which is interesting because they are adjacent to a <scene name='84/842913/Ssbonds_21-36/1'>disulfide bridge</scene>.
 ==Function==
-Vm24 is a potent and selective inhibitor of Kv1.3 potassium channels of human T lymphocytes. In vitro, Kv1.3 current is reduced by approximately 2/3 <sub>rds</sub> in the presence of 3pM of Vm24
+Vm24 is a potent and selective inhibitor of Kv1.3 potassium channels of human T lymphocytes. In vitro, Kv1.3 current is reduced by approximately 2/3 <sub>rds</sub> in the presence of 3pM of Vm24. The synthetic and natural forms of this protein have nearly identical activity, but the synthetic toxin could be slightly more potent. K<sub>d synthetic</sub> =0.5pM and K<sub>d native</sub> = 2.9 pM, but this difference is mostly attributed to measurement difficulties at low concentrations [https://pubmed-ncbi-nlm-nih-gov.ezproxy.uvm.edu/22540187/?from_single_result=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.&expanded_search_query=Structure%2C+function%2C+and+chemical+synthesis+of+Vaejovis+mexicanus+peptide+24%3A+a+novel+potent+blocker+of+Kv1.3+potassium+channels+of+human+T+lymphocytes.]. At a higher concentrations of 100pM, both the synthetic and native peptides reduce Kv1.3 current by 90%.