|
|
The acid-sensing ion channel (ASIC) family is involved with pain perception, learning, and memory. In addition, the ion channels may contribute to brain injury and neuronal death. ASICs are stimulated by H+ ligand and their activation is calcium dependent [1,2]. Peptide toxins have been invaluable tools for inhibition of ion conductance pathways and in functional/structural studies of channels. Psalmotoxin 1 (PTX-4435-s), isolated from the venom of tarantula Psalmopoeus cambridgei, is the first potent peptide blocker shown to inhibit ASIC1a by increasing affinity of the channel for H+, leading to receptor desensitization [4,5,6]. This toxin showed promise as a neuroprotective agent for ASIC1a mediated ischemic brain injury (100 ng/ml) and could selectively inhibit malignant glioma (IC50 = 36 pM) Na+ channels (both inward and outward) [7,8]. Further studies of Psalmotoxin ASIC1a interaction could lead to potential diagnosis and therapy of these and other ASIC1a-related diseases. |
|
||||||||||||
|
1. E.L. Bässler, T.J. Ngo-Anh, H.S. Geisler, J.P.
Ruppersberg, and S.Gründer, J. Biol. Chem., 276, 33782 (2001). |
||||||||||||
Please contact our technical sales specialists to discuss your project needs and for custom inquiries. |
||||||||||||
Please contact Peptides International for ordering information. |
||||||||||||
|
||||||||||||