The purpose of this site is to give a brief overview of some biochemical properties of dendrotoxin and a few elements from the biological and chemical research; it aims to stimulate interest and pass on a couple of the intriguing hints from the literature. Please see the sources for more topic expertise and feel free to email me with any questions.
Reptile || Molecule || Bibliography Source of molecular
images: Protein Data Bank
(http://www.rcsb.org/pdb/), Berman,
Westbrook, Feng, Gilliland,
Bhat, Weissig, Shindyalov,
Bourne:
The Protein Data Bank. Nucleic Acids Research,
accessed April 5-10, 2003
Green mambas secrete a pre-synaptic neurotoxin and proteinase inhibitor, which works by blocking potassium channels in the space between nerve synapses. Similar to the action of several other snake venoms, the a-DTX binds to voltage activated potassium channels and facilitates release of neural transmitters at peripheral and central synapses.4 Cholinergic agonists mainly excite or inhibit the autonomic effector cells (responsive to parasympathetic neurons) and are referred to as "parasympathomimetic" [mimicking the neuronal] agents5.
Research in molecular biology has identified and studied some of the chemical transmitters at the synapse of nerve cells by using pharmacological agents which react with the synaptically released transmitter in an identical way. The scientists seek natural substances with very specific electrochemical action, like the K+ -induced depolarization that causes the release of amino acid transmitters in the synaptic channel.6 Both carriers and electro-chemical channels have been proposed in connection with the transport of substrates across neurological membranes. Many experiments have tried to define or isolate transport substances and mechanisms.7 In another example, polyamine spider toxins are being used to study inhibitory mechanisms of micro-molar voltage, Ca+ activated currents in neurons.8
In 1991, Tadeusz Skarzynski of Blackett Laboratory, Imperial College, London, compared dendrotoxin to bovine pancreatic trypsin inhibitor [two molecules that are similar in their relation to potassium ion channels, though dendrotoxin is smaller.] He had noticed that a-DTX, a smaller molecule than the bovine one, was unable to inhibit trypsin, and his research pointed to different electrostatic interactions with the proteins on the enzyme side chains. Over the last decade or so, chemical researchers have found compound similarities between the protease inhibitors like several snake toxins and the amyloid beta-protein precursor found in Alzheimer's patients.9 Closer study of the (noticeably very specific) binding action of the venom toxins, may eventually offer better understanding of Alzheimer's and other human neurological disorders.
In the effort to solve the structure of the a-DTX molecule, more than 30 partial or complete data sets of crystals soaked in different heavy-atom solutions were examined. Rotation function calculations employed a variety of models and search procedures, and an ideal model was worked out by Hendrickson-Konnert in 1985, using a "restrained least squares" program. The final refined model consisted of 477 protein atoms, five sulphate ions, and 59 water molecules. The molecular weight is 7138. All main-chain atoms could be mapped for electron density with Fourier coefficients, allowing clear interpretation.10