The solution structure of the complex between alpha-bungarotoxin (alpha-BTX) and a 13-residue library-derived peptide (MRYYESSLKSYPD) has been solved using two-dimensional proton-NMR spectroscopy. (rcsb.org)
loop_ _audit_author.name _audit_author.pdbx_ordinal 'Harel, M.' 1 'Kasher, R.' 2 'Sussman, J.L.' 3 # _citation.id primary _citation.title ;The Binding Site of Acetylcholine Receptor as Visualized in the X-Ray Structure of a Complex between Alpha-Bungarotoxin and a Mimotope Peptide. (rcsb.org)
Receptors8
In actuality, venom contains several distinct bungarotoxins, each varying in which receptors they act on and how powerful they are. (wikipedia.org)
α-Bungarotoxin irreversibly blocks the binding of acetylcholine (ACh) to postsynaptic nicotinic acetylcholine receptors (nAchR) on both muscle and neurons. (wikipedia.org)
Similarly, κ-bungarotoxin acts to block postsynaptic nAchRs, but its effect is primarily on neuronal receptors rather than muscular nicotinic receptors. (wikipedia.org)
We thus demonstrate that synthetic fluorescent-tagged α-bungarotoxin preserves excellent properties for binding onto muscle nicotinic receptors. (univ-grenoble-alpes.fr)
The monomeric form binds with high affinity to muscular and neuronal alpha-7/CHRNA7 nicotinic acetylcholine receptors (nAChR). (snakevenomdb.org)
This study demonstrates the utility of [3H]-MLA for characterization of alpha7-type nicotinic receptors in mammalian brain, and suggests that it labels a population identical to that defined by [125I]-alpha-bungarotoxin. (ox.ac.uk)
Postsynaptic alpha neurotoxins such as alpha bungarotoxin and cobrotoxin contain about 60 to 70 amino acid residues, and bind to acetylcholine receptors on the motor end-plate. (brainkart.com)
Cobra's alpha bungarotoxin, binds to the acetylcholine receptors and inhibits neural transmis-sion at the neuromuscular junction. (brainkart.com)
NAChR2
TMB-8 is a potent inhibitor (IC50 approximately 400 nM) of agonist-stimulated ion flux mediated by functional human muscle nAChR or ganglionic alpha 3 beta 4-nAChR subtypes expressed by TE671/RD or SH-SY5Y cells. (aspetjournals.org)
TMB-8 is much less potent (IC50 approximately 30-200 microM) as an inhibitor of high-affinity 3H-labeled acetylcholine or 125I-labeled alpha-bungarotoxin binding to human muscle nAChR, ganglionic alpha 3 beta 4-nAChR, or ganglionic alpha 7-nAChR subtypes. (aspetjournals.org)
Toxin6
Glu-5 and Leu-8, which also remarkably contribute to the contact area with the toxin, are present in all the library-derived peptides that bind strongly to alpha-BTX. (rcsb.org)
Although both peptides bind to similar sites on alpha-BTX, the latter adopts an extended conformation when bound to the toxin [Basus, V., Song, G. & Hawrot, E. (1993) Biochemistry 32, 12290-12298], whereas the library peptide is nearly globular and occupies a larger surface area of alpha-BTX binding site. (rcsb.org)
Bungarotoxins are a group of closely related neurotoxic proteins of the three-finger toxin superfamily found in the venom of kraits including Bungarus multicinctus (the many-banded krait). (wikipedia.org)
The four characterized toxins are: α-Bungarotoxin β-Bungarotoxin (not a three-finger toxin) γ-Bungarotoxin (Q9YGJ0) k-Bungarotoxin Research involving bungarotoxins has been significant in improving our understanding of neurotransmission. (wikipedia.org)
α-bungarotoxin is a large, 74 amino acid toxin containing five disulphide bridges, initially identified in the venom of Bungarus multicinctus snake. (univ-grenoble-alpes.fr)
There must be 5 molecules of cobra toxin (red) to block the receptor (blue) as each molecule binds with an individual alpha chain on the acetylcholine receptor. (proteopedia.org)
Receptor4
The structure of the complex may explain the fact that the library-derived peptide binds alpha-BTX with a 15-fold higher affinity than that shown by the acetylcholine receptor peptide (alpha185-196). (rcsb.org)
Next, we determined the efficacy of the fluorescent-tagged α-bungarotoxin to block acetylcholine (ACh)-mediated currents in response to muscle nicotinic receptor activation in TE671 cells. (univ-grenoble-alpes.fr)
Using automated patch-clamp recordings, we demonstrate that fluorescent synthetic α-bungarotoxin has the expected nanomolar affinity for the nicotinic receptor. (univ-grenoble-alpes.fr)
Formulas for weight loss that contain very low calories update your a role for the nicotinic alpha-bungarotoxin receptor in neurite outgrowth in PC12 cells. (mikochico.com)
Subunit2
Presynaptic beta neurotoxins such as beta-bungarotoxin, cobrotoxin, and taipoxin contain about 120-140 amino acid residues, and a phospholipase A subunit, and prevent release of acetylcholine at the neuromuscular junction. (brainkart.com)
DNA analysis revealed that each harbors a single missense mutation in the AChR alpha-subunit gene, alphaF256L. (ox.ac.uk)
Peptide4
The peptide fills an alpha-BTX pocket made of residues located at fingers I and II, as well as at the C-terminal region. (rcsb.org)
These findings are in accord with the previous data in which it had been shown that substitution of these aromatic residues by aliphatic amino acids leads to loss of binding of the modified peptide with alpha-BTX. (rcsb.org)
Chemical synthesis of α-bungarotoxin requires hydrazide-based coupling of three peptide fragments in successive steps. (univ-grenoble-alpes.fr)
The blocking effect of fluorescent α-bungarotoxin could be displaced by incubation with a 20-mer peptide mimicking the α-bungarotoxin binding site. (univ-grenoble-alpes.fr)
Toxins2
Bungarotoxins are toxins found in the venom of snakes and kraits. (wikipedia.org)
Like most large toxins, chemical synthesis of α-bungarotoxin is challenging, explaining why all previous reports use purified or recombinant α-bungarotoxin. (univ-grenoble-alpes.fr)
Autoradiography2
Here we have extended the study to mouse brain, using autoradiography to examine the distribution of [3H]-MLA and [125I]-alpha-bungarotoxin binding sites. (ox.ac.uk)
The distributions of [125I]-alpha-bungarotoxin and [3H]-MLA binding sites were compared by autoradiography, and binding was quantitated in 72 brain regions. (ox.ac.uk)
Presynaptic1
Common Indian krait venom contains both presynaptic beta bungarotoxin and alpha bungarotoxin (Bawaskar & Bawaskar, 2015 ). (springeropen.com)
Brain2
An autoradiographic analysis of [3H]alpha-bungarotoxin distribution in the rat brain after intraventricular injection. (rupress.org)
its pharmacology and distribution in crudely dissected brain regions closely paralleled that of the well-established alpha7-ligand [125I]-alpha-bungarotoxin. (ox.ac.uk)
Patch-clamp1
Functional analysis of mutations was by alpha-bungarotoxin binding studies and by patch clamp analysis of mutant AChR expressed in human embryonic kidney cells. (ox.ac.uk)
Venom1
These symptoms are the result of bungarotoxin presence in the venom. (wikipedia.org)
Beta2
Krait's beta bungarotoxin causes an initial release of acetylcholine, but then damages the nerve terminal and prevents any further release. (brainkart.com)
If viewed from the synaptic cleft, the protein will look like a pseudo-symmetrical rosette shown in the picture below composed of 10 different alpha and 4 different beta subunits. (proteopedia.org)
Found1
Alpha-bisabolol was found to have strong antimicrobial activity against Campylobacter spp. (terpene.info)
Specific2
Specific binding, defined by unlabelled MLA (Ki = 0.69 nM), was completely inhibited by (-)-nicotine (Ki = 1.62 microM), whereas alpha-bungarotoxin inhibited only 85% of specific binding (Ki = 3.5 nM). (ox.ac.uk)
Furthermore, the specific binding of bungarotoxin was not attenuated by bisabolol. (terpene.info)
Presence1
Serial sections labelled with [3H]-MLA in the absence or presence of unlabelled MLA or alpha-bungarotoxin provided no evidence for any alpha-bungarotoxin-resistant binding. (ox.ac.uk)
Effect1
Since CYP2B1 converts AFB1 and CP into mutagenic metabolites, and CYP1A1 activates B[a]P, 2-AA and 2-AF, the study suggest that alpha-bisabolol antimutagenicity could be carried out by an inhibitory effect on the metabolic liver activation of these promutagens. (terpene.info)
Release1
Conversely, β- and γ-bungarotoxins act presynaptically to cause excessive acetylcholine release and subsequent depletion, resulting in paralysis. (wikipedia.org)
Sites1
The results are discussed in terms of binding sites that are inaccessible to alpha-bungarotoxin in membrane preparations. (ox.ac.uk)
Made1
Purified alpha-bungarotoxin was isolated by chromatography and made radioactive with tritium ([3H]acetamidino-alpha-bungarotoxin). (rupress.org)
Shown1
The mutagenic effects of mutagens AFB1, CP, B[a]P, 2-AA and 2-AF were shown to be markedly reduced by alpha-bisabolol. (terpene.info)
Nicotinic19
Alpha-Cbt did not show any blockade of the nicotine-evoked release of DA at the doses studied while alpha-Bgt did block it only at the higher dose (4.2 microM) These results indicate that short neurotoxins show a stronger interaction with striatal nicotinic receptors subtypes controlling DA release when compared to the long ones. (nih.gov)
α-Bungarotoxin irreversibly blocks the binding of acetylcholine (ACh) to postsynaptic nicotinic acetylcholine receptors (nAchR) on both muscle and neurons. (wikipedia.org)
Similarly, κ-bungarotoxin acts to block postsynaptic nAchRs, but its effect is primarily on neuronal receptors rather than muscular nicotinic receptors. (wikipedia.org)
The α7 subunit of the neuronal nicotinic acetylcholine receptor (nAChR) is abundantly expressed in hippocampus and is implicated in modulating neurotransmitter release and in binding α-bungarotoxin (α-BGT). (jneurosci.org)
In the vertebrate brain, two categories of nicotinic receptors are distinguishable based on high-affinity binding of the agonist nicotine or high-affinity binding of the antagonist α-bungarotoxin (α-BGT). (jneurosci.org)
1. Synaptic potentials mediated by alpha 7 nicotinic acetylcholine receptors in supraoptic nucleus. (nih.gov)
9. Fast synaptic transmission mediated by alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in lamina X neurones of neonatal rat spinal cord. (nih.gov)
13. Synaptic potentials mediated via alpha-bungarotoxin-sensitive nicotinic acetylcholine receptors in rat hippocampal interneurons. (nih.gov)
The human neuromedulloblastoma cell line TE671 is shown by single- channel recordings to express nicotinic acetylcholine receptors (AChRs) that are blocked by alpha-bungarotoxin (alpha Bgt). (jneurosci.org)
These AChRs do not react with antisera to the alpha Bgt-binding protein of brain or with monoclonal antibodies (mAbs) to brain nicotinic AChRs that do not bind alpha Bgt. (jneurosci.org)
Antagonists of nicotinic receptors, such as alpha-bungarotoxin or mecamylamine, only partially reversed these neuroprotective effects of nicotine. (nih.gov)
In the past year we have used alpha-bungarotoxin-horseradish peroxidase conjugate to identify the synoptic sites of nicotinic acetylcholine receptors aggregation on cultured skeletal muscle cells by neuroblastoma-glioma hybrid cells and by substances secreted by those cells. (nih.gov)
Human β-amyloid (Aβ) was measured by ELISA, synaptophysin by Western blot and α7 neuronal nicotinic acetylcholine receptors (nAChRs) were analyzed by [(125)I]α-bungarotoxin autoradiography. (nih.gov)
The protein encoded by this gene forms a homo-oligomeric channel, displays marked permeability to calcium ions and is a major component of brain nicotinic receptors that are blocked by, and highly sensitive to, alpha-bungarotoxin. (nih.gov)
Nicotinic receptor subtypes in the developing chick brain: appearance of a species containing the alpha 4, beta 2, and alpha 5 gene products. (yes4yes.com)
Characterisation of the binding of [3H]methyllycaconitine: a new radioligand for labelling alpha 7-type neuronal nicotinic acetylcholine receptors. (ox.ac.uk)
Methyllycaconitine (MLA), a norditerpenoid alkaloid isolated from Delphinium seeds, is one of the most potent non-proteinacious ligands that is selective for alpha bungarotoxin-sensitive neuronal nicotinic acetylcholine receptors (nAChR). (ox.ac.uk)
The radioligand binding displayed nicotinic pharmacology, consistent with an interaction with alpha bungarotoxin-sensitive nAChR. (ox.ac.uk)
In actuality, venom contains several distinct bungarotoxins, each varying in which receptors they act on and how powerful they are. (wikipedia.org)
Summary of the ASPET-sponsored Colloquium: Alpha-2 adrenergic receptors: structure, function, and therapeutic implications, October 25-27, 1995. (aspetjournals.org)
To this purpose histochemical localization of alpha-bungarotoxin bound to the receptors is used in conjunction with light and electron microscopy. (nih.gov)
Phospholipase A III was also shown to compete with α-bungarotoxin for binding to purified acetylcholine receptors, suggesting that these phospholipases block transmission by occupying the acetylcholine-binding site and not by uncoupling or blocking receptor ion channels. (strath.ac.uk)
Bungarus1
Bungarotoxins are a group of closely related neurotoxic proteins of the three-finger toxin superfamily found in the venom of kraits including Bungarus multicinctus (the many-banded krait). (wikipedia.org)
Neurons2
Bungarotoxins function by modulating acetylcholine neurotransmission in both muscles and neurons. (wikipedia.org)
Ravdin, P.M., Nitkin, R.M. and Berg, D.K. (1981) Internalization of alpha-bungarotoxin on neurons induced by a neurotoxin that blocks neuronal acetylcholine sensitivity, J. Neurosci . (nih.gov)
125I6
29.6% (mean value) of the total 125I-alpha-bungarotoxin (alpha-BuTx) binding sites in the TE671 extracts was not inhibited by d-tubocurarine (dTC). (nih.gov)
The receptor protein is detected by receptor autoradiography using 125I alpha-Bungarotoxin, a ligand specific for the alpha7 nAChR (right side). (tamu.edu)
The distribution of [3H]MLA binding sites in crudely dissected rat brain regions was identical to that of [125I] alpha bungarotoxinbinding sites, with a high binding site density in hippocampus and hypothalamus, but low density in striatum and cerebellum. (ox.ac.uk)
Purified receptor preparations had specific activities of 0.5-3.5mumol a bungarotoxin binding sites per gram protein and sedi-mented as a single 125I-alpha bungarotoxin-binding species in sucrose density gradient centrifugation with S20,w =9.5. (bath.ac.uk)
The purified protein focussed as a single sharp band at pH 6.6 when labelled directly with 125I and at pH 5.1 when complexed to 125I-alpha bungarotoxin. (bath.ac.uk)
The purified receptor bound 125I-alpha bungarotoxin and d-tubo-curarine with kD values of 0.5nM and 0.25muM respectively. (bath.ac.uk)
Presynaptically2
Conversely, β- and γ-bungarotoxins act presynaptically to cause excessive acetylcholine release and subsequent depletion, resulting in paralysis. (wikipedia.org)
beta- and gamma-bungarotoxins act presynaptically causing acetylcholine release and depletion. (bvsalud.org)
Nicotine2
The short toxins alpha-Ebt and FAS blocked the extracellular increase of DA evoked by nicotine at 4.2 microM concentrations and alpha-Ebt was more potent, as reflected by the blockade at the lower dose of 0.42 microM. (nih.gov)
The snake alpha-toxins, alpha bungarotoxin and alpha cobratoxin, displaced [3H]MLA with high affinity (Ki = 1.8 +/- 0.5 and 5.5 +/- 0.9 nM, respectively), whereas nicotine was less potent (Ki = 6.1 +/- 1.1 microM). (ox.ac.uk)
Snake1
In particular, the use of alpha-bungarotoxin, a compound derived from snake venom, that bound to specific portions of the acetylcholine receptor (AChR) was pioneered by pharmacologists C. C. Chang, C. Y. Lee, and L. F. Tseng. (naqlafshk.com)
Antibody1
The usual AChR antibody test measures the binding of antibody to AChR labeled with radioactive alpha-bungarotoxin. (medicalnotes.info)
Subunit1
Sequences of cDNAs for the ACh- binding alpha subunit and the delta subunit of this AChR further identify it as muscle AChR. (jneurosci.org)
Protein1
b -Bungarotoxin has been shown to contain several components, the major protein being designated as b 1 - or b -bungarotoxin. (drugfuture.com)
Treatment1
understanding the mechanism by which bungarotoxins work can improve treatment options in such situations. (wikipedia.org)
Classes1
Both event classes were blocked by alpha‐bungarotoxin. (elsevierpure.com)
Type1
3H]MLA, therefore, is a novel radiolabel for characterising alpha 7-type nAChR. (ox.ac.uk)