Vipoxin (T3D2643)
| Record Information | |||||||||||
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| Version | 2.0 | ||||||||||
| Creation Date | 2009-07-06 21:35:49 UTC | ||||||||||
| Update Date | 2014-12-24 20:25:48 UTC | ||||||||||
| Accession Number | T3D2643 | ||||||||||
| Identification | |||||||||||
| Common Name | Vipoxin | ||||||||||
| Class | Protein | ||||||||||
| Description | Vipoxin is a heterodimeric neurotoxin isolated from the venom of the Bulgarian long-nosed viper or Eastern sand viper (Vipera ammodytes meridionalis). This is the most toxic snake in Europe. Vipoxin represents a noncovalent association of two subunits - a basic and toxic phospholipase A2 enzyme, and an acidic non-enzymatic component (vipoxin's acidic component). The function of the acidic component is to stabilize the neurotoxin's quaternary structure, required for its toxic and enzymatic activities, similarly to the role of the acidic component of crotoxin. The venom has both proteolytic and neurotoxic components and contains hemotoxins with blood coagulant properties, similar to and as powerful as in crotalid venom. Other properties include anticoagulant effects, hemoconcentration and hemorrhage. Bites promote symptoms typical of viperid envenomation, such as pain, swelling and discoloration, all of which may be immediate. There are also reports of dizziness and tingling. Humans respond rapidly to this venom, as do mice and birds. Lizards are less affected, while amphibians may even survive a bite. European snakes, such as Coronella and Natrix, are possibly immune. V. ammodytes venom is used in the production of antivenin for the bite of other European vipers and the snake is farmed for this purpose. | ||||||||||
| Compound Type |
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| Protein Structure |  | ||||||||||
| Synonyms |
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| Chemical Formula | Not Available | ||||||||||
| Average Molecular Mass | 13827.665 g/mol | ||||||||||
| CAS Registry Number | Not Available | ||||||||||
| Sequence | Not Available | ||||||||||
| Chemical Taxonomy | |||||||||||
| Description | Not Available | ||||||||||
| Kingdom | Organic Compounds | ||||||||||
| Super Class | Organic Acids | ||||||||||
| Class | Carboxylic Acids and Derivatives | ||||||||||
| Sub Class | Amino Acids, Peptides, and Analogues | ||||||||||
| Direct Parent | Peptides | ||||||||||
| Alternative Parents | Not Available | ||||||||||
| Substituents | Not Available | ||||||||||
| Molecular Framework | Not Available | ||||||||||
| External Descriptors | Not Available | ||||||||||
| Biological Properties | |||||||||||
| Status | Detected and Not Quantified | ||||||||||
| Origin | Exogenous | ||||||||||
| Cellular Locations | Not Available | ||||||||||
| Biofluid Locations | Not Available | ||||||||||
| Tissue Locations | Not Available | ||||||||||
| Pathways | Not Available | ||||||||||
| Applications | Not Available | ||||||||||
| Biological Roles | Not Available | ||||||||||
| Chemical Roles | Not Available | ||||||||||
| Physical Properties | |||||||||||
| State | Liquid | ||||||||||
| Appearance | Clear solution. | ||||||||||
| Experimental Properties |
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| Predicted Properties | Not Available | ||||||||||
| Spectra | |||||||||||
| Spectra |
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| Toxicity Profile | |||||||||||
| Route of Exposure | Injection (sting/bite) (6) | ||||||||||
| Mechanism of Toxicity | Vipoxin inhibits the binding of ligands to biogenic amine receptors including dopamine, serotonin and alpha1/alpha2 adrenergic receptors. Vipoxin also exhibits hemolytic and anticoagulant properties. Vipoxin is composed of two subunits - a basic and toxic phospholipase A2 enzyme and an acidic, non-enzymatic component. The phospholipase A2 (PLA2 activity is responsible for the hemolytic properties. Phospholipases are enzymes that release fatty acids from the second carbon group of glycerol. PLA2 specifically recognizes the sn-2 acyl bond of phospholipids and catalytically hydrolyzes the bond releasing arachidonic acid and lysophospholipids. The vipoxin LPA2 is also a weakly anticoagulant enzyme. (1) | ||||||||||
| Metabolism | Free toxin may be removed by opsonization via the reticuloendothelial system (primarily the liver and kidneys) or it may be degraded through cellular internalization via the lysosomes. Lysosomes are membrane-enclosed organelles that contain an array of digestive enzymes, including several proteases. | ||||||||||
| Toxicity Values | LD50: 6.59 mg/kg (Subcutaneous, Mouse) (5) LD50: 0.8 mg/kg (Intravenous, Mouse) (5) LD50: 0.415 mg/kg (Intraperitoneal, Mouse) (5) LD50 of the heterodimer is 0.7-1.2 mg/kg by intraperitoneal injection into mice and 0.9-1.3 mg/kg by intravenous injection into mice. LD50 of the basic component is 10-13 mg/kg by intraperitoneal injection into mice, and 2.2-3.0 mg/kg by intravenous injection into mice, corresponding to 2.4-fold and more than 10-fold the LD50 of the heterodimer, respectively. (2) | ||||||||||
| Lethal Dose | Not Available | ||||||||||
| Carcinogenicity (IARC Classification) | No indication of carcinogenicity to humans (not listed by IARC). | ||||||||||
| Uses/Sources | Vipoxin is a peptide toxin produced by the Eastern sand viper (Vipera ammodytes meridionalis). (4) | ||||||||||
| Minimum Risk Level | Not Available | ||||||||||
| Health Effects | Neurotoxicity, myotoxicity, cardiotoxicity, anticoagulant, convulsant, antiplatelet, hemorrhagic, hemolytic, and edema-inducing effects | ||||||||||
| Symptoms | Bites from snakes in the Viperidae family cause local pain, swelling, edema, skin discoloration, and ecchymosis. (3) | ||||||||||
| Treatment | An antivenom exists for viper venom. (5) | ||||||||||
| Normal Concentrations | |||||||||||
| Not Available | |||||||||||
| Abnormal Concentrations | |||||||||||
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| External Links | |||||||||||
| DrugBank ID | Not Available | ||||||||||
| HMDB ID | Not Available | ||||||||||
| PubChem Compound ID | Not Available | ||||||||||
| ChEMBL ID | Not Available | ||||||||||
| ChemSpider ID | Not Available | ||||||||||
| KEGG ID | Not Available | ||||||||||
| UniProt ID | P14420 | ||||||||||
| OMIM ID | |||||||||||
| ChEBI ID | Not Available | ||||||||||
| BioCyc ID | Not Available | ||||||||||
| CTD ID | Not Available | ||||||||||
| Stitch ID | Not Available | ||||||||||
| PDB ID | 1AOK | ||||||||||
| ACToR ID | Not Available | ||||||||||
| Wikipedia Link | Not Available | ||||||||||
| References | |||||||||||
| Synthesis Reference | Not Available | ||||||||||
| MSDS | Not Available | ||||||||||
| General References |
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| Gene Regulation | |||||||||||
| Up-Regulated Genes | Not Available | ||||||||||
| Down-Regulated Genes | Not Available | ||||||||||
Targets
- General Function:
- Serotonin receptor activity
- Specific Function:
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling inhibits adenylate cyclase activity and activates a phosphatidylinositol-calcium second messenger system that regulates the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of 5-hydroxytryptamine release and in the regulation of dopamine and 5-hydroxytryptamine metabolism. Plays a role in the regulation of dopamine and 5-hydroxytryptamine levels in the brain, and thereby affects neural activity, mood and behavior. Plays a role in the response to anxiogenic stimuli.
- Gene Name:
- HTR1A
- Uniprot ID:
- P08908
- Molecular Weight:
- 46106.335 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances, such as lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Regulates the release of 5-hydroxytryptamine, dopamine and acetylcholine in the brain, and thereby affects neural activity, nociceptive processing, pain perception, mood and behavior. Besides, plays a role in vasoconstriction of cerebral arteries.
- Gene Name:
- HTR1B
- Uniprot ID:
- P28222
- Molecular Weight:
- 43567.535 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for ergot alkaloid derivatives, various anxiolytic and antidepressant drugs and other psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity. Regulates the release of 5-hydroxytryptamine in the brain, and thereby affects neural activity. May also play a role in regulating the release of other neurotransmitters. May play a role in vasoconstriction.
- Gene Name:
- HTR1D
- Uniprot ID:
- P28221
- Molecular Weight:
- 41906.38 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
- Gene Name:
- HTR1F
- Uniprot ID:
- P30939
- Molecular Weight:
- 41708.505 Da
- General Function:
- Virus receptor activity
- Specific Function:
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates phospholipase C and a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and promotes the release of Ca(2+) ions from intracellular stores. Affects neural activity, perception, cognition and mood. Plays a role in the regulation of behavior, including responses to anxiogenic situations and psychoactive substances. Plays a role in intestinal smooth muscle contraction, and may play a role in arterial vasoconstriction.(Microbial infection) Acts as a receptor for human JC polyomavirus/JCPyV.
- Gene Name:
- HTR2A
- Uniprot ID:
- P28223
- Molecular Weight:
- 52602.58 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Plays a role in the regulation of dopamine and 5-hydroxytryptamine release, 5-hydroxytryptamine uptake and in the regulation of extracellular dopamine and 5-hydroxytryptamine levels, and thereby affects neural activity. May play a role in the perception of pain. Plays a role in the regulation of behavior, including impulsive behavior. Required for normal proliferation of embryonic cardiac myocytes and normal heart development. Protects cardiomyocytes against apoptosis. Plays a role in the adaptation of pulmonary arteries to chronic hypoxia. Plays a role in vasoconstriction. Required for normal osteoblast function and proliferation, and for maintaining normal bone density. Required for normal proliferation of the interstitial cells of Cajal in the intestine.
- Gene Name:
- HTR2B
- Uniprot ID:
- P41595
- Molecular Weight:
- 54297.41 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins and mediate activation of alternative signaling pathways. Signaling activates a phosphatidylinositol-calcium second messenger system that modulates the activity of phosphatidylinositol 3-kinase and down-stream signaling cascades and promotes the release of Ca(2+) ions from intracellular stores. Regulates neuronal activity via the activation of short transient receptor potential calcium channels in the brain, and thereby modulates the activation of pro-opiomelacortin neurons and the release of CRH that then regulates the release of corticosterone. Plays a role in the regulation of appetite and eating behavior, responses to anxiogenic stimuli and stress. Plays a role in insulin sensitivity and glucose homeostasis.
- Gene Name:
- HTR2C
- Uniprot ID:
- P28335
- Molecular Weight:
- 51820.705 Da
- General Function:
- Voltage-gated potassium channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3A
- Uniprot ID:
- P46098
- Molecular Weight:
- 55279.835 Da
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3B
- Uniprot ID:
- O95264
- Molecular Weight:
- 50291.3 Da
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3C
- Uniprot ID:
- Q8WXA8
- Molecular Weight:
- 50219.07 Da
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3D
- Uniprot ID:
- Q70Z44
- Molecular Weight:
- 50190.625 Da
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3E
- Uniprot ID:
- A5X5Y0
- Molecular Weight:
- 51437.415 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
- Gene Name:
- HTR4
- Uniprot ID:
- Q13639
- Molecular Weight:
- 43760.975 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins.
- Gene Name:
- HTR5A
- Uniprot ID:
- P47898
- Molecular Weight:
- 40254.69 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through the regulation of CDK5 activity (By similarity). Is an activator of TOR signaling (PubMed:23027611).
- Gene Name:
- HTR6
- Uniprot ID:
- P50406
- Molecular Weight:
- 46953.625 Da
- General Function:
- Serotonin receptor activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
- Gene Name:
- HTR7
- Uniprot ID:
- P34969
- Molecular Weight:
- 53554.43 Da
- General Function:
- Protein heterodimerization activity
- Specific Function:
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
- Gene Name:
- ADRA1A
- Uniprot ID:
- P35348
- Molecular Weight:
- 51486.005 Da
- General Function:
- Protein heterodimerization activity
- Specific Function:
- This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
- Gene Name:
- ADRA1B
- Uniprot ID:
- P35368
- Molecular Weight:
- 56835.375 Da
- General Function:
- Alpha1-adrenergic receptor activity
- Specific Function:
- This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.
- Gene Name:
- ADRA1D
- Uniprot ID:
- P25100
- Molecular Weight:
- 60462.205 Da
- General Function:
- Thioesterase binding
- Specific Function:
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol.
- Gene Name:
- ADRA2A
- Uniprot ID:
- P08913
- Molecular Weight:
- 48956.275 Da
- General Function:
- Epinephrine binding
- Specific Function:
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol.
- Gene Name:
- ADRA2B
- Uniprot ID:
- P18089
- Molecular Weight:
- 49565.8 Da
- General Function:
- Protein homodimerization activity
- Specific Function:
- Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
- Gene Name:
- ADRA2C
- Uniprot ID:
- P18825
- Molecular Weight:
- 49521.585 Da
- General Function:
- G-protein coupled amine receptor activity
- Specific Function:
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name:
- DRD1
- Uniprot ID:
- P21728
- Molecular Weight:
- 49292.765 Da
- General Function:
- G-protein coupled amine receptor activity
- Specific Function:
- Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
- Gene Name:
- DRD5
- Uniprot ID:
- P21918
- Molecular Weight:
- 52950.5 Da
- General Function:
- Potassium channel regulator activity
- Specific Function:
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
- Gene Name:
- DRD2
- Uniprot ID:
- P14416
- Molecular Weight:
- 50618.91 Da
- General Function:
- G-protein coupled amine receptor activity
- Specific Function:
- Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
- Gene Name:
- DRD3
- Uniprot ID:
- P35462
- Molecular Weight:
- 44224.335 Da
- General Function:
- Sh3 domain binding
- Specific Function:
- Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Its activity is mediated by G proteins which inhibit adenylyl cyclase. Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (By similarity).
- Gene Name:
- DRD4
- Uniprot ID:
- P21917
- Molecular Weight:
- 48359.86 Da