Synthetic peptide toxins

Synthetic peptide toxins ideal for studying ion channels

Venoms issued from spiders, snakes, mollusks...  contain potent toxins enabling the characterization of a large number of ion channels. These peptide toxins are very hard to obtain directly from animals and quantities obtained are not enough for providing research labs.

tebu-bio provides synthetic toxins with the ideal tools to study ion channels, which are becoming an important therapeutic target for drug discovery.

Key characteristics

• Broadest selection of highly innovative toxins (not found elsewhere)
• Originate from snakes, spiders, cone snails, scorpions, lizards...
• <70 amino acids
• Peptide sequence and folding guaranteed
• High purity (HPLC)
• Quality control by mass spectrometry
• Custom synthesis and modifications upon request

Ion channels and their targeted venomous toxins

Potential cation channel

• Vanillotoxin 3: selective ligand of TRPV1 channel

Sodium channel

• Protoxin II: selective inhibitor of Nav1.7
• Jingzhaotoxin-III: selective inhibitor of Nav1.5 channels
• Protoxin II-biotin: customized Protoxin II to perform new studies
• Hainantoxin-IV: potent antagonist of tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels (VGSCs)
• Huwentoxin IV: lethal neurotoxin selectively acting on tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels, with an IC50 of 30 nM in rat DRG neurons.
• Huwentoxin I: selective inhibitor of N-type calcium channels, and TTXs channels
• μ-Conotoxin PIIIA: binding inhibitor of site 1 of voltage-gated sodium channels
• GsAF-I: voltage-gated sodium channel blocker
• GsAF-II: voltage-gated sodium channel blocker
• Phrixotoxin-3 (PaurTx3 or Beta-theraphotoxin-Ps1a): VGSC blocker
• Mu-conotoxin GIIIB : blocks Na-1.4 voltage-dependent sodium channels, which are predominantly expressed in muscle

Potassium channel

• Iberiotoxin: selective inhibitor of Maxi-K channel
• Charybdotoxin:  blocker of voltage gated and Ca2+ activated K+ channels
• Leiurotoxin 1: Modulator of SK channels (small conductance Ca2+-activated K+ channels)
• Tamapin: Modulator of small conductance Ca2+-activated K+ channels (SK channels)
• Guangxitoxin 1E: inhibitor of Kv2.1 with an IC50 value of 1 nM and Kv2.2 with an IC50 value of 3 nM.
• ShK: voltage-dependent potassium channels inhibitor
• Margatoxin: Kv1.3 inhibitor
• HsTx1
• Apamin   
• Tertiapin-Q
• ADWX-1: inhibitor of Kv1.3 channel with an IC50 of 1.89 pM
• Phrixotoxin-2 : specifically blocks recombinant Kv4.2 and Kv4.3 potassium channels

Calcium channel

• ω-agatoxin IVA: blocks specifically P/Q-type calcium channel
• ω-conotoxin GVIA:  blocks specifically Cav2.2 channel
• ω-conotoxin MVIIC isolated from the venom of the cone Conus magus
• Protoxin II: inhibits voltage-gated calcium and sodium channel
• SNX482: modulator of the R-type current associated with the class α1E calcium channel (Cav2.3 from the CACNA1E gene)
• Maurocalcine: acting on ryanodine receptors with an affinity in the 10 nM range.
• Huwentoxin I
• ω Conotoxin SO-3
• ω-Conotoxin MVIIA
   

Chloride channel

• GaTx1: CFTR blocker
• GaTx2:  is the most potent peptide inhibitor of ClC-2 chloride channel ever described.
• Chlorotoxin:  binds to Cl- channels (small conductance epithelial chloride channels)

Acetylcholine receptor

• Waglerin 1: selective antagonist of muscle nicotinic acetylcholine receptors
• α-Conotoxin MI: acting on postsynaptic membranes. It binds onto and blocks nicotinic acetylcholine receptors (nAChR).
• α-Conotoxin GI: acting on postsynaptic membranes, which bind to the nicotinic acetylcholine receptor (nAChR).
• α-Conotoxin IMI:  acting on postsynaptic membranes, and inhibitors of nicotinic acetylcholine receptors (nAChR)
• alpha-conotoxin GID: selectively blocks neuronal nicotinic acetylcholine receptors

NMDA

• Conantokin G: selective inhibitor of NR2B sub units of N-methyl-D-aspartate (NMDA) receptor-mediated calcium influx in central nervous system neurons.

ASIC channel

• APETx2: selective blocker of the H(+)-gated sodium channel ASIC3 (ACCN3). The blockage is rapid and reversible
• Psalmotoxin 1 (PcTx1): ASIC1 channel selective blocker

Purinergic

• Purotoxin 1: the only one selective inhibitor of P2X3 receptor channel

Others

• Morphiceptin: the most selective agonist of µ-opoid receptors
• Lys-conopressin G: vasopressin-like peptide.
• GsMTx4: This toxin blocks mechanosensitive ion channels (strech-activated channels SAC).