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GPCR Modulator Array Library

Library Code: T-VDAGPCR
 
Although not typically expected as a pathway for venoms, GPCR modulation has been discovered in several snake venoms including muscarinic acetylcholine receptor blockers. Snake venoms are a rich source of GPCR tools such as the three-finger toxin motif that is particularly effective at binding GPCRs. The GPCR Targeted Venom Discovery Array™ libraries contain pure venom fractions from 12, 24, 48 or 96 species optimized for identification of novel tools. Each array contains literature-cited, characterized venoms active in GPCR pathways as positive controls. Other venom fractions making up the library have been specially selected by our drug discovery scientists to maximize novel hit potential.
 
T-VDAGPCR control venoms include:
  • Crotalus atrox (western diamondback rattlesnake) where the bradykinin B2 receptor antagonist has been discovered1
  • Dendroaspis angusticeps (eastern green mamba) where several novel muscarinic receptor antagonists have been discovered2
  • Naja kaouthia (monocled cobra) venom which contains a large abundance of three-finger proteins including antagonizing nicotinic and muscarinic nicotine receptors3
References
  1. Calvete J.J., Fasoli E., Sanz L., Boschetti E., Righetti P.G. (2009). Exploring the venom proteome of the western diamondback rattlesnake, Crotalus atrox, via snake venomics and combinatorial peptide ligand library approaches. J. Proteome Res. 8:3055-3067
  2. Max S.I., Liang J.-S., Potter L.T. (1993). Purification and properties of m1-toxin, a specific antagonist of m1 muscarinic receptors. J. Neurosci. 13:4293-4300
  3. Utkin Y.N., Kukhtina V.V., Kryukova E.V., Chiodini F., Bertrand D., Methfessel C., Tsetlin V.I. (2001). 'Weak toxin' from Naja kaouthia is a nontoxic antagonist of alpha 7 and muscle-type nicotinic acetylcholine receptors. J. Biol. Chem. 276:15810-15815
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