3zkt

SOLUTION STRUCTURE OF THE SOMATOSTATIN SST3 RECEPTOR ANTAGONIST TAU- CONOTOXIN CnVA

spinqualitylabelsall models 3zkt Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3zkt is a 1 chain structure with sequence from Conus consors. Full experimental information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: NH2 Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function CT5A_CONCN Publication Abstract from PubMed Conopeptides are a diverse array of small linear and reticulated peptides that interact with high potency and selectivity with a large diversity of receptors and ion channels. They are used by cone snails for prey capture or defense. Recent advances in venom gland transcriptomic and venom peptidomic/proteomic technologies combined with bioactivity screening approaches lead to the identification of new toxins with original pharmacological profiles. Here, from transcriptomic/proteomic analyses of the Conus consors cone snail, we identified a new conopeptide called tau-CnVA, which displays the typical cysteine framework V of the T1-conotoxin superfamily. This peptide was chemically synthesized and its three-dimensional structure was solved by NMR analysis and compared to that of TxVA belonging to the same family, revealing very few common structural features apart a common orientation of the intercysteine loop. Because of the lack of a clear biological function associated with the T-conotoxin family, tau-CnVA was screened against more than fifty different ion channels and receptors, highlighting its capacity to interact selectively with the somatostatine sst3 receptor. Pharmacological and functional studies show that tau-CnVA displays a micromolar (Ki of 1.5muM) antagonist property for the sst3 receptor, being currently the only known toxin to interact with this GPCR subfamily. Identification, structural and pharmacological characterization of tau-CnVA, a conopeptide that selectively interacts with somatostatin sst receptor.,Petrel C, Hocking HG, Reynaud M, Upert G, Favreau P, Biass D, Paolini-Bertrand M, Peigneur S, Tytgat J, Gilles N, Hartley O, Boelens R, Stocklin R, Servent D Biochem Pharmacol. 2013 Apr 5. pii: S0006-2952(13)00219-0. doi:, 10.1016/j.bcp.2013.03.019. PMID:23567999 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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