Conopeptide rho-TIA

Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs[1].

O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CSSC[C@@](NC([C@@H](NC1=O)C)=O)([H])C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H]2CC3=CN=CN3)=O)CC(N)=O)=O)CCCNC(N)=N)=O)CCCNC(N)=N)=O)C(N[C@](CSSC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC2=O)CCCCN)=O)CCCCN)=O)CC4=CC=CC=C4)=O)C(N)=O)([H])C(N[C@H](C(N[C@@](C(N5[C@@]1([H])CCC5)=O)([H])[C@@H](C)CC)=O)CC(C)C)=O)=O)=O)[C@@H](NC([C@H](CC(N)=O)NC([C@@H](N)CC6=CC=CC=C6)=O)=O)CC7=CNC8=CC=CC=C78

[1]Chen Z, et al. Subtype-selective noncompetitive or competitive inhibition of human alpha1-adrenergic receptors by rho-TIA. J Biol Chem. 2004 Aug 20;279(34):35326-33. |[2]Sharpe IA, et al. Allosteric alpha 1-adrenoreceptor antagonism by the conopeptide rho-TIA. J Biol Chem. 2003 Sep 5;278(36):34451-7.