Peptide Information

General Information of This Peptide
Peptide ID
BTDP008554
Peptide Name
Tertiapin
Symonym
TPN
Species
Apis mellifera (Honeybee)
Uniprot Name
TERT_APIME
Alphafold ID
P56587
3D Structure
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2D Sequence
3D Structure
Source
RSCB PDB: 1TER
Sequence
ALCNCNRIIIPHMCWKKCGKK
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Sequence Length
21
Mass (Da)
2460
Sequence Removed Signal Peptide
ALCNCNRIIIPHMCWKKCGKK
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Disulfide Bond
3-14;5-18
PDB ID
1TER
        Click to Show/Hide the Complete Species Lineage
Kingdom: Metazoa
Phylum: Arthropoda
Class: Insecta
Order: Hymenoptera
Family: Apidae
Genus: Apis
Species: Apis mellifera
Full List of Activity Data of This Peptide Toxin
                        Target Name Activity Data Type Activity Data Concentration Note Reference
 Target Info    Kir1.1 Dissociation constant
2 nM
 . . [1- 11]
 Target Info    Kir3.1/3.4 Dissociation constant
8.6 nM
 . . [1- 11]
 Target Info    Kir2.1 Inhibition rate .
2 μM
 . [1- 11]
References
Ref 1 A novel high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry. 1998 Sep 22;37(38):13291-9. doi: 10.1021/bi981178p.
Ref 2 [Interaction of tertiapin, a neurotoxin from bee venom, with calmodulin]. Bioorg Khim. 1983 Jan;9(1):26-32.
Ref 3 Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry. 1999 Oct 26;38(43):14286-93. doi: 10.1021/bi991205r.
Ref 4 Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. Biochemistry. 1999 Oct 26;38(43):14294-301. doi: 10.1021/bi991206j.
Ref 5 The bee venom peptide tertiapin underlines the role of I(KACh) in acetylcholine-induced atrioventricular blocks. Br J Pharmacol. 2000 Oct;131(3):569-77. doi: 10.1038/sj.bjp.0703611.
Ref 6 Tertiapin potently and selectively blocks muscarinic K(+) channels in rabbit cardiac myocytes. J Pharmacol Exp Ther. 2000 Apr;293(1):196-205.
Ref 7 Titration of tertiapin-Q inhibition of ROMK1 channels by extracellular protons. Biochemistry. 2001 Mar 27;40(12):3601-5. doi: 10.1021/bi002584n.
Ref 8 Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner. J Pharmacol Exp Ther. 2005 Sep;314(3):1353-61. doi: 10.1124/jpet.105.085928. Epub 2005 Jun 9.
Ref 9 Tertiapin, a selective IKACh blocker, terminates atrial fibrillation with selective atrial effective refractory period prolongation. Pharmacol Res. 2006 Aug;54(2):136-41. doi: 10.1016/j.phrs.2006.03.021. Epub 2006 Apr 1.
Ref 10 Characterization of Kir1.1 channels with the use of a radiolabeled derivative of tertiapin. Biochemistry. 2006 Aug 22;45(33):10129-39. doi: 10.1021/bi060509s.
Ref 11 Solution structure of tertiapin determined using nuclear magnetic resonance and distance geometry. Proteins. 1993 Oct;17(2):124-37. doi: 10.1002/prot.340170203.
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