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001-es BibID:BIBFORM044563
Első szerző:Gurrola-Briones, Georgina
Cím:Structure, function, and chemical synthesis of Vaejovis mexicanus peptide 24 : a novel potent blocker of Kv1.3 potassium channels of human T lymphocytes / Gurrola G. B., Hernandez-Lopez R. A., Rodriguez de la Vega R. C., Varga Z., Batista C. V., Salas-Castillo S. P., Panyi G., del Rio-Portilla Federico, Possani L. D.
Dátum:2012
Megjegyzések:Animal venoms are rich sources of ligands for studying ion channels and other pharmacological targets. Proteomic analyses of the soluble venom from the Mexican scorpion Vaejovis mexicanus smithi showed that it contains more than 200 different components. Among them, a 36-residue peptide with a molecular mass of 3864 Da (named Vm24) was shown to be a potent blocker of Kv1.3 of human lymphocytes (K(d) approximately 3 pM). The three-dimensional solution structure of Vm24 was determined by nuclear magnetic resonance, showing the peptide folds into a distorted cystine-stabilized alpha/beta motif consisting of a single-turn alpha-helix and a three-stranded antiparallel beta-sheet, stabilized by four disulfide bridges. The disulfide pairs are formed between Cys6 and Cys26, Cys12 and Cys31, Cys16 and Cys33, and Cys21 and Cys36. Sequence analyses identified Vm24 as the first example of a new subfamily of alpha-type K(+) channel blockers (systematic number alpha-KTx 23.1). Comparison with other Kv1.3 blockers isolated from scorpions suggests a number of structural features that could explain the remarkable affinity and specificity of Vm24 toward Kv1.3 channels of lymphocytes
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Amino Acid Motifs
Animal
Animals
antagonists & inhibitors
article
chemical synthesis
chemistry
Disulfides
drug effects
Drug Evaluation,Preclinical
Human
Humans
Ion Channels
Kv1.3 Potassium Channel
ligand
Ligands
lymphocyte
Lymphocytes
Magnetic Resonance Spectroscopy
methods
Mexico
Mice
Models,Molecular
Peptides
pharmacology
Phylogeny
Potassium
Potassium Channel Blockers
Potassium Channels
Protein Conformation
Research
Research Support
Scorpion Venoms
Scorpions
Support
t lymphocyte
T-Lymphocytes
Megjelenés:Biochemistry 51 : 19 (2012), p. 4049-4061. -
További szerzők:Hernandez-Lopez, Rogelio A. Rodriguez de la Vega, Ricardo C. Varga Zoltán (1969-) (biofizikus, szakfordító) Batista, Cesar V. F. Salas-Castillo, Saida P. Panyi György (1966-) (biofizikus) del Rio-Portilla, Federico Possani, Lourival Domingos
Internet cím:DOI
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