2NZZ

NMR structure analysis of the Penetratin conjugated Gas (374-394) peptide

2NZZ の概要

• エントリーDOI: 10.2210/pdb2nzz/pdb
• 関連するPDBエントリー: 2O00
• 分子名称: Penetratin conjugated Gas (374-394) peptide (1 entity in total)
• 機能のキーワード: conformational analysis, g protein, gas subunit, a2a adenosine receptor, cell-penetrating peptides, penetratin, membrane protein
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 4927.89

構造登録者

D'Ursi, A.M.,Rovero, P.,Albrizio, S.,Espsito, C.,D'Errico, G.,Novellino, E. (登録日: 2006-11-27, 公開日: 2007-06-05, 最終更新日: 2023-12-27)

主引用文献

Albrizio, S.,Giusti, L.,D'Errico, G.,Esposito, C.,Porchia, F.,Caliendo, G.,Novellino, E.,Mazzoni, M.R.,Rovero, P.,D'Ursi, A.M.
Driving forces in the delivery of penetratin conjugated G protein fragment.
J.Med.Chem., 50:1458-1464, 2007

PubMed Abstract: A42 is a chimera peptide consisting of Galphas(374-394)C379A--the 21-mer C terminus of the Galphas protein, able of adenosine inhibitory activity--and penetratin--the 16 residue fragment, derived from the homeodomain of the Drosophila transcription factor Antennapedia. A42 is able to cross cell membranes and to inhibit A2A and A2B adenosine and beta-adrenergic receptor stimulated camps (D'Ursi et al. Mol. Pharmacol. 2006, 69, 727-36). Here we present an extensive biophysical study of A42 in different membrane mimetics, with the objective to evaluate the molecular mechanisms which promote the membrane permeation. Fluorescence, CD, and NMR data were acquired in the presence of negatively charged and zwitterionic sodium dodecyl sulfate and dodecylphosphocholine surfactants. To validate the spectroscopic results in a larger scale, fluorescence microscopy experiments were performed on negatively charged and zwitterionic dipalmitoylphosphatidylglycerol and dipalmitoylphosphatidylcholine vesicles. Our results show that the internalization of A42 is mainly driven by electrostatic interactions, hydrophobic interactions playing only a secondary, sinergistic role. The distribution of the charges along the molecule has an important role, highlighting that internalization is a process which requires a specific matching of peptide and membrane properties.

PubMed: 17348636
DOI: 10.1021/jm060935b

実験手法

SOLUTION NMR