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PMID: 15951187 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Synthetic multifunctional pores that open and close in response to chemical stimulation.

Bioorganic & medicinal chemistry ·Vol. 13 ·No. 17 ·2005-09-01 ·Pages 5171-80

Gorteau V, Bollot G, Mareda J, Pasini D, Tran DH, Lazar AN, Coleman AW, Sakai N, Matile S

Abstract

Studies on synthetic multifunctional pores with external and internal active sites for ligand gating and noncompetitive blockage are presented, with emphasis on the contribution of external ligands to the characteristics of pore. A comparison between different synthetic multifunctional pores reveals that the location of functional groups in rigid-rod beta-barrel pores is precisely reflected in the function: molecular recognition at the outer barrel surface results in pore opening, while molecular recognition at the inner barrel surface results in pore closing. Negligible nonspecific leakage, disappearance of pH gating, inhibition of intervesicular pore transfer, and maybe also the flickering of currents of single open pores characterize external ligands as adhesive cushions that liberate the pore from lateral pressure exerted by the surrounding membrane. Refined molecular models show good agreement with pore design and experimental facts with regard to function.

MeSH Terms
Hydrogen-Ion Concentration Ligands Models, Molecular Phosphatidylcholines/chemistry
Chemicals
Ligands Phosphatidylcholines
Authors & Affiliations
9 authors, click to expand affiliations / ORCID
Gorteau Virginie
Department of Organic Chemistry, University of Geneva, Geneva, Switzerland.
Bollot Guillaume
Mareda Jiri
Pasini Dario
Tran Duy-Hien
Lazar Adina N
Coleman Anthony W
Sakai Naomi
Matile Stefan
Article Info
Journal
Bioorganic & medicinal chemistry
Abbr.
Bioorg Med Chem
ISSN
0968-0896
Published
2005-09-01
Pages
5171-80
Language
English
Region
England
NLM ID
9413298
Subset
IM
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