Synthesis and functional studies of THF-gramicidin hybrid ion channels.

نویسندگان

  • Andrea Vescovi
  • Andrea Knoll
  • Ulrich Koert
چکیده

THF-gramicidin hybrids 2-4 with the L-THF amino acid 1 in positions 11 and 12 and compounds 5-8 with the D-THF amino acid ent-1 in positions 10 and 11 were synthesized and their ion channel properties were studied by single-channel-current analysis. The replacement of positions 11 and 12 by the L-THF amino acid 1 gave a strongly reduced channel performance. In contrast, replacement of positions 10 and 11 by the D-THF amino acid ent-1 gave rise to new and interesting channel properties. For the permeability ratios, the ion selectivity shifts from Eisenman I towards Eisenman III selectivity and the channels display ms-dynamics. Most remarkable is the asymmetric compound 8, which inserts selectively into a DPhPC membrane and displays voltage-directed gating dynamics.

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عنوان ژورنال:
  • Organic & biomolecular chemistry

دوره 1 16  شماره 

صفحات  -

تاریخ انتشار 2003