Interaction of spin-labeled inhibitors of the vacuolar H+-ATPase with the trans membrane Vo-sector

Neil Dixon, Tibor Páli, Terence P. Kee, Stephen Ball, Michael A. Harrison, John B.C. Findlay, Jonas Nyman, Kalervo Väänänen, Malcolm E. Finbow

Research output: Contribution to journalArticle

Abstract

The osteoclast variant of the vacuolar H+-ATPase (V-ATPase) is a potential therapeutic target for combating the excessive bone resorption that is involved in osteoporosis. The most potent in a series of synthetic inhibitors based on 5-(5,6-dichloro-2-indolyl)-2-methoxy-2,4-pentadienamide (INDOL0) has demonstrated specificity for the osteoclast enzyme, over other V-ATPases. Interaction of two nitroxide spin-labeled derivatives (INDOL6 and INDOL5) with the V-ATPase is studied here by using the transport-active 16-kDa proteolipid analog of subunit c from the hepatopancreas of Nephrops norvegicus, in conjunction with electron paramagnetic resonance (EPR) spectroscopy.

Original languageEnglish
Pages (from-to)506-514
Number of pages9
JournalBiophysical Journal
Volume94
Issue number2
DOIs
Publication statusPublished - 1 Jan 2008

Keywords

  • osteoporosis
  • biochemistry
  • vacuolar H+-ATPase

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