Benzoxazoles as Transthyretin Amyloid Fibril Inhibitors: Synthesis, Evaluation, and Mechanism of Action | Academic Article individual record
abstract

Benzoxazoles pevent misfolding: Benzoxazole-based inhibitors of transthyretin (TTR) amyloid fibril formation are among the most effective found to date. They stabilize TTR against both acid-mediated misfolding and urea denaturation by raising the activation barrier to tetramer dissociation, the rate-limiting step for amyloid formation. The figure depicts the cocrystal structure of one of the better benzoxazole inhibitors bound to TTR.

author list (cited authors)
Razavi, H., Palaninathan, S. K., Powers, E. T., Wiseman, R. L., Purkey, H. E., Mohamedmohaideen, N. N., ... Kelly, J. W.
publication date
2003
publisher
Wiley Publisher
keywords
  • Inhibitors
  • Structure-activity Relationships
  • Bioorganic Chemistry
  • Aggregation
  • Drug Design
altmetric score

9.0

citation count

137