Benzoxazoles as Transthyretin Amyloid Fibril Inhibitors: Synthesis, Evaluation, and Mechanism of Action Academic Article uri icon

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.

altmetric score

  • 9

author list (cited authors)

  • Razavi, H., Palaninathan, S. K., Powers, E. T., Wiseman, R. L., Purkey, H. E., Mohamedmohaideen, N. N., ... Kelly, J. W.

citation count

  • 154

complete list of authors

  • Razavi, Hossein||Palaninathan, Satheesh K||Powers, Evan T||Wiseman, R Luke||Purkey, Hans E||Mohamedmohaideen, Nilofar N||Deechongkit, Songpon||Chiang, Kyle P||Dendle, Maria TA||Sacchettini, James C||Kelly, Jeffery W

publication date

  • June 2003

publisher