Benzoxazoles as Transthyretin Amyloid Fibril Inhibitors: Synthesis, Evaluation, and Mechanism of Action
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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.
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