Benzoxazoles as transthyretin amyloid fibril inhibitors: synthesis, evaluation, and mechanism of action. Academic Article

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.

authors

• Sacchettini, James

published proceedings

• Angew Chem Int Ed Engl

altmetric score

• 15

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

• 181

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

• Wiley  Publisher

published in

• Angewandte Chemie International Edition  Journal

keywords

• Amyloid
• Benzoxazoles
• Chromatography, High Pressure Liquid
• Crystallography, X-Ray
• Models, Molecular
• Prealbumin

PubMed Central ID

• 12820260

Digital Object Identifier (DOI)

• 10.1002/anie.200351179

start page

• 2758

end page

• 2761

volume

• 42

issue

• 24