A small-molecule fragment that emulates binding of receptor and broadly neutralizing antibodies to influenza A hemagglutinin
Year: 2018
Type: article
Abstract: Significance Influenza is a contagious and sometimes lethal disease of the human respiratory tract. Current preventative measures include annual vaccination and a limited number of antiviral drugs. However, the effectiveness of the seasonal vaccine is unpredictable, and resistance has been developing to all approved drugs. Therefore, novel influenza therapeutics with new targets and mechanisms are essential to protect against future pandemics, epidemics, and seasonal flu. Here, we report on the serendipitous discovery of a noncarbohydrate-based small-molecule N -cyclohexyltaurine that binds to the receptor-binding site of influenza virus hemagglutinin. Our structural findings provide much needed insights on how to effectively and specifically target the hemagglutinin receptor-binding site with small-molecule ligands, a goal which has evaded researchers for many years.
Authors: Rameshwar U. Kadam, Ian A. Wilson
Institution: Scripps Research Institute
Language: English
Subfield: Epidemiology
Field: Medicine
Domain: Health Sciences
Open Access status: green
Funders: National Science Foundation, U.S. Department of Energy, Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung, National Institutes of Health, Office of Science, National Cancer Institute, National Institute of General Medical Sciences, National Institute of Allergy and Infectious Diseases, Basic Energy Sciences, Argonne National Laboratory
Awards: G102163711, G107546177, G1286251239, G1313983767, G1384768361, G1664757510, G2219523378, G222407312, G2287611682, G2363639003, G262962599, G3075337988, G3152346458, G3244038948, Exploiting Vulnerability on Influenza Virus, G3351052168, Exploiting sites of vulnerability on influenza viruses, G402281873, G409777406, G426311843, G4385809619, G4866076653, G498139845, G513797252, G5387317844, G5607048534, G6004781752, G6848031779, G6918803902, G7374214904, G7583137537, G7583901999, G7688398576, G969889393, G993149817
OpenAlex ID: W4238816505
