TY - JOUR
T1 - Discovery and Structure-Activity Relationships of the Neoseptins
T2 - A New Class of Toll-like Receptor-4 (TLR4) Agonists
AU - Morin, Matthew D.
AU - Wang, Ying
AU - Jones, Brian T.
AU - Su, Lijing
AU - Surakattula, Murali M.R.P.
AU - Berger, Michael
AU - Huang, Hua
AU - Beutler, Elliot K.
AU - Zhang, Hong
AU - Beutler, Bruce
AU - Boger, Dale L.
N1 - Publisher Copyright: © 2016 American Chemical Society.
PY - 2016/5/26
Y1 - 2016/5/26
N2 - Herein, we report studies leading to the discovery of the neoseptins and a comprehensive examination of the structure-activity relationships (SARs) of this new class of small-molecule mouse Toll-like receptor 4 (mTLR4) agonists. The compounds in this class, which emerged from screening an α-helix mimetic library, stimulate the immune response, act by a well-defined mechanism (mouse TLR4 agonist), are easy to produce and structurally manipulate, exhibit exquisite SARs, are nontoxic, and elicit improved and qualitatively different responses compared to lipopolysaccharide, even though they share the same receptor.
AB - Herein, we report studies leading to the discovery of the neoseptins and a comprehensive examination of the structure-activity relationships (SARs) of this new class of small-molecule mouse Toll-like receptor 4 (mTLR4) agonists. The compounds in this class, which emerged from screening an α-helix mimetic library, stimulate the immune response, act by a well-defined mechanism (mouse TLR4 agonist), are easy to produce and structurally manipulate, exhibit exquisite SARs, are nontoxic, and elicit improved and qualitatively different responses compared to lipopolysaccharide, even though they share the same receptor.
UR - http://www.scopus.com/inward/record.url?scp=84971595222&partnerID=8YFLogxK
U2 - https://doi.org/10.1021/acs.jmedchem.6b00177
DO - https://doi.org/10.1021/acs.jmedchem.6b00177
M3 - مقالة
C2 - 27050713
SN - 0022-2623
VL - 59
SP - 4812
EP - 4830
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 10
ER -
