 |
PDBsum entry 4wlb
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Transcription
|
PDB id
|
|
|
|
4wlb
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
References listed in PDB file
|
|
|
Key reference
|
|
|
Title
|
|
A reversed sulfonamide series of selective rorc inverse agonists.
|
|
|
Authors
|
|
M.B.Van niel,
B.P.Fauber,
M.Cartwright,
S.Gaines,
J.C.Killen,
O.René,
S.I.Ward,
G.De leon boenig,
Y.Deng,
C.Eidenschenk,
C.Everett,
E.Gancia,
A.Ganguli,
A.Gobbi,
J.Hawkins,
A.R.Johnson,
J.R.Kiefer,
H.La,
P.Lockey,
M.Norman,
W.Ouyang,
A.Qin,
N.Wakes,
B.Waszkowycz,
H.Wong.
|
|
|
Ref.
|
|
Bioorg Med Chem Lett, 2014,
24,
5769-5776.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
The identification of a new series of RORc inverse agonists is described.
Comprehensive structure-activity relationship studies of this reversed
sulfonamide series identified potent RORc inverse agonists in biochemical and
cellular assays which were also selective against a panel of nuclear receptors.
Our work has contributed a compound that may serve as a useful in vitro tool to
delineate the complex biological pathways involved in signalling through RORc.
An X-ray co-crystal structure of an analogue with RORc has also provided useful
insights into the binding interactions of the new series.
|
|
|
|
|
|
|
