 |
PDBsum entry 6i2x
|
|
|
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
 |
|
|
|
|
|
|
|
|
|
|
Immune system
|
PDB id
|
|
|
|
6i2x
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
Contents |
 |
|
|
|
|
|
|
|
|
|
648 a.a.
|
 |
|
|
|
|
|
|
|
815 a.a.
|
 |
|
|
|
|
|
|
|
951 a.a.
|
 |
|
|
|
|
|
|
|
|
|
|
|
References listed in PDB file
|
 |
|
Key reference
|
 |
|
Title
|
 |
A small-Molecule inhibitor of c5 complement protein.
|
 |
|
Authors
|
 |
K.Jendza,
M.Kato,
M.Salcius,
H.Srinivas,
A.De erkenez,
A.Nguyen,
D.Mclaughlin,
C.Be,
C.Wiesmann,
J.Murphy,
P.Bolduc,
M.Mogi,
J.Duca,
A.Namil,
M.Capparelli,
V.Darsigny,
E.Meredith,
R.Tichkule,
L.Ferrara,
J.Heyder,
F.Liu,
P.A.Horton,
M.J.Romanowski,
M.Schirle,
N.Mainolfi,
K.Anderson,
G.A.Michaud.
|
 |
|
Ref.
|
 |
Nat Chem Biol, 2019,
15,
666-668.
[DOI no: ]
|
 |
|
PubMed id
|
 |
|
 |
 |
|
Abstract
|
 |
|
The complement pathway is an important part of the immune system, and
uncontrolled activation is implicated in many diseases. The human complement
component 5 protein (C5) is a validated drug target within the complement
pathway, as an anti-C5 antibody (Soliris) is an approved therapy for paroxysmal
nocturnal hemoglobinuria. Here, we report the identification, optimization and
mechanism of action for the first small-molecule inhibitor of C5 complement
protein.
|
 |
|
|
|
|
 |