 |
PDBsum entry 4jqh
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Signaling protein
|
PDB id
|
|
|
|
4jqh
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
References listed in PDB file
|
|
|
Key reference
|
|
|
Title
|
|
Insights into soluble guanylyl cyclase activation derived from improved heme-Mimetics.
|
|
|
Authors
|
|
M.Von wantoch rekowski,
V.Kumar,
Z.Zhou,
J.Moschner,
A.Marazioti,
M.Bantzi,
G.A.Spyroulias,
F.Van den akker,
A.Giannis,
A.Papapetropoulos.
|
|
|
Ref.
|
|
J Med Chem, 2013,
56,
8948-8952.
[DOI no: ]
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
Recently, the structure of BAY 58-2667 bound to the Nostoc sp. H-NOX domain was
published. On the basis of this structural information, we designed BAY 58-2667
derivatives and tested their effects on soluble guanylyl cyclase (sGC) activity.
Derivative 20 activated sGC 4.8-fold more than BAY 58-2667. Co-crystallization
of 20 with the Ns H-NOX domain revealed that the increased conformational
distortion at the C-terminal region of αF helix containing 110-114 residues
contributes to the higher activation triggered by 20.
|
|
|
|
|
|
|
