 |
PDBsum entry 3h0c
|
|
|
|
References listed in PDB file
|
 |
|
Key reference
|
|
|
Title
|
|
Discovery of beta-Homophenylalanine based pyrrolidin-2-Ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase iv.
|
|
|
Authors
|
|
S.Nordhoff,
S.Cerezo-Gálvez,
H.Deppe,
O.Hill,
M.López-Canet,
C.Rummey,
M.Thiemann,
V.G.Matassa,
P.J.Edwards,
A.Feurer.
|
|
|
Ref.
|
|
Bioorg Med Chem Lett, 2009,
19,
4201-4203.
|
|
|
PubMed id
|
|
|
|
|
Note In the PDB file this reference is
annotated as "TO BE PUBLISHED".
The citation details given above were identified by an automated
search of PubMed on title and author
names, giving a
percentage match of
97%.
|
|
|
|
Abstract
|
|
|
Modifications of DPP-4 inhibitor 5, that was discovered by structure based
design, are described and structure-activity relationships discussed. With
analogue 7k one of the most potent non-covalent inhibitors of DPP-4 reported to
date (IC(50)=0.38nM) was discovered. X-ray structure of inhibitor 7k bound to
DPP-4 revealed a hydrogen bonding interaction with Q553. First successful
efforts in balancing overall properties, as demonstrated by improved metabolic
stability, highlight the potential of this series.
|
|
|
|
|
|
|
