Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Pivot Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Target Concepts:
Gene/Protein
Disease
Symptom
Drug
Enzyme
Compound
Query: EC:3.4.23.5 (
cathepsin D
)
4,130
document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)
An effective approach for enhancing the selectivity of
beta-site amyloid precursor protein cleaving enzyme
(BACE 1) inhibitors is developed based on the unique features of the S1' pocket of the enzyme. A series of low molecular weight (<600) compounds were synthesized with different moieties at the P1' position. The selectivity of BACE 1 inhibitors versus
cathepsin D
and renin was enhanced 120-fold by replacing the hydrophobic propyl group with a hydrophilic propionic acid group.
...
PMID:Rational design and synthesis of selective BACE-1 inhibitors. 1474 Dec 51
Structure-based design, synthesis, and X-ray structure of protein-ligand complexes of
memapsin 2
are described. The inhibitors are designed specifically to interact with S2- and S3-active site residues to provide selectivity over memapsin 1 and
cathepsin D
. Inhibitor 6 has exhibited exceedingly potent inhibitory activity against
memapsin 2
and selectivity over memapsin 1 (>3800-fold) and
cathepsin D
(>2500-fold). A protein-ligand crystal structure revealed cooperative interactions in the S2- and S3-active sites of
memapsin 2
. These interactions may serve as an important guide to design selectivity over memapsin 1 and
cathepsin D
.
...
PMID:Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors. 1662 80
