|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
1
|
|
pubmed:dateCreated |
2005-11-18
|
|
pubmed:abstractText |
The synthesis of novel macrocyclic peptidomimetic inhibitors of the enzyme BACE1 is described. These macrocycles are derived from a hydroxyethylene core structure. Compound 7 was co-crystallized with BACE1 and the X-ray structure of the complex elucidated at 1.6 Angstrom resolution. This molecule inhibits the production of the Abeta peptide in HEK293 cells overexpressing APP751sw.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jan
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
191-5
|
|
pubmed:dateRevised |
2009-11-19
|
|
pubmed:meshHeading |
pubmed-meshheading:16249081-Alzheimer Disease,
pubmed-meshheading:16249081-Amyloid Precursor Protein Secretases,
pubmed-meshheading:16249081-Amyloid beta-Protein Precursor,
pubmed-meshheading:16249081-Animals,
pubmed-meshheading:16249081-Aspartic Acid Endopeptidases,
pubmed-meshheading:16249081-Cell Line,
pubmed-meshheading:16249081-Chemistry, Pharmaceutical,
pubmed-meshheading:16249081-Crystallography, X-Ray,
pubmed-meshheading:16249081-Drug Design,
pubmed-meshheading:16249081-Endopeptidases,
pubmed-meshheading:16249081-Humans,
pubmed-meshheading:16249081-Kinetics,
pubmed-meshheading:16249081-Models, Chemical,
pubmed-meshheading:16249081-Models, Molecular,
pubmed-meshheading:16249081-Protein Conformation,
pubmed-meshheading:16249081-Protein Structure, Tertiary
|
|
pubmed:year |
2006
|
|
pubmed:articleTitle |
Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex.
|
|
pubmed:affiliation |
Lilly S.A., Avenida de la Industria 30, 28108 Alcobendas, Spain. irojo@lilly.com
|
|
pubmed:publicationType |
Journal Article
|
