Linked Life Data

17191784

Source:http://linkedlifedata.com/resource/pubmed/id/17191784

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2006-12-28
pubmed:abstractText
TMC-95A, a cyclic tripeptide metabolite of Apiospora montagnei, is a potent competitive inhibitor of proteasome. Based on the X-ray structure of its complex with yeast proteasome, the synthetically challenging structure of this natural product was simplified in a first generation of analogues by replacing the highly oxidized side-chain biaryl system with a phenyl-oxindole group. In the present study, the TMC-95 biaryl group was substituted with a biphenyl ether with retainment of significant proteasome inhibition. Because of the facile synthetic access of tripeptides containing in i, i+2 positions residues of the isodityrosine type, this new generation of TMC-95 analogues may represent promising lead structures for further optimization of affinity and selectivity of proteasome inhibitors.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
1612-1880
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
1
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
161-73
pubmed:meshHeading
pubmed:year
2004
pubmed:articleTitle
TMC-95A analogues with endocyclic biphenyl ether group as proteasome inhibitors.
pubmed:affiliation
Max-Planck-Institut für Biochemie, AG Bioorganische Chemie, Am Klopferspilz 18A, D-82152 Martinsried.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't