Linked Life Data

15658862

Source:http://linkedlifedata.com/resource/pubmed/id/15658862

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2005-1-20
pubmed:abstractText
Endothelin-1 (ET-1) is mitogenic and/or antiapoptotic in human cancers, and antagonists to ET-1 receptors are under evaluation for cancer treatment. Inhibition of ET-1 activation by the endothelin-converting enzymes 1(a)(-)(d) (ECE-1(a)(-)(d); EC 3.4.24.71) represents another approach to block the ET-1 effect in cancer. To evaluate this potential, we synthesized and characterized a series of low nanomolar nonpeptidic thiol-containing ECE-1 inhibitors, and evaluated their effect, as well as the effect of inhibitors for the related metalloproteases neprilysin (NEP; EC 3.4.24.11) and angiotensin-converting enzyme (ACE; EC 3.4.15.1), on human glioblastoma cell growth. Only ECE-1 inhibitors inhibited DNA synthesis by human glioblastoma cells. Exogenous addition of ET-1 or bigET-1 to glioblastoma cells did not counterbalance the growth inhibition elicited by ECE-1 inhibitors, suggesting that ECE-1 inhibitors block the proliferation of human glioblastoma cells most likely via a mechanism not involving extracellular production of ET-1. This class of molecules may thus represent novel therapeutic agents for the potential treatment of human cancer.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:day
27
pubmed:volume
48
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
483-98
pubmed:dateRevised
2009-11-19
pubmed:meshHeading
pubmed-meshheading:15658862-Antineoplastic Agents, pubmed-meshheading:15658862-Aspartic Acid Endopeptidases, pubmed-meshheading:15658862-Carbamates, pubmed-meshheading:15658862-Cell Line, Tumor, pubmed-meshheading:15658862-Cell Proliferation, pubmed-meshheading:15658862-Central Nervous System Neoplasms, pubmed-meshheading:15658862-Drug Screening Assays, Antitumor, pubmed-meshheading:15658862-Endothelin-1, pubmed-meshheading:15658862-Glioblastoma, pubmed-meshheading:15658862-Humans, pubmed-meshheading:15658862-Hydrazines, pubmed-meshheading:15658862-Metalloendopeptidases, pubmed-meshheading:15658862-Proline, pubmed-meshheading:15658862-Pyrimidines, pubmed-meshheading:15658862-Pyrrolidines, pubmed-meshheading:15658862-Structure-Activity Relationship, pubmed-meshheading:15658862-Sulfhydryl Compounds
pubmed:year
2005
pubmed:articleTitle
Endothelin-converting enzyme-1 inhibition and growth of human glioblastoma cells.
pubmed:affiliation
University Institute of Pathology, University of Lausanne, Bugnon 25, CH1011 Lausanne, Switzerland.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't