Linked Life Data

19921722

Source:http://linkedlifedata.com/resource/pubmed/id/19921722

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
2009-12-28
pubmed:abstractText
Substantial evidence over the last decades has implicated uncontrolled angiogenesis with various pathological states, including cancer. Vascular endothelial growth factor (VEGF) plays a critical role in its regulation. Because the tyrosine kinase VEGF receptor-2 (VEGFR-2) is the major mediator of the mitogenic, angiogenic, and permeability-enhancing effects of VEGF, it has become one of the most profound anti-angiogenesis targets. Inspired by the anthranilamide class of VEGFR-2 inhibitors, we performed a computational analysis of some potent representative members, using docking and molecular dynamics calculations. Based on the observations drawn from introducing the effect of the receptor's flexibility in implicit aqueous environment, we designed, synthesized, and characterized several new analogues of related scaffolds with modifications in their steric and electronic characteristics. In vitro evaluation of these compounds revealed several novel VEGFR-2 inhibitors that are less cytotoxic and more potent than the parent compounds.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
1860-7187
pubmed:author
pubmed:issnType
Electronic
pubmed:volume
5
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
118-29
pubmed:meshHeading
pubmed:year
2010
pubmed:articleTitle
Discovery of potent vascular endothelial growth factor receptor-2 inhibitors.
pubmed:affiliation
Laboratory of Chemical Biology of Natural Products and Designed Molecules, Institute of Physical Chemistry, NCSR "Demokritos", 15310 Ag. Paraskevi Attikis, Athens, Greece.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't