Structure-based design of ligands and inhibitors targeting glutamate carboxypeptidase II and its homologs
Public support
Provider
Ministry of Education, Youth and Sports
Programme
KONTAKT
Call for proposals
KONTAKT 8 (SMSM2010ME5)
Main participants
—
Contest type
VS - Public tender
Contract ID
2062/2011-320
Alternative language
Project name in Czech
Racionální návrh ligandů a inhibitorů glutamát karboxypeptidasy II a jejích homologů
Annotation in Czech
Vývoj nového aktivitního stanovení využitelného k identifikaci a optimalizaci inhibitorů GCPII a GCPIII. Optimalizace inhibitorů uvedených enzymů s využitím rentgenostrukturní analýzy.
Scientific branches
R&D category
ZV - Basic research
CEP classification - main branch
CE - Biochemistry
CEP - secondary branch
EB - Genetics and molecular biology
CEP - another secondary branch
—
OECD FORD - equivalent branches <br>(according to the <a href="http://www.vyzkum.cz/storage/att/E6EF7938F0E854BAE520AC119FB22E8D/Prevodnik_oboru_Frascati.pdf">converter</a>)
10603 - Genetics and heredity (medical genetics to be 3)<br>10604 - Reproductive biology (medical aspects to be 3)<br>10605 - Developmental biology<br>10608 - Biochemistry and molecular biology<br>10609 - Biochemical research methods<br>30101 - Human genetics
Completed project evaluation
Provider evaluation
V - Vynikající výsledky projektu (s mezinárodním významem atd.)
Project results evaluation
We developed novel assay based on fluorescence polarization used for the high-throughput screening of inhibitors of human glutamate carboxypeptidase II (GCPII). Using the assay we screened a library of 50,000 small molecules and identified novel GCPII-inhibiting compounds. In complementary approaches, we used in silico and structure-assisted methods to identify and evaluate novel GCPII inhibitors.
Solution timeline
Realization period - beginning
May 1, 2010
Realization period - end
Dec 31, 2012
Project status
U - Finished project
Latest support payment
Feb 16, 2012
Data delivery to CEP
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data delivery code
CEP13-MSM-ME-U/01:1
Data delivery date
Jun 28, 2013
Finance
Total approved costs
1,947 thou. CZK
Public financial support
1,947 thou. CZK
Other public sources
0 thou. CZK
Non public and foreign sources
0 thou. CZK