-
Je něco špatně v tomto záznamu ?
Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II
J. Tykvart, J. Schimer, A. Jančařík, J. Bařinková, V. Navrátil, J. Starková, K. Šrámková, J. Konvalinka, P. Majer, P. Šácha,
Jazyk angličtina Země Spojené státy americké
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- glutamátkarboxypeptidasa II antagonisté a inhibitory chemie metabolismus MeSH
- HEK293 buňky účinky léků MeSH
- inhibitory enzymů chemie metabolismus farmakologie MeSH
- konformace proteinů MeSH
- lidé MeSH
- močovina chemie MeSH
- molekulární struktura MeSH
- preklinické hodnocení léčiv metody MeSH
- racionální návrh léčiv MeSH
- techniky syntetické chemie MeSH
- vazebná místa MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
We present here a structure-aided design of inhibitors targeting the active site as well as exosites of glutamate carboxypeptidase II (GCPII), a prostate cancer marker, preparing potent and selective inhibitors that are more than 1000-fold more active toward GCPII than its closest human homologue, glutamate carboxypeptidase III (GCPIII). Additionally, we demonstrate that the prepared inhibitor conjugate can be used for sensitive and selective imaging of GCPII in mammalian cells.
Citace poskytuje Crossref.org
- 000
- 00000naa a2200000 a 4500
- 001
- bmc15031367
- 003
- CZ-PrNML
- 005
- 20151013123159.0
- 007
- ta
- 008
- 151005s2015 xxu f 000 0|eng||
- 009
- AR
- 024 7_
- $a 10.1021/acs.jmedchem.5b00278 $2 doi
- 035 __
- $a (PubMed)25923815
- 040 __
- $a ABA008 $b cze $d ABA008 $e AACR2
- 041 0_
- $a eng
- 044 __
- $a xxu
- 100 1_
- $a Tykvart, Jan $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic. ‡Department of Biochemistry, Faculty of Science, Charles University, Albertov 6, Prague 2, 128 43, Czech Republic.
- 245 10
- $a Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II / $c J. Tykvart, J. Schimer, A. Jančařík, J. Bařinková, V. Navrátil, J. Starková, K. Šrámková, J. Konvalinka, P. Majer, P. Šácha,
- 520 9_
- $a We present here a structure-aided design of inhibitors targeting the active site as well as exosites of glutamate carboxypeptidase II (GCPII), a prostate cancer marker, preparing potent and selective inhibitors that are more than 1000-fold more active toward GCPII than its closest human homologue, glutamate carboxypeptidase III (GCPIII). Additionally, we demonstrate that the prepared inhibitor conjugate can be used for sensitive and selective imaging of GCPII in mammalian cells.
- 650 _2
- $a vazebná místa $7 D001665
- 650 _2
- $a techniky syntetické chemie $7 D060326
- 650 _2
- $a racionální návrh léčiv $7 D015195
- 650 _2
- $a preklinické hodnocení léčiv $x metody $7 D004353
- 650 _2
- $a inhibitory enzymů $x chemie $x metabolismus $x farmakologie $7 D004791
- 650 _2
- $a glutamátkarboxypeptidasa II $x antagonisté a inhibitory $x chemie $x metabolismus $7 D043425
- 650 _2
- $a HEK293 buňky $x účinky léků $7 D057809
- 650 _2
- $a lidé $7 D006801
- 650 _2
- $a molekulární struktura $7 D015394
- 650 _2
- $a konformace proteinů $7 D011487
- 650 _2
- $a vztahy mezi strukturou a aktivitou $7 D013329
- 650 _2
- $a močovina $x chemie $7 D014508
- 655 _2
- $a časopisecké články $7 D016428
- 655 _2
- $a práce podpořená grantem $7 D013485
- 700 1_
- $a Schimer, Jiří $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic. ‡Department of Biochemistry, Faculty of Science, Charles University, Albertov 6, Prague 2, 128 43, Czech Republic.
- 700 1_
- $a Jančařík, Andrej $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic.
- 700 1_
- $a Bařinková, Jitka $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic.
- 700 1_
- $a Navrátil, Václav $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic. ‡Department of Biochemistry, Faculty of Science, Charles University, Albertov 6, Prague 2, 128 43, Czech Republic.
- 700 1_
- $a Starková, Jana $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic.
- 700 1_
- $a Šrámková, Karolína $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic.
- 700 1_
- $a Konvalinka, Jan $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic. ‡Department of Biochemistry, Faculty of Science, Charles University, Albertov 6, Prague 2, 128 43, Czech Republic.
- 700 1_
- $a Majer, Pavel $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic.
- 700 1_
- $a Šácha, Pavel $u †Gilead Sciences and IOCB Research Centre, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, v.v.i., Flemingovo n. 2, Prague 6, 166 10, Czech Republic. ‡Department of Biochemistry, Faculty of Science, Charles University, Albertov 6, Prague 2, 128 43, Czech Republic.
- 773 0_
- $w MED00010049 $t Journal of medicinal chemistry $x 1520-4804 $g Roč. 58, č. 10 (2015), s. 4357-63
- 856 41
- $u https://pubmed.ncbi.nlm.nih.gov/25923815 $y Pubmed
- 910 __
- $a ABA008 $b sig $c sign $y a $z 0
- 990 __
- $a 20151005 $b ABA008
- 991 __
- $a 20151013123349 $b ABA008
- 999 __
- $a ok $b bmc $g 1092243 $s 914493
- BAS __
- $a 3
- BAS __
- $a PreBMC
- BMC __
- $a 2015 $b 58 $c 10 $d 4357-63 $e 20150507 $i 1520-4804 $m Journal of medicinal chemistry $n J Med Chem $x MED00010049
- LZP __
- $a Pubmed-20151005