-
Je něco špatně v tomto záznamu ?
The "specific" P-glycoprotein inhibitor zosuquidar (LY335979) also weakly inhibits human organic cation transporters
G. Bajraktari-Sylejmani, R. Kamaraj, D. Theile, P. Pávek, J. Weiss
Jazyk angličtina Země Německo
Typ dokumentu časopisecké články
Grantová podpora
Physician Scientist and Olympia Morata
Medical Faculty, University of Heidelberg
SVV 260 663
Charles University, Prague
- MeSH
- chinoliny * farmakologie MeSH
- dibenzocyklohepteny MeSH
- HEK293 buňky MeSH
- lidé MeSH
- P-glykoprotein * antagonisté a inhibitory MeSH
- proteiny přenášející organické kationty * antagonisté a inhibitory metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Zosuquidar (LY335979) is a widely used experimental P-glycoprotein (P-gp) inhibitor, which is commended as very potent but also as very specific for P-gp. In this in vitro and in silico study, we demonstrated for the first time that zosuquidar also inhibits organic cation transporters (OCT) 1-3, albeit less potently than P-gp. This still has to be kept in mind when zosuquidar is used to inhibit cellular efflux of P-gp substrates that are concurrently transported into the cells by OCTs. To avoid interference in these assays, zosuquidar concentrations should be kept below 1 μM.
Citace poskytuje Crossref.org
- 000
- 00000naa a2200000 a 4500
- 001
- bmc25015581
- 003
- CZ-PrNML
- 005
- 20250731091108.0
- 007
- ta
- 008
- 250708s2025 gw f 000 0|eng||
- 009
- AR
- 024 7_
- $a 10.1007/s00210-024-03743-y $2 doi
- 035 __
- $a (PubMed)39718614
- 040 __
- $a ABA008 $b cze $d ABA008 $e AACR2
- 041 0_
- $a eng
- 044 __
- $a gw
- 100 1_
- $a Bajraktari-Sylejmani, Gzona $u Internal Medicine IX - Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University, Medical Faculty Heidelberg, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120, Heidelberg, Germany
- 245 14
- $a The "specific" P-glycoprotein inhibitor zosuquidar (LY335979) also weakly inhibits human organic cation transporters / $c G. Bajraktari-Sylejmani, R. Kamaraj, D. Theile, P. Pávek, J. Weiss
- 520 9_
- $a Zosuquidar (LY335979) is a widely used experimental P-glycoprotein (P-gp) inhibitor, which is commended as very potent but also as very specific for P-gp. In this in vitro and in silico study, we demonstrated for the first time that zosuquidar also inhibits organic cation transporters (OCT) 1-3, albeit less potently than P-gp. This still has to be kept in mind when zosuquidar is used to inhibit cellular efflux of P-gp substrates that are concurrently transported into the cells by OCTs. To avoid interference in these assays, zosuquidar concentrations should be kept below 1 μM.
- 650 _2
- $a lidé $7 D006801
- 650 12
- $a proteiny přenášející organické kationty $x antagonisté a inhibitory $x metabolismus $7 D027701
- 650 12
- $a P-glykoprotein $x antagonisté a inhibitory $7 D020168
- 650 _2
- $a HEK293 buňky $7 D057809
- 650 12
- $a chinoliny $x farmakologie $7 D011804
- 650 _2
- $a dibenzocyklohepteny $7 D003986
- 655 _2
- $a časopisecké články $7 D016428
- 700 1_
- $a Kamaraj, Rajamanikkam $u Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University in Prague, Heyrovskeho 1203, 50005, Hradec Kralove, Czech Republic
- 700 1_
- $a Theile, Dirk $u Internal Medicine IX - Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University, Medical Faculty Heidelberg, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120, Heidelberg, Germany
- 700 1_
- $a Pávek, Petr $u Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University in Prague, Heyrovskeho 1203, 50005, Hradec Kralove, Czech Republic
- 700 1_
- $a Weiss, Johanna $u Internal Medicine IX - Department of Clinical Pharmacology and Pharmacoepidemiology, Heidelberg University, Medical Faculty Heidelberg, Heidelberg University Hospital, Im Neuenheimer Feld 410, 69120, Heidelberg, Germany. johanna.weiss@med.uni-heidelberg.de
- 773 0_
- $w MED00003462 $t Naunyn-Schmiedeberg's archives of pharmacology $x 1432-1912 $g Roč. 398, č. 6 (2025), s. 7147-7153
- 856 41
- $u https://pubmed.ncbi.nlm.nih.gov/39718614 $y Pubmed
- 910 __
- $a ABA008 $b sig $c sign $y - $z 0
- 990 __
- $a 20250708 $b ABA008
- 991 __
- $a 20250731091103 $b ABA008
- 999 __
- $a ok $b bmc $g 2366436 $s 1252706
- BAS __
- $a 3
- BAS __
- $a PreBMC-MEDLINE
- BMC __
- $a 2025 $b 398 $c 6 $d 7147-7153 $e 20241224 $i 1432-1912 $m Naunyn-Schmiedeberg's archives of pharmacology $n Naunyn Schmiedebergs Arch Pharmacol $x MED00003462
- GRA __
- $a Physician Scientist and Olympia Morata $p Medical Faculty, University of Heidelberg
- GRA __
- $a SVV 260 663 $p Charles University, Prague
- LZP __
- $a Pubmed-20250708
