-
Something wrong with this record ?
α1-Adrenoceptor agonist methoxamine inhibits base excision repair via inhibition of apurinic/apyrimidinic endonuclease 1 (APE1)
A. Kohutova, D. Münzova, M. Pešl, V. Rotrekl
Language English Country Poland
Document type Journal Article
NLK
Directory of Open Access Journals
from 2007
Free Medical Journals
from 2003
ProQuest Central
from 2007-03-01
Open Access Digital Library
from 2007-01-01
Open Access Digital Library
from 2007-02-28
Health & Medicine (ProQuest)
from 2007-03-01
Sciendo
from 2007-02-28
ROAD: Directory of Open Access Scholarly Resources
from 1997
- MeSH
- Epinephrine * MeSH
- Receptors, Adrenergic MeSH
- Endonucleases MeSH
- Humans MeSH
- Methoxamine MeSH
- DNA Repair * MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
Methoxamine (Mox) is a well-known α1-adrenoceptor agonist, clinically used as a longer-acting analogue of epinephrine. 1R,2S-Mox (NRL001) has been also undergoing clinical testing to increase the canal resting pressure in patients with bowel incontinence. Here we show, that Mox hydrochloride acts as an inhibitor of base excision repair (BER). The effect is mediated by the inhibition of apurinic/apyrimidinic endonuclease APE1. We link this observation to our previous report showing the biologically relevant effect of Mox on BER - prevention of converting oxidative DNA base damage to double-stranded breaks. We demonstrate that its effect is weaker, but still significant when compared to a known BER inhibitor methoxyamine (MX). We further determined Mox's relative IC50 at 19 mmol L-1, demonstrating a significant effect of Mox on APE1 activity in clinically relevant concentrations.
References provided by Crossref.org
- 000
- 00000naa a2200000 a 4500
- 001
- bmc23011073
- 003
- CZ-PrNML
- 005
- 20230801132809.0
- 007
- ta
- 008
- 230718s2023 pl f 000 0|eng||
- 009
- AR
- 024 7_
- $a 10.2478/acph-2023-0012 $2 doi
- 035 __
- $a (PubMed)37307375
- 040 __
- $a ABA008 $b cze $d ABA008 $e AACR2
- 041 0_
- $a eng
- 044 __
- $a pl
- 100 1_
- $a Kohutova, Aneta $u 1Masaryk University, Faculty of Medicine, Department of Biology 625 00, Brno, Czech Republic
- 245 10
- $a α1-Adrenoceptor agonist methoxamine inhibits base excision repair via inhibition of apurinic/apyrimidinic endonuclease 1 (APE1) / $c A. Kohutova, D. Münzova, M. Pešl, V. Rotrekl
- 520 9_
- $a Methoxamine (Mox) is a well-known α1-adrenoceptor agonist, clinically used as a longer-acting analogue of epinephrine. 1R,2S-Mox (NRL001) has been also undergoing clinical testing to increase the canal resting pressure in patients with bowel incontinence. Here we show, that Mox hydrochloride acts as an inhibitor of base excision repair (BER). The effect is mediated by the inhibition of apurinic/apyrimidinic endonuclease APE1. We link this observation to our previous report showing the biologically relevant effect of Mox on BER - prevention of converting oxidative DNA base damage to double-stranded breaks. We demonstrate that its effect is weaker, but still significant when compared to a known BER inhibitor methoxyamine (MX). We further determined Mox's relative IC50 at 19 mmol L-1, demonstrating a significant effect of Mox on APE1 activity in clinically relevant concentrations.
- 650 _2
- $a lidé $7 D006801
- 650 _2
- $a methoxamin $7 D008729
- 650 12
- $a oprava DNA $7 D004260
- 650 12
- $a adrenalin $7 D004837
- 650 _2
- $a adrenergní receptory $7 D011941
- 650 _2
- $a endonukleasy $7 D004720
- 655 _2
- $a časopisecké články $7 D016428
- 700 1_
- $a Münzova, Dita $u 1Masaryk University, Faculty of Medicine, Department of Biology 625 00, Brno, Czech Republic
- 700 1_
- $a Pešl, Martin $u 1Masaryk University, Faculty of Medicine, Department of Biology 625 00, Brno, Czech Republic $u 2International Clinical Research Center (ICRC), St.Anne's University hospital in Brno, 625 00, Brno, Czech Republic $1 https://orcid.org/0000000187041005 $7 xx0143722
- 700 1_
- $a Rotrekl, Vladimir $u 1Masaryk University, Faculty of Medicine, Department of Biology 625 00, Brno, Czech Republic $u 2International Clinical Research Center (ICRC), St.Anne's University hospital in Brno, 625 00, Brno, Czech Republic $1 https://orcid.org/0000000212980849 $7 jk01102795
- 773 0_
- $w MED00000116 $t Acta pharmaceutica (Zagreb, Croatia) $x 1846-9558 $g Roč. 73, č. 2 (2023), s. 281-291
- 856 41
- $u https://pubmed.ncbi.nlm.nih.gov/37307375 $y Pubmed
- 910 __
- $a ABA008 $b sig $c sign $y p $z 0
- 990 __
- $a 20230718 $b ABA008
- 991 __
- $a 20230801132805 $b ABA008
- 999 __
- $a ok $b bmc $g 1963467 $s 1197338
- BAS __
- $a 3
- BAS __
- $a PreBMC-MEDLINE
- BMC __
- $a 2023 $b 73 $c 2 $d 281-291 $e 20230612 $i 1846-9558 $m Acta pharmaceutica $n Acta Pharm $x MED00000116
- LZP __
- $a Pubmed-20230718
