Assessment of the Drug Interaction Potential of Unconjugated and GalNAc3-Conjugated 2′-MOE-ASOs
Antisense oligonucleotides are metabolized by nucleases and drug interactions with small drug molecules at either the cytochrome P450 (CYP) enzyme or transporter levels have not been observed to date.
Colby S. Shemesh +13 more
doaj +1 more source
Repositioning of Lansoprazole as a Protective Agent Against Cisplatin-Induced Ototoxicity
Cisplatin (CDDP) is a well-known chemotherapeutic drug approved for various cancers. However, CDDP accumulates in the inner ear cochlea via organic cation transporter 2 (OCT2) and causes ototoxicity, which is a major clinical limitation.
Eri Wakai +6 more
doaj +1 more source
Stereoselectivity is well known and very pronounced in drug metabolism and receptor binding. However, much less is known about stereoselectivity in drug membrane transport. Here, we characterized the stereoselective cell uptake of chiral phenylethylamine derivatives by human monoamine transporters (NET, DAT, and SERT) and organic cation transporters ...
Gebauer, Lukas +3 more
openaire +5 more sources
Identification of the Tetraspanin CD9 as an Interaction Partner of Organic Cation Transporters 1 and 2 [PDF]
Organic cation transporters (OCTs) are membrane proteins with relevant physiological (because they accept neurotransmitters as substrate) and pharmacological (because of their interaction with drugs) roles. The human OCTs hOCT1 (SLC22A1/hOCT1) and hOCT2 (SLC22A2/hOCT2) are highly expressed in hepatic (hOCT1) and in renal and neuronal tissue (hOCT2 ...
Snieder, Beatrice +11 more
openaire +2 more sources
Beta-2 Adrenergic Agonists Are Substrates and Inhibitors of Human Organic Cation Transporter 1
Beta-2-adrenergic agonists are first line therapeutics in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Upon inhalation, bronchodilation is achieved after binding to beta(2)-receptors, which are primarily localized on airway ...
Hagos, Yohannes +13 more
core +1 more source
Interaction of Chitosan Derivatives with Organic Cation Transporter 1 and 2
The present study was to investigate the interactions of chitosan derivatives including quaternized chitosan (QC), N‐benzyl‐N,O‐succinyl chitosan (BSCS), N‐naphthyl‐N,O‐succinyl chitosan (NSCS) and N‐octyl‐N,O‐succinyl chitosan (OSCS), with organic cation transporter 1 (OCT1) and OCT2.
Sirima Soodvilai +4 more
openaire +1 more source
Deficiency in the Organic Cation Transporters 1 and 2 (Oct1/Oct2 [Slc22a1/Slc22a2]) in Mice Abolishes Renal Secretion of Organic Cations [PDF]
The polyspecific organic cation transporters 1 and 2 (Oct1 and -2) transport a broad range of substrates, including drugs, toxins, and endogenous compounds. Their strategic localization in the basolateral membrane of epithelial cells in the liver, intestine (Oct1), and kidney (Oct1 and Oct2) suggests that they play an essential role in removing noxious
Johan W, Jonker +3 more
openaire +2 more sources
Supplemental Material, sj-pdf-1-het-10.1177_09603271211047915 for Wedelolactone protects against cisplatin-induced nephrotoxicity in mice via inhibition of organic cation transporter 2 by Guangju Wang, Yajuan Bi, Hui Xiong, Tongwei Bo, Lifeng Han, Lijun ...
Yajuan Bi (9508802) +7 more
core +1 more source
Quercetin declines plasma exposure of metoprolol tartrate in the rat model
The study was undertaken to evaluate the effect of quercetin on the pharmacokinetics of Metoprolol tartrate. A single dose in vivo pharmacokinetic study was carried out in rat models.
Siva R Challa +2 more
doaj +1 more source
Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells
Human hepatoma cells may represent a valuable alternative to the use of human hepatocytes for studying hepatic drug transporters, which is now a regulatory issue during drug development. In the present work, we have characterized hepatic drug transporter
Elodie Jouan +4 more
doaj +1 more source

