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| Fältnamn | Indikatorer | Metadata |
|---|---|---|
| 000 | 04896naa a2200541 4500 | |
| 001 | oai:DiVA.org:uu-485595 | |
| 003 | SwePub | |
| 008 | 220926s2022 | |||||||||||000 ||eng| | |
| 009 | oai:gup.ub.gu.se/313630 | |
| 024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-4855952 URI |
| 024 | 7 | a https://doi.org/10.1007/s11095-022-03171-82 DOI |
| 024 | 7 | a https://gup.ub.gu.se/publication/3136302 URI |
| 040 | a (SwePub)uud (SwePub)gu | |
| 041 | a engb eng | |
| 042 | 9 SwePub | |
| 072 | 7 | a ref2 swepub-contenttype |
| 072 | 7 | a art2 swepub-publicationtype |
| 100 | 1 | a Chen, Eugene C.u Genentech Inc, Dept Drug Metab & Pharmacokinet, San Francisco, CA 94080 USA4 aut |
| 245 | 1 0 | a High Throughput Screening of a Prescription Drug Library for Inhibitors of Organic Cation Transporter 3, OCT3 |
| 264 | c 2022-01-28 | |
| 264 | 1 | b Springer,c 2022 |
| 338 | a electronic2 rdacarrier | |
| 520 | a Introduction The organic cation transporter 3 (OCT3, SLC22A3) is ubiquitously expressed and interacts with a wide array of compounds including endogenous molecules, environmental toxins and prescription drugs. Understudied as a determinant of pharmacokinetics and pharmacodynamics, OCT3 has the potential to be a major determinant of drug absorption and disposition and to be a target for drug-drug interactions (DDIs).Goal The goal of the current study was to identify prescription drug inhibitors of OCT3.Methods We screened a compound library consisting of 2556 prescription drugs, bioactive molecules, and natural products using a high throughput assay in HEK-293 cells stably expressing OCT3.Results We identified 210 compounds that at 20 mu M inhibit 50% or more of OCT3-mediated uptake of 4-Di-1-ASP (2 mu M). Of these, nine were predicted to inhibit the transporter at clinically relevant unbound plasma concentrations. A Structure-Activity Relationship (SAR) model included molecular descriptors that could discriminate between inhibitors and non-inhibitors of OCT3 and was used to identify additional OCT3 inhibitors. Proteomics of human brain microvessels (BMVs) indicated that OCT3 is the highest expressed OCT in the human blood-brain barrier (BBB).Conclusions This study represents the largest screen to identify prescription drug inhibitors of OCT3. Several are sufficiently potent to inhibit the transporter at therapeutic unbound plasma levels, potentially leading to DDIs or off-target pharmacologic effects. | |
| 650 | 7 | a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmaceutiska vetenskaper0 (SwePub)301012 hsv//swe |
| 650 | 7 | a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmaceutical Sciences0 (SwePub)301012 hsv//eng |
| 650 | 7 | a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Farmakologi och toxikologi0 (SwePub)301022 hsv//swe |
| 650 | 7 | a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Pharmacology and Toxicology0 (SwePub)301022 hsv//eng |
| 653 | a Solute carrier superfamily | |
| 653 | a extraneuronal monoamine transporter | |
| 653 | a EMT | |
| 653 | a EMT | |
| 653 | a extraneuronal monoamine transporter | |
| 653 | a Solute carrier superfamily | |
| 700 | 1 | a Matsson, Pär,d 1978u Gothenburg University,Göteborgs universitet,Institutionen för neurovetenskap och fysiologi, sektionen för farmakologi,Institute of Neuroscience and Physiology, Department of Pharmacology4 aut0 (Swepub:gu)xmatsp |
| 700 | 1 | a Azimi, Minau Univ Calif San Francisco, Dept Bioengn & Therapeut Sci, San Francisco, CA 94143 USA4 aut |
| 700 | 1 | a Zhou, Xujiau Univ Calif San Francisco, Dept Bioengn & Therapeut Sci, San Francisco, CA 94143 USA4 aut |
| 700 | 1 | a Handin, Niklasu Uppsala universitet,Institutionen för farmaci4 aut0 (Swepub:uu)nikha230 |
| 700 | 1 | a Yee, Sook Wahu Univ Calif San Francisco, Dept Bioengn & Therapeut Sci, San Francisco, CA 94143 USA4 aut |
| 700 | 1 | a Artursson, Peru Uppsala universitet,Institutionen för farmaci,Science for Life Laboratory, SciLifeLab4 aut0 (Swepub:uu)perartur |
| 700 | 1 | a Giacomini, Kathleen M.u Univ Calif San Francisco, Dept Bioengn & Therapeut Sci, San Francisco, CA 94143 USA4 aut |
| 710 | 2 | a Genentech Inc, Dept Drug Metab & Pharmacokinet, San Francisco, CA 94080 USAb Institutionen för neurovetenskap och fysiologi, sektionen för farmakologi4 org |
| 773 | 0 | t Pharmaceutical researchd : Springerg 39:7, s. 1599-1613q 39:7<1599-1613x 0724-8741x 1573-904X |
| 856 | 4 | u https://doi.org/10.1007/s11095-022-03171-8y Fulltext |
| 856 | 4 | u https://uu.diva-portal.org/smash/get/diva2:1699061/FULLTEXT01.pdfx primaryx Raw objecty fulltext:print |
| 856 | 4 | u https://link.springer.com/content/pdf/10.1007/s11095-022-03171-8.pdf |
| 856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-485595 |
| 856 | 4 8 | u https://doi.org/10.1007/s11095-022-03171-8 |
| 856 | 4 8 | u https://gup.ub.gu.se/publication/313630 |
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