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Analogs of the lignan pinoresinol as novel lead compounds for P-glycoprotein (P-gp) inhibitorsLaiolo, Jeronimo ...To find novel P-gp-inhibitors, a library of pregnane X receptor (PXR) ligands and the ZINC DrugsNow library were superimposed on the P-gp inhibitor (+)-pinoresinol (1) used as a query for a 3D ... similarity search. After determining the TanimotoCombo index of similarity with 1, eight compounds from the PXR library and two ZINC compounds were selected for biological evaluation. The P-gp inhibition study showed that compounds 7, 8 and 9 successfully increased intracellular doxorubicin (DOX) accumulation in the P-gp overexpressed Lucena 1 cells from 25, 12.5 and 6.25 %M, respectively. Among a series of analogs of 9, compounds 26-30 were shown to be active, with 26 and 27 causing a significant increase in DOX accumulation from 1.56 %M and rendering Lucena 1 sensitive to DOX from 1.56 and 0.78 %M, respectively. Molecular modeling studies showed that both compounds bind to the P-gp at transmembrane helices (TMH) 4, 5 and 6, with 27 also showing contacts with TMH 3.Vir: ACS Medicinal Chemistry Letters. - ISSN 1948-5875 (Vol. 9, iss. 12, 2018, str. 1186-1192)Vrsta gradiva - članek, sestavni delLeto - 2018Jezik - angleškiCOBISS.SI-ID - 4642161
Avtor
Laiolo, Jeronimo |
Tomašič, Tihomir |
Vera, D. Mariano A. |
González L., María L |
Lanza A., Priscila |
Gancedo N., Samanta |
Hodnik, Žiga, farmacevt |
Peterlin-Mašič, Lucija |
Kikelj, Danijel |
Carpinella, María Cecilia
Teme
MDR reversing agents |
P-glycoprotein |
pinoresinol |
diethylstilbestrol derivatives |
structure-activity relationship |
molecular docking
Avtor | Laiolo, Jeronimo ... |
Naslov | Analogs of the lignan pinoresinol as novel lead compounds for P-glycoprotein (P-gp) inhibitors |
Datum objave | 2018-11-21 |
COBISS.SI-ID | 4642161 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Ni določeno |
Embargo | Takojšnja javna objava |
Projekti, iz katerih je bila financirana objava
Naziv | Akronim | Številka projekta | Financer |
---|---|---|---|
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
Datoteke, ki spadajo k objavi
Povezava |
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https://pubs.acs.org/doi/10.1021/acsmedchemlett.8b00324 |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Laiolo, Jeronimo | |
Tomašič, Tihomir | 28334 |
Vera, D. Mariano A. | |
González L., María L | |
Lanza A., Priscila | |
Gancedo N., Samanta | |
Hodnik, Žiga, farmacevt | 33052 |
Peterlin-Mašič, Lucija | 19317 |
Kikelj, Danijel | 01463 |
Carpinella, María Cecilia |
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