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Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity in vitro and in vivo [Elektronski vir]Mitrović, Ana ...Lysosomal cysteine peptidase cathepsin B, involved in multiple processes associated with tumor progression, is validated as a target for anti-cancer therapy. Nitroxoline, a known antimicrobial agent, ... is a potent and selective inhibitor of cathepsin B, hence reducing tumor progression in vitro and in vivo. In order to further improve its anti-cancer properties we developed a number of derivatives using structure-based chemical synthesis. Of these, the 7-aminomethylated derivative (compound 17) exhibited significantly improved kinetic properties over nitroxoline, inhibiting cathepsin B endopeptidase activity selectively. In the present study, we have evaluated its anti-cancer properties. It was more effective than nitroxoline in reducing tumor cell invasion and migration, as determined in vitro on two-dimensional cell models and tumor spheroids, under either endpoint or real time conditions. Moreover, it exhibited improved action over nitroxoline in impairing tumor growth in vivo in LPB mouse fibrosarcoma tumors in C57Bl/6 mice. Taken together, the addition of a 2-(ethylamino)acetonitrile group to nitroxoline at position 7 significantly improves its pharmacological characteristics and its potential for use as an anti-cancer drug.Vir: Oncotarget [Elektronski vir]. - ISSN 1949-2553 (Vol. 8, no. 35, 2017, str. 59136-59147)Vrsta gradiva - e-članek ; neleposlovje za odrasleLeto - 2017Jezik - angleškiCOBISS.SI-ID - 4360305
Avtor
Mitrović, Ana |
Sosič, Izidor |
Kos, Špela, farmacija |
Lampreht Tratar, Urša |
Breznik, Barbara, 1989- |
Kranjc Brezar, Simona |
Mirković, Bojana |
Gobec, Stanislav, 1970- |
Lah Turnšek, Tamara |
Čemažar, Maja |
Serša, Gregor |
Kos, Janko, 1959-
Teme
nitroxoline derivative |
cathepsin B |
inhibition |
tumor invasion |
cell migration
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Avtor | Mitrović, Ana ... |
Naslov | Addition of 2-(ethylamino)acetonitrile group to nitroxoline results in significantly improved anti-tumor activity in vitro and in vivo [Elektronski vir] |
Datum objave | 2017-07-17 |
COBISS.SI-ID | 4360305 |
Verzija objave v repozitoriju | Založnikova različica |
Licenca objave v repozitoriju | Creative Commons Priznanje avtorstva 4.0 Mednarodna |
Embargo | Takojšnja javna objava |
Projekti, iz katerih je bila financirana objava
Naziv | Akronim | Številka projekta | Financer |
---|---|---|---|
Nitroksolin in njegovi derivati kot nova protitumorska zdravila | J4-5529-2013 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Farmacevtska biotehnologija: znanost za zdravje | P4-0127-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
|
Strukturno podprta optimizacija na nitroksolinu osnovanih zaviralcev katepsina B kot potencialnih zdravil za zdravljenje raka | Z1-7181-2016 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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Baze podatkov, v katerih je revija indeksirana
Ime baze podatkov | Področje | Leto |
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Povezave do osebnih bibliografij avtorjev | Povezave do podatkov o raziskovalcih v sistemu SICRIS |
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Mitrović, Ana | 36440 |
Sosič, Izidor | 30816 |
Kos, Špela, farmacija | 36366 |
Lampreht Tratar, Urša | 36367 |
Breznik, Barbara, 1989- | 36319 |
Kranjc Brezar, Simona | 19058 |
Mirković, Bojana | 29604 |
Gobec, Stanislav, 1970- | 15284 |
Lah Turnšek, Tamara | 07802 |
Čemažar, Maja | 14575 |
Serša, Gregor | 08800 |
Kos, Janko, 1959- | 04648 |
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