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Št. zadetkov: 4
3D pharmacophore-based discovery of novel Kv10.1 inhibitors with antiproliferative activity
Žan Toplak, Louise Antonia Hendrickx, Špela Gubič, Štefan Možina, Bojana Žegura, Alja Štraser, Matjaž Novak, Xiaoyi Shi, Tihomir Tomašić, Lucija Peterlin-Mašič
Izvirni znanstveni članek
Oznake: KV10.1;ion channels;hERG;pharmacophore modelling;virtual screening;antiproliferative activity;
Background: The voltage-gated potassium channel KV10.1 (Eag1) is considered a near- universal tumour marker and represents a promising new target for the discovery of novel anticancer drugs. (2) Methods: We utilized the ligand-based drug discovery methodology using 3D pharmacophore modelling and med ...
Leto: 2021 Vir: Fakulteta za farmacijo (UL FFA)
Design of new potent and selective thiophene-based Kv1.3 inhibitors and their potential for anticancer activity
Špela Gubič, Louise Antonia Hendrickx, Xiaoyi Shi, Žan Toplak, Štefan Možina, Kenny M. Van Theemsche, Ernesto Lopes Pinheiro-Junior, Steve Peigneur, Tihomir Tomašić, Lucija Peterlin-Mašič
Izvirni znanstveni članek
Oznake: Kv1.3;kalijevi ionski kanali;antiproliferativno delovanje;zdravila proti raku;potassium ion channels;antiproliferative activity;apoptosis;anticancer drugs;
The voltage-gated potassium channel KV1.3 has been recognized as a tumor marker and represents a promising new target for the discovery of new anticancer drugs. We designed a novel structural class of KV1.3 inhibitors through structural optimization of benzamide-based hit compounds and structure-act ...
Leto: 2022 Vir: Fakulteta za farmacijo (UL FFA)
Discovery and Hit-to-Lead Optimization of Benzothiazole scaffold-based DNA gyrase inhibitors with potent activity against Acinetobacter baumannii and Pseudomonas aeruginosa
Andrej Emanuel Cotman, Martina Durcik, Davide Benedetto Tiz, Federica Fulgheri, Maša Sterle, Štefan Možina, Žiga Skok, Nace Zidar, Anamarija Zega, Janez Ilaš, Lucija Peterlin-Mašič, Tihomir Tomašić, Danijel Kikelj
Izvirni znanstveni članek
Oznake: antibacterial activity;bacteria;genetics;inhibitors;solubility;
We have developed compounds with a promising activity against Acinetobacter baumannii and Pseudomonas aeruginosa, which are both on the WHO priority list of antibiotic-resistant bacteria. Starting from DNA gyrase inhibitor 1, we identified compound 27, featuring a 10-fold improved aqueous solubility ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
New dual inhibitors of bacterial topoisomerases with broad-spectrum antibacterial activity and In vivo efficacy against vancomycin - intermediate Staphylococcus aureus
Martina Durcik, Andrej Emanuel Cotman, Žan Toplak, Štefan Možina, Žiga Skok, Maria Vittoria Piras, Nace Zidar, Janez Ilaš, Anamarija Zega, Jurij Trontelj, Danijel Kikelj, Tihomir Tomašić, Lucija Peterlin-Mašič
Izvirni znanstveni članek
Oznake: antibacterial activity;bacteria;inhibitors;
A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and topoisomerase IV were developed. The resulting compounds show excellent broad-spectrum antibacterial activities against Gram-positive Enterococcus faecalis, Enterococcus faecium and multidrug resistant (MDR) Stap ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 4
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