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Št. zadetkov: 3
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)
New diarylamine KV10.1 inhibitors and their anticancer potential
Špela Gubič, Žan Toplak, Xiaoyi Shi, Jaka Dernovšek, Louise Antonia Hendrickx, Ernesto Lopes Pinheiro-Junior, Steve Peigneur, Jan Tytgat, Luis A. Pardo, Lucija Peterlin-Mašič, Tihomir Tomašić
Izvirni znanstveni članek
Oznake: KV10.1;ionski kanali;hERG;SAR;antiproliferativno delovanje;ion channels;antiproliferative activity;
Expression of the voltage-gated potassium channel KV10.1 (Eag1) has been detected in over 70% of human cancers, making the channel a promising new target for new anticancer drug discovery. A new structural class of KV10.1 inhibitors was prepared by structural optimisation and exploration of the stru ...
Leto: 2022 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)
Št. zadetkov: 3
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