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Št. zadetkov: 5
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)
Discovery of K V 1.3 ion channel inhibitors
Špela Gubič, Louise Antonia Hendrickx, Žan Toplak, Maša Sterle, Steve Peigneur, Tihomir Tomašić, Luis A. Pardo, Jan Tytgat, Anamarija Zega, Lucija Peterlin-Mašič
Pregledni znanstveni članek
Oznake: KV1.3 channel;design of KV1.3 inhibitors;mitochondrial KV1.3;peptide inhibitors;small-molecule inhibitors;
The KV1.3 voltage gated potassium ion channel is involved in many physiological processes both at the plasma membrane and in the mitochondria, chiefly in the immune and nervous systems. Therapeutic targeting KV1.3 with specific peptides and small molecule inhibitors shows great potential for treatin ...
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)
Immunosuppressive effects of new thiophene-based Kv1.3 inhibitors
Špela Gubič, Alberto Montalbano, Cesare Sala, Andrea Becchetti, Louise Antonia Hendrickx, Kenny M. Van Theemsche, Ernesto Lopes Pinheiro-Junior, Janez Ilaš, Tihomir Tomašić, Lucija Peterlin-Mašič
Izvirni znanstveni članek
Oznake: inhibitorji;ionski kanal KV1.3;T-limfocitni imunosupresiv;ion channel;KV1.3 inhibitor;T-lymphocyte;immunosuppressive;
Voltage-gated potassium channel KV1.3 inhibitors have been shown to be effective in preventing T-cell proliferation and activation by affecting intracellular Ca2+ homeostasis. Here, we present the structure-activity relationship, KV1.3 inhibition, and immunosuppressive effects of new thiophene-based ...
Leto: 2023 Vir: Fakulteta za farmacijo (UL FFA)
Št. zadetkov: 5
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