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Št. zadetkov: 4
Attenuation of Nicotine Effects on A549 Lung Cancer Cells by Synthetic α7 nAChR Antagonists APS7-2 and APS8-2
Ahmad Joukhan, Veno Kononenko, Tadeja Bele, Marija Sollner Dolenc, Steve Peigneur, Ernesto Lopes Pinheiro-Junior, Jan Tytgat, Tom Turk, Igor Križaj, Damjana Drobne
Izvirni znanstveni članek
Oznake: marine toxin;nicotinic acetylcholine receptor;nAChR antagonist;APS7-2;APS8-2;
Nicotine binds to nicotinic acetylcholine receptors (nAChRs) that are overexpressed in different cancer cells, promoting tumor growth and resistance to chemotherapy. In this study, we aimed to investigate the potential of APS7-2 and APS8-2, synthetic analogs of a marine sponge toxin, to inhibit nico ...
Leto: 2024 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: 4
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