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Št. zadetkov: 5
Action of clathrodin and analogues on voltage-gated sodium channels
Steve Peigneur, Aleš Žula, Nace Zidar, Fiona Chan-Porter, Robert Kirby, David J. Madge, Janez Ilaš, Danijel Kikelj, Jan Tytgat
Izvirni znanstveni članek
Oznake: oroidin;hymenidin;clathrodin;voltage-gated sodium channels;sodium channel modulator;sponge;
Clathrodin is a marine alkaloid and believed to be a modulator of voltage-gated sodium (NaV) channels. Since there is an urgent need for small molecule NaV channel ligands as novel therapeutics, clathrodin could representan interesting lead compound. Therefore, clathrodin was reinvestigated for its ...
Leto: 2014 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)
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)
Št. zadetkov: 5
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