[HTML][HTML] Potassium channels as a target for cancer therapy: Current perspectives

L Zúñiga, A Cayo, W González, C Vilos… - OncoTargets and …, 2022 - ncbi.nlm.nih.gov
Potassium (K+) channels are highly regulated membrane proteins that control the potassium
ion flux and respond to different cellular stimuli. These ion channels are grouped into three …

Computational methods for unlocking the secrets of potassium channels: Structure, mechanism, and drug design

L Wang, Q Zhang, HHY Tong, X Yao… - Wiley Interdisciplinary …, 2024 - Wiley Online Library
Potassium (K+) channels play vital roles in various physiological functions, including
regulating K+ flow in cell membranes, impacting nervous system signal transduction …

New dual inhibitors of bacterial topoisomerases with broad-spectrum antibacterial activity and in vivo efficacy against vancomycin-intermediate Staphylococcus …

M Durcik, AE Cotman, Z Toplak, S Mozina… - Journal of medicinal …, 2023 - ACS Publications
A new series of dual low nanomolar benzothiazole inhibitors of bacterial DNA gyrase and
topoisomerase IV were developed. The resulting compounds show excellent broad …

Development of narrow-spectrum topoisomerase-targeting antibacterials against mycobacteria

M Sterle, E Habjan, M Piga, P Peršolja, M Durcik… - European Journal of …, 2024 - Elsevier
New 2-pyrrolamidobenzothiazole-based inhibitors of mycobacterial DNA gyrase were
discovered. Among these, compounds 49 and 51, show excellent antibacterial activity …

[HTML][HTML] Anti-tumor pharmacology of natural products targeting mitosis

M Huang, C Liu, Y Shao, S Zhou, G Hu… - Cancer Biology & …, 2022 - ncbi.nlm.nih.gov
Cancer has been an insurmountable problem in the history of medical science. The
uncontrollable proliferation of cancer cells is one of cancer's main characteristics, which is …

New Diarylamine KV10.1 Inhibitors and Their Anticancer Potential

Š Gubič, Ž Toplak, X Shi, J Dernovšek, LA Hendrickx… - Pharmaceutics, 2022 - mdpi.com
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 …

Corydaline binds to a druggable pocket of hEAG1 channel and inhibits hepatic carcinoma cell viability

B Ma, S Shi, S Ren, C Qu, Z Zhao, H An - European Journal of …, 2024 - Elsevier
Abstract Ether-à-go-go (EAG) potassium channels play a crucial role in the regulation of
neuronal excitability and cancer progression, rendering them potential drug targets for …

Molecular Dynamics-Derived Pharmacophore Model Explaining the Nonselective Aspect of KV10.1 Pore Blockers

Ž Toplak, F Merzel, LA Pardo, L Peterlin Mašič… - International journal of …, 2021 - mdpi.com
The KV10. 1 voltage-gated potassium channel is highly expressed in 70% of tumors, and
thus represents a promising target for anticancer drug discovery. However, only a few …

Structure-Function Studies of Sponge-Derived Compounds on the Cardiac CaV3.1 Channel

AS Depuydt, PA Patel, Ž Toplak, C Bhat… - International journal of …, 2023 - mdpi.com
T-type calcium (CaV3) channels are involved in cardiac automaticity, development, and
excitation–contraction coupling in normal cardiac myocytes. Their functional role becomes …

Conopeptides as tools for studying pacemaker channels and for the development of novel cardiovascular drugs

AS Depuydt, J Tytgat, S Peigneur - 2022 - lirias.kuleuven.be
Cardiovascular diseases are the leading cause of death in the world, accounting for the
death of 17.9 million people every year. Based on data from the World Health Organization …