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KU124 (9,10,10-trioxo-N-(2-phenylphenyl)thioxanthene-3-carboxamide) as a novel inhibitor of TASK-1

by Aleynik, Alexander , Valdizno, Rhustie , Awoleye, Oluwatoni , Blaisdell, Megan , Jacob, Annette , Julemis, Martha , Martins, Patrick , Korotka, Sofiia , Lee, Lamont , Dennis, Marilyn , Contreras, Anthony , George, Rinchu , Patino, Justin , Best, Jessica , Schwartz, Sarah , Farrag, Yara , Graham, David , Figueroa Chea, Diana , Amankwaa, Abena , Anin, Irene , Yousuf, Shuayb , Pelley, Chelsea , Dumani, Ana , Marciano, Jenna , Patel, Hinaben , Zahed, Ramish , Elhowary, Youssef , Lang, Sophia , Chavez, Diego , Kiszka, Gianna , Lopez, Joana , Comollo, Thomas Walter , Salgado, Ericka , Brown, Jonelle , Medeiros, Gianna , Mastrodomenico, Nikki , Almazan, Steven

in Apoptosis / Cardiac arrhythmia / Cardiomyocytes / Cell growth / Excitability / inhibitor / KU124 / Ligands / molecular dynamics / Nervous system / Non-small cell lung carcinoma / Pharmacology / Potassium / Potassium channels / Small cell lung carcinoma / Smooth muscle / Stimulants / thallium flux / Thioxanthene / TWIK-related acid-sensitive potassium channel 1 / virtual screening

2025

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KU124 (9,10,10-trioxo-N-(2-phenylphenyl)thioxanthene-3-carboxamide) as a novel inhibitor of TASK-1

2025

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KU124 (9,10,10-trioxo-N-(2-phenylphenyl)thioxanthene-3-carboxamide) as a novel inhibitor of TASK-1

2025

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Journal Article

KU124 (9,10,10-trioxo-N-(2-phenylphenyl)thioxanthene-3-carboxamide) as a novel inhibitor of TASK-1

Aleynik, Alexander,

Valdizno, Rhustie,

Awoleye, Oluwatoni,

Blaisdell, Megan,

Jacob, Annette,

Julemis, Martha,

Martins, Patrick,

Korotka, Sofiia,

Lee, Lamont,

Dennis, Marilyn,

Contreras, Anthony,

George, Rinchu,

Patino, Justin,

Best, Jessica,

Schwartz, Sarah,

Farrag, Yara,

Graham, David,

Figueroa Chea, Diana,

Amankwaa, Abena,

Anin, Irene,

Yousuf, Shuayb,

Pelley, Chelsea,

Dumani, Ana,

Marciano, Jenna,

Patel, Hinaben,

Zahed, Ramish,

Elhowary, Youssef,

Lang, Sophia,

Chavez, Diego,

Kiszka, Gianna,

Lopez, Joana,

Comollo, Thomas Walter,

Salgado, Ericka,

Brown, Jonelle,

Medeiros, Gianna,

Mastrodomenico, Nikki,

Almazan, Steven

2025

Overview

TASK-1 is a two-pore K + leak channel. The name, TASK-1, stands for TWIK-related acid-sensitive potassium channel 1, and this channel is encoded by the KCNK3 gene. TASK-1 channels are expressed in humans and modulate cell excitability in excitable cells such as neurons, cardiomyocytes, and vascular smooth muscle cells. TASK-1 inhibition is a mechanism of action for some respiratory stimulants, such as doxapram. TASK-1 channels have also been suggested to play a role in circumventing cell apoptosis in a population of non-small-cell lung cancer cells. We propose that the inner vestibule of the TASK-1 channel, a known binding site of known TASK-1 inhibitors, BAY10000493 and BAY2341237, can be exploited via virtual screening to find other novel TASK-1 inhibitors. Our results show that by targeting the inner vestibule site, we found an active TASK-1 inhibitor. We suspect that this region of interest can be further exploited to discover additional TASK-1 inhibitors. Our initial success lends validity to our virtual screening methodology and parameters. In this study, we identified a novel TASK-1 inhibitor, KU124, which we verified using an in vitro assay.

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Frontiers Media SA,Frontiers Media S.A

Subject

/ KU124