Synthesis of novel purpurealidin analogs and evaluation of their effect on the cancer-relevant potassium channel KV10.1
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DOI: 10.1371/journal.pone.0188811
Abstract: In the search for novel anticancer drugs, the potassium channel KV10.1 has emerged as an interesting cancer target. Here, we report a new group of KV10.1 inhibitors, namely the purpurealidin analogs. These alkaloids are produced… read more here.
Keywords: channel kv10; kv10; purpurealidin analogs; potassium channel ... See more keywords
A Multidisciplinary Approach Establishes a Link between Transglutaminase 2 and the Kv10.1 Voltage-Dependent K+ Channel in Breast Cancer
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DOI: 10.3390/cancers15010178
Abstract: Simple Summary This work intends to unravel one of the roles played by transglutaminase 2 within the cell. We highlighted its physical interaction with the voltage-dependent Kv10.1 K+ channel, an important target of therapies in… read more here.
Keywords: breast cancer; voltage dependent; kv10; transglutaminase ... See more keywords
Molecular Dynamics-Derived Pharmacophore Model Explaining the Nonselective Aspect of KV10.1 Pore Blockers
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DOI: 10.3390/ijms22168999
Abstract: 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 ligands are known to inhibit KV10.1, and almost all… read more here.
Keywords: kv10; molecular dynamics; kv10 pore; dynamics derived ... See more keywords
New Diarylamine KV10.1 Inhibitors and Their Anticancer Potential
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DOI: 10.3390/pharmaceutics14091963
Abstract: 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… read more here.
Keywords: 17a 18b; diarylamine kv10; kv10 inhibitors; new diarylamine ... See more keywords