Imaging of the calcium activated potassium channel 3.1 (K 3.1) in vivo using a senicapoc-derived positron emission tomography tracer.

The calcium-activated potassium channel 3.1 (K 3.1) is overexpressed in many tumor entities and has predictive power concerning disease progression and outcome.

Targeting K3.1 Channels in Cancer.

The K3.1 channels, previously designated as IK1 or SK4 channels and encoded by the KCNN4 gene, are activated by a rise of the intracellular Ca concentration. These K channels are widely expressed in many organs and involved in many pathologies.

Diastereoselective synthesis of conformationally restricted KOR agonists.

In order to analyze the bioactive conformation of flexible KOR agonists the ethylenediamine KOR pharmacophore was conformationally constrained by incorporation into a bicyclic system. For this purpose, 2-azabicyclo[3.2.

Computational Ion Channel Research: from the Application of Artificial Intelligence to Molecular Dynamics Simulations.

Although ion channels are crucial in many physiological processes and constitute an important class of drug targets, much is still unclear about their function and possible malfunctions that lead to diseases. In recent years, computational methods have evolved into important and invaluable approaches for studying ion channels and their functions. This is mainly due to their demanding mechanism of action where a static picture of an ion channel structure is often insufficient to fully understand the underlying mechanism.

Co-staining of K 3.1 Channels in NSCLC Cells with a Small-Molecule Fluorescent Probe and Antibody-Based Indirect Immunofluorescence.

The Ca activated potassium channel 3.1 (K 3.1) is involved in critical steps of the metastatic cascade, such as proliferation, migration, invasion and extravasation.

Synthesis of Small-Molecule Fluorescent Probes for the In Vitro Imaging of Calcium-Activated Potassium Channel K 3.1.

Small-molecule probes for the in vitro imaging of K 3.1 channel-expressing cells were developed. Senicapoc, showing high affinity and selectivity for the K 3.