Kv1.5 Potassium Channel Blocker Focused Library from OTAVA

- Jan 27, 2015 - Potassium channels are attractive therapeutic targets for treatment of cardiovascular and cancer diseases which are the top two public-health problems for the aging population. OTAVA Ltd. offersKv1.5 Potassium Channel Blocker focused libraryfor ion channel-related research and drug discovery projects.

Potassium voltage-gated channel, member 5, also known as KCNA5, or Kv1.5, is expressed in the heart and pancreatic beta-cells. It was found that mutations in KCNA5 gene are related to atrial fibrillation and sudden cardiac death. Kv1.5 channels have been shown to restore the resting membrane potential of beta cells after depolarization, which indicates their role in regulation of insulin secretion.

Accumulating evidences demonstrate that Kv1.5 channels are aberrantly expressed in a number of human cancers. These channels could serve both as novel markers of the metastatic phenotype and as potential new therapeutic targets.

The new Kv1.5 Potassium Channel Blocker focused library from OTAVA comprises 1,071 drug-like compounds. The library has been designed as a special screening collection containing compounds with predicted Kv1.5 blocking activity and selectivity. A four-center pharmacophore model developed by Yang et al. which includes one aromatic ring, two hydrophobic points, and a hydrogen-bond acceptor has been used for the library design. The model was obtained from forty Kv1.5 blocker compounds with distinct chemical structure types.

More information about this library you can find at the OTAVA’s web-site: www.otavachemicals.com .