Key result
Quantitative structure-activity relationship (QSAR) studies on Kv1.3-channel and I(Ks)-channel blockers were conducted to provide guidelines for antiarrhythmic and immunosuppressive drug development.
This computational study provides structural guidelines for developing novel potassium channel blockers targeting Kv1.3 and I(Ks) channels.
May guide preclinical Kv1.3/I(Ks) blocker design; leaves open clinical translation for arrhythmia or immunosuppression.
There has been an increasing interest in compounds that modulate potassium ion channels (K(+)-channels) since they can be developed as important therapeutic agents against ischemic heart diseases. Of the diverse family of K(+)-channels, the voltage-gated potassium channel Kv1.3 constitutes an attractive target for the selective suppression of effector memory T cells in autoimmune diseases. For the development of antiarrythmic drugs, the blockade of the rapidly activating delayed rectifier (I(Kr)) and slowly activating delayed rectifier (I(Ks)) potassium currents has been specifically studied. Since the discovery of I(Ks)-channel, its blockers have been particularly more studied. In this communication, we present QSAR studies on a few series of Kv1.3-channel blockers and a series of I(Ks)-channel blockers in order to provide some guidelines to the drug development.
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Satuluri et al. (2009) studied Ischemic heart diseases and autoimmune diseases (target conditions). Kv1.3-channel blockers and I(Ks)-channel blockers was evaluated. Quantitative structure-activity relationship (QSAR) studies on Kv1.3-channel and I(Ks)-channel blockers were conducted to provide guidelines for antiarrhythmic and immunosuppressive drug development.
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