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Blockade of the voltage-gated potassium channel Kv1.3 inhibits immune responses in vivo.
In vivo evidence is provided that Kv1.3 is a novel target for immunomodulation by demonstrating that the voltage activated K+ channel is present on peripheral T cells of miniswine and that blockade of Kv 1.3 inhibits both a delayed-type hypersensitivity reaction and an Ab response to an allogeneic challenge.
Identification and biochemical characterization of a novel nortriterpene inhibitor of the human lymphocyte voltage-gated potassium channel, Kv1.3.
Correolide is the first potent, small molecule inhibitor of Kv1 series channels to be identified from a natural product source and will be useful as a probe for studying potassium channel structure and the physiological role of such channels in target tissues of interest.
The inhibition of receptor-mediated and voltage-dependent calcium entry by the antiproliferative L-651,582.
The inhibition of cellular proliferation and the production of arachidonate metabolites by L-651,582 may be the result of the nearly equipotent block of receptor-operated and voltage-gated calcium channels.
Identification of a new class of inhibitors of the voltage-gated potassium channel, Kv1.3, with immunosuppressant properties.
Data suggest that DSC derivatives represent a new class of immunosuppressant agents and that specific interactions of trans DSC analogues with channel conformations related to C-type inactivation may permit development of selective K(v)1.3 channel inhibitors useful for the safe treatment of autoimmune diseases.
Protein surface recognition by rational design: nanomolar ligands for potassium channels.
The rational design and development of four-fold symmetrical ligands for potassium channels is described.
Characterization of a new class of potent inhibitors of the voltage-gated sodium channel Nav1.7.
Members of the novel 1-benzazepin-2-one structural class of Nav1 blockers can display selectivity toward the peripheral nerve Nav1.7 channel subtype, and with appropriate pharmacokinetic and drug metabolism properties, these compounds could be developed as analgesic agents.
Bis(benzylisoquinoline) analogs of tetrandrine block L-type calcium channels: evidence for interaction at the diltiazem-binding site.
Data indicate that a variety of bis(benzylisoquinoline) congeners act to block the L-type Ca2+ channel by binding to the benzothiazepine site on the channel.
Binding of Correolide to the Kv1.3 Potassium Channel: Characterization of the Binding Domain by Site-Directed Mutagenesis†
Correolide is a novel immunosuppressant that inhibits the voltage-gated potassium channel Kv1.3 [Felix et al. (1999) Biochemistry 38, 4922−4930]. [3H]Dihydrocorreolide (diTC) binds with high affini...
Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile.
A large body of evidence is presented which indicates that the potencies of wild-type ShK peptide for both K( v)1.3 and K(v) 1.1 channels have been previously underestimated and suggests that ShK-Dap(22) will not have the same in vivo immunosuppressant efficacy of other K.3 blockers, such as margatoxin or ShK.
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.
A series of benzodiazepines and benzazepinones were synthesized and evaluated as potential sodium channel blockers in a functional, membrane potential-based assay. One member of the benzazepinone