2009
DOI: 10.1016/j.bmcl.2009.02.077
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Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants

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Cited by 49 publications
(34 citation statements)
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“…In 2009, Pegaro et al reported the discovery of two structurally new classes of Kv1.3 and KCa3.1 inhibitors based on a virtual high throughput screening approach [84]. A homology model of the Kv1.3 channel was created from the crystal structure of the bacterial KcsA channel and used for a virtual screen of around 3.3 million compounds.…”
Section: Small Molecule Kv13 Blockersmentioning
confidence: 99%
“…In 2009, Pegaro et al reported the discovery of two structurally new classes of Kv1.3 and KCa3.1 inhibitors based on a virtual high throughput screening approach [84]. A homology model of the Kv1.3 channel was created from the crystal structure of the bacterial KcsA channel and used for a virtual screen of around 3.3 million compounds.…”
Section: Small Molecule Kv13 Blockersmentioning
confidence: 99%
“…Thecatalytic cycle is initiated with an amino-assisted CÀHb ond cleavage of 1a by Pd-(OAc) 2 to give rise to as table palladacycle (4). Next, this dimeric palladium complex is broken into its component parts by 2 to form the intermediate I.N otably,i tw as known from prior work that migratory insertion of the alkyne 2 with 4 favored ar egioselective insertion into the PdÀCb ond to afford the eight-membered intermediate II.…”
Section: Methodsmentioning
confidence: 98%
“…[2] Functionalized dibenzo [b,d]azepines were also investigated as serotonin (5-HT) receptor [3] and potassium channel inhibitor. [4] Therefore, the search for new reliable synthetic approaches for the preparation of dibenzo [b,d]azepines from readily available starting materials is of great interest.…”
mentioning
confidence: 99%
“…Finally, potassium channels are attractive targets for drug discovery because of its implication in essential processes in biological systems. Pegoraro et al [115] identified blockers of Kv1.3 potassium channels using a KcsA template for homology modeling, and a virtual screening approach. The new compounds displayed inhibitory effects on T-cell and keratinocytes proliferation and immunosuppressant activity.…”
Section: Structure-based Methods Docking Virtual Screening and Molementioning
confidence: 99%