title: Modulation of the voltage-gated potassium channel Kv2.1 by the anti-tumor alkylphospholipid perifosine.
abstract: BACKGROUND
  The aim of the present study was to assess the effects of perifosine-a third generation alkylphospholipid analog with anti-tumor properties-on the activity of Kv2.1 channels.
  
  
  METHODS
  The whole-cell patch clamp technique was applied to follow the modulatory effect of perifosine on Kv2.1 channels expressed in HEK293 cells.
  
  
  RESULTS
  Obtained data provide evidence that perifosine application decreases the whole cell Kv2.1 currents in a concentration-independent manner. Perifosine induces a hyperpolarizing shift in the voltage dependence of Kv2.1 channels inactivation without altering the voltage dependence of channels activation. The kinetics of Kv2.1 closed-state inactivation was accelerated by perifosine, with no significant effects on the recovery rate from inactivation.
  
  
  CONCLUSIONS
  Taken together, these results show that perifosine modified the Kv2.1 inactivation gating resulting in a decrease of the current amplitude. These data will help to elucidate the mechanism of action of this promising anti-cancer drug on ion channels and their possible implications.
authors.affiliation: Departamento de Fisiología y Biofísica, Facultad de Medicina, Universidad Autónoma de San Luis Potosí, San Luis Potosí, México.
authors.forename: Mayra
authors.initials: M
authors.lastname: Delgado-Ramírez
authors.affiliation: Departamento de Fisiología y Biofísica, Facultad de Medicina, Universidad Autónoma de San Luis Potosí, San Luis Potosí, México.
authors.forename: Rita
authors.initials: R
authors.lastname: Morán-Zendejas
authors.affiliation: Departamento de Fisiología y Biofísica, Facultad de Medicina, Universidad Autónoma de San Luis Potosí, San Luis Potosí, México.
authors.forename: Ivan A
authors.initials: IA
authors.lastname: Aréchiga-Figueroa
authors.affiliation: Departamento de Ciencias Computacionales, Centro Universitario de Ciencias Exactas e Ingenierías, Universidad de Guadalajara, Jalisco, México.
authors.forename: Carmen
authors.initials: C
authors.lastname: Toro-Castillo
authors.affiliation: Departamento de Fisiología y Biofísica, Facultad de Medicina, Universidad Autónoma de San Luis Potosí, San Luis Potosí, México.
authors.forename: Juan F
authors.initials: JF
authors.lastname: Ramírez-Martínez
authors.affiliation: Departamento de Fisiología y Biofísica, Facultad de Medicina, Universidad Autónoma de San Luis Potosí, San Luis Potosí, México. Electronic address: aldo.rodriguez@uaslp.mx.
authors.forename: Aldo A
authors.initials: AA
authors.lastname: Rodríguez-Menchaca
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D002460:Cell Line; D057809:HEK293 Cells; D006801:Humans; D015640:Ion Channel Gating / Q000187:drug effects*; D007700:Kinetics; D008564:Membrane Potentials / Q000187:drug effects; D018408:Patch-Clamp Techniques / Q000379:methods; D010767:Phosphorylcholine / Q000031:analogs & derivatives* / Q000494:pharmacology; D011188:Potassium / Q000378:metabolism; D024642:Potassium Channels, Voltage-Gated / Q000378:metabolism*; D051669:Shab Potassium Channels / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; C496988:KCNB1 protein, human; D024642:Potassium Channels, Voltage-Gated; D051669:Shab Potassium Channels; D010767:Phosphorylcholine; C105905:perifosine; D011188:Potassium
keywords: Alkylphospholipid; Kv2.1; Perifosine; Potassium channels