Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8366760 | Steroids | 2016 | 8 Pages |
Abstract
A survey of nearly two hundred reports shows that rapid estrogenic actions can be detected across a range of kinds of estrogens, a range of doses, on a wide range of tissue, cell and ion channel types. Striking is the fact that preparations of estrogenic agents that do not permeate the cell membrane almost always mimic the actions of the estrogenic agents that do permeate the membrane. All kinds of estrogens, ranging from natural ones, through receptor modulators, endocrine disruptors, phytoestrogens, agonists, and antagonists to novel G-1 and STX, have been reported to be effective. For actions on specific types of ion channels, the possibility of opposing actions, in different cases, is the rule, not the exception. With this variety there is no single, specific action mechanism for estrogens per se, although in some cases estrogens can act directly or via some signaling pathways to affect ion channels. We infer that estrogens can bind a large number of substrates/receptors at the membrane surface. As against the variety of subsequent routes of action, this initial step of the estrogen's binding action is the key.
Keywords
P2X3PLCPKCBPANMDARDPNKirTMXPKGKATPEBTSERM2me2GIRKSTX5-HT3RXenoestrogenPIP2Delayed rectifier K+ channelKCNQ1DTPSelective estrogen receptor modulator (SERM)Ion channel kineticsE-BSA[Ca++]iAMPARcGMPTPEPPTCAVEE2nAChRpKaHERGCREB17β-estradiolcAMPERK1/2MAPKα-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptorCyclic adenosine monophosphateDESIsKBisphenol ABBPintracellular Ca2+ concentrationphospholipase CPhytoestrogenendocrine disruptorSelective estrogen receptor modulatorSignaling pathwaycyclic guanosine monophosphateNitric oxidecAMP response element-binding proteinprotein kinase Aprotein kinase GProtein kinase CKarL-type Ca2+ channelT-type Ca2+ channelVoltage-gated Ca2+ channelVoltage-gated K+ channelATP-sensitive K+ channelinward rectifier K+ channelN-type Ca2+ channelextracellular signal-regulated kinase 1/2mitogen-activated protein kinasesGABAARN-methyl-d-aspartate receptornicotinic acetylcholine receptor
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Authors
Lee-Ming Kow, Donald W. Pfaff,