PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 31019304-0 2019 Serotonin transporter-ibogaine complexes illuminate mechanisms of inhibition and transport. Ibogaine 22-30 solute carrier family 6 member 4 Homo sapiens 0-21 35114149-2 2022 The cryo-EM structures of SERT bound to ibogaine and the physiological substrate serotonin resolved in different states provided a glimpse of functional conformations at atomistic resolution. Ibogaine 40-48 solute carrier family 6 member 4 Homo sapiens 26-30 7596224-3 1995 We report here that 12-hydroxyibogamine, a primary metabolite of ibogaine, displays high affinity for the 5-HT transporter and elevates extracellular 5-HT. Ibogaine 65-73 solute carrier family 6 member 4 Homo sapiens 106-122 31019304-7 2019 To elucidate structure-based mechanisms for transport in SERT we investigated its complexes with ibogaine, a hallucinogenic natural product with psychoactive and anti-addictive properties13,14. Ibogaine 97-105 solute carrier family 6 member 4 Homo sapiens 57-61 31019304-9 2019 Here we report cryo-electron microscopy structures of SERT-ibogaine complexes captured in outward-open, occluded and inward-open conformations. Ibogaine 59-67 solute carrier family 6 member 4 Homo sapiens 54-58 23776432-1 2013 The competitive inhibitor cocaine and the non-competitive inhibitor ibogaine induce different conformational states of the human serotonin transporter. Ibogaine 68-76 solute carrier family 6 member 4 Homo sapiens 129-150 23706649-7 2013 Inhibitor binding assays showed that both of the thermostabilised SERT mutants bound [(125)I]RTI55 (beta-CIT) with affinity similar to that of the wild-type transporter, although cocaine bound with increased affinity (17- to 56-fold) whilst ibogaine, imipramine and paroxetine all bound with lower affinity (up to 90-fold). Ibogaine 241-249 solute carrier family 6 member 4 Homo sapiens 66-70 28405636-4 2016 The folding trajectory of DAT itself is not understood, though many insights have been gained from studies of folding-deficient mutants of the closely related serotonin transporter (SERT); i.e. their functional rescue by pharmacochaperoning with (nor)ibogaine or heat-shock protein inhibitors. Ibogaine 251-259 solute carrier family 6 member 4 Homo sapiens 159-180 28405636-4 2016 The folding trajectory of DAT itself is not understood, though many insights have been gained from studies of folding-deficient mutants of the closely related serotonin transporter (SERT); i.e. their functional rescue by pharmacochaperoning with (nor)ibogaine or heat-shock protein inhibitors. Ibogaine 251-259 solute carrier family 6 member 4 Homo sapiens 182-186 23776432-2 2013 It has been shown from accessibility experiments that cocaine mainly induces an outward-facing conformation, while the non-competitive inhibitor ibogaine, and its active metabolite noribogaine, have been proposed to induce an inward-facing conformation of the human serotonin transporter similar to what has been observed for the endogenous substrate, serotonin. Ibogaine 145-153 solute carrier family 6 member 4 Homo sapiens 266-287 20889976-9 2010 SERT-RI(607,608)AA and SERT-RII(607-609)AAA were partially rescued by treatment of cells with the nonspecific chemical chaperone DMSO or the specific pharmacochaperone ibogaine (which binds to the inward facing conformation of SERT) but not by other classes of ligands (inhibitors, substrates, amphetamines). Ibogaine 168-176 solute carrier family 6 member 4 Homo sapiens 0-4 22451652-1 2012 Ibogaine, a hallucinogenic alkaloid proposed as a treatment for opiate withdrawal, has been shown to inhibit serotonin transporter (SERT) noncompetitively, in contrast to all other known inhibitors, which are competitive with substrate. Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 109-130 22451652-1 2012 Ibogaine, a hallucinogenic alkaloid proposed as a treatment for opiate withdrawal, has been shown to inhibit serotonin transporter (SERT) noncompetitively, in contrast to all other known inhibitors, which are competitive with substrate. Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 132-136 22451652-2 2012 Ibogaine binding to SERT increases accessibility in the permeation pathway connecting the substrate-binding site with the cytoplasm. Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 20-24 22451652-3 2012 Because of the structural similarity between ibogaine and serotonin, it had been suggested that ibogaine binds to the substrate site of SERT. Ibogaine 45-53 solute carrier family 6 member 4 Homo sapiens 136-140 22451652-3 2012 Because of the structural similarity between ibogaine and serotonin, it had been suggested that ibogaine binds to the substrate site of SERT. Ibogaine 96-104 solute carrier family 6 member 4 Homo sapiens 136-140 22451652-5 2012 Ibogaine noncompetitively inhibited transport by both SERT and the homologous dopamine transporter (DAT). Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 54-58 22451652-7 2012 When present on the cell exterior, ibogaine inhibited SERT substrate-induced currents, but not when it was introduced into the cytoplasm through the patch electrode. Ibogaine 35-43 solute carrier family 6 member 4 Homo sapiens 54-58 22451652-9 2012 The kinetics of inhibitor binding and dissociation, as determined by their effect on SERT currents, indicated that ibogaine does not inhibit by forming a long-lived complex with SERT, but rather binds directly to the transporter in an inward-open conformation. Ibogaine 115-123 solute carrier family 6 member 4 Homo sapiens 85-89 22451652-9 2012 The kinetics of inhibitor binding and dissociation, as determined by their effect on SERT currents, indicated that ibogaine does not inhibit by forming a long-lived complex with SERT, but rather binds directly to the transporter in an inward-open conformation. Ibogaine 115-123 solute carrier family 6 member 4 Homo sapiens 178-182 20889976-9 2010 SERT-RI(607,608)AA and SERT-RII(607-609)AAA were partially rescued by treatment of cells with the nonspecific chemical chaperone DMSO or the specific pharmacochaperone ibogaine (which binds to the inward facing conformation of SERT) but not by other classes of ligands (inhibitors, substrates, amphetamines). Ibogaine 168-176 solute carrier family 6 member 4 Homo sapiens 23-27 20889976-9 2010 SERT-RI(607,608)AA and SERT-RII(607-609)AAA were partially rescued by treatment of cells with the nonspecific chemical chaperone DMSO or the specific pharmacochaperone ibogaine (which binds to the inward facing conformation of SERT) but not by other classes of ligands (inhibitors, substrates, amphetamines). Ibogaine 168-176 solute carrier family 6 member 4 Homo sapiens 23-27 17698848-1 2007 Ibogaine, a hallucinogenic alkaloid with purported anti-addiction properties, inhibited serotonin transporter (SERT) noncompetitively by decreasing V(max) with little change in the K(m) for serotonin (5-HT). Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 88-109 17698848-1 2007 Ibogaine, a hallucinogenic alkaloid with purported anti-addiction properties, inhibited serotonin transporter (SERT) noncompetitively by decreasing V(max) with little change in the K(m) for serotonin (5-HT). Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 111-115 17698848-2 2007 Ibogaine also inhibited binding to SERT of the cocaine analog 2beta-2-carbomethoxy-3-(4-[(125)I]iodophenyl)tropane. Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 35-39 17698848-4 2007 Ibogaine increased the reactivity of cysteine residues positioned in the proposed cytoplasmic permeation pathway of SERT but not at nearby positions out of that pathway. Ibogaine 0-8 solute carrier family 6 member 4 Homo sapiens 116-120 17698848-6 2007 These results are consistent with the proposal that ibogaine binds to and stabilizes the state of SERT from which 5-HT dissociates to the cytoplasm, in contrast with cocaine, which stabilizes the state that binds extracellular 5-HT. Ibogaine 52-60 solute carrier family 6 member 4 Homo sapiens 98-102