ABCMdb

PMID: 23665564

Ortiz D, Gossack L, Quast U, Bryan J
Reinterpreting the action of ATP analogs on K(ATP) channels.
J Biol Chem. 2013 Jun 28;288(26):18894-902. doi: 10.1074/jbc.M113.476887. Epub 2013 May 12., [PubMed]

Sentences

No. Mutations Sentence Comment

81 ABCC8 p.Gln1178Arg The E1507Q and Q1178R substitutions do not have large effects on the affinities of the apo-receptors for GBC, given by the dissociation constants (KG), which are determined in independent experiments (Table 1). Login to comment 89 ABCC8 p.Gln1178Arg Dashed curves are fits to a logistic equation used to estimate the IC50 values (in òe;M): WT: 1163 afe; 439, slope afd; 0.8 afe; 0.1; Q1178R: 17 afe; 3, slope afd; 0.8 afe; 0.1; E1507Q: 2.7 afe; 0.4, slope afd; 0.8 afe; 0.1. Login to comment 92 ABCC8 p.Gln1178Arg The parameters are KT afd; 1 òe;M and beta afd; 40 with a defined valueforKG afd;0.63nM.B,theeffectofATP4afa; onGBCbinding.Thecurvesarethebest fitstothefour-statemodel.TheparametersareKT afd;94,2550,and13,400òe;Mandbetaafd; 40,9.2,and15.1withKGdefinedas0.63,1.0,and0.25nM,forE1507Q,Q1178R,andWT, respectively. Login to comment 94 ABCC8 p.Gln1178Arg TABLE 1 Binding parameters (KG, IC50, and KT values) for WT, Q1178R, and E1507Q KG values are nM; all IC50 and KT values are òe;M. Login to comment 96 ABCC8 p.Gln1178Arg KG IC50 KT MgATP MgADP MgATP (beta) ATP4d1a; (beta) MgATPॹS (beta) ATPॹS4d1a; (beta) WT 0.25 afe; 0.02 1163 afe; 439 161 afe; 28 - 13,400 afe; 3360 (15.1 afe; 9.4) - - Q1178R 1.0 afe; 0.1 17 afe; 3 25 afe; 2 - 2550 afe; 290 (9.2 afe; 1.4) - - E1507Q 0.63 afe; 0.16 2.7 afe; 0.4 - 1 afe; 0.2 (40 afe; 3) 94 afe; 8 (40 afe; 1) 29 afe; 7 (11.6 afe; 3) 234 afe; 31 (3.2 afe; 0.1) Action of ATP Analogs on SUR1 18896 four-state model. Login to comment 135 ABCC8 p.Gln1178Arg The solid lines are fits to a logistic equation: IC50 values: WT: 161 afe; 28, slope afd; 1.7 afe; 0.4; Q1178R: 25 afe; 2, slope afd; 1.5 afe; 0.1. Login to comment 193 ABCC8 p.Gln1178Arg Substi- TABLE 2 Binding parameters (S0.5 and K1, K2, and KA values) for Q1178R and E1507Q Values are òe;M; K1 and K2, the affinities for MgATP at NBD1 and NBD2, respectively and KA, the affinity for MgAMP-PNP at NBD1, were estimated using an eight-state model. Login to comment 195 ABCC8 p.Gln1178Arg SUR1 S0.5 K1 K2 KA MgAMP-PNP MgAMP-PCP AMP-PNP4d1a; Q1178R 530 afe; 124 - - - - - E1507Q 573 afe; 103 3360 afe; 410 31100 afe; 2240 0.7 afe; 0.2 1.5 afe; 0.1 1.2 afe; 0.2 FIGURE 5. Login to comment