ABCC2 p.Lys324Ala
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PMID: 14965249
[PubMed]
Haimeur A et al: "The MRP-related and BCRP/ABCG2 multidrug resistance proteins: biology, substrate specificity and regulation."
No.
Sentence
Comment
400
However, four of the mutants (Lys324Ala in TM6, Lys483Ala in TM9, Arg1210Ala in TM16 and Arg1257Ala in TM17) showed decreased efflux of GSH conjugated methylfluorescein [281].
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ABCC2 p.Lys324Ala 14965249:400:30
status: NEW
PMID: 20082599
[PubMed]
Jemnitz K et al: "ABCC2/Abcc2: a multispecific transporter with dominant excretory functions."
No.
Sentence
Comment
97
Mutant Predicted location Substrate Activity changes Reference Human MRP2 Δ1-188 TMD0 LTC4 ↓ Fernandez et al., 2002 K316A JC, TM6 GMF ↔ Ryu et al., 2000 K324A TM6 GMF ↓ Ryu et al., 2000 K329A TM6 GMF ↔ Ryu et al., 2000 R412G DJ IC MTX ↓ Hulot et al., 2005 W417I IC, TM7-TM8 E2-17βG ↓ Hirouchi et al., 2004 LTC4 ↓ DNP-SG ↓ H439A TM8 GMF ↔ Ryu et al., 2000 K483A IC, JM, TM9 GMF ↓ Ryu et al., 2000 K590A JC, TM11 GMF ↔ Ryu et al., 2000 S789F NBD1 E2-17βG ↓ Hirouchi et al., 2004 LTC4 ↓ DNP-SG ↓↓ R1023A EC, JM, TM13 GMF ↔ Ryu et al., 2000 H1042A TM13 GMF ↔ Ryu et al., 2000 R1100A JC, TM14 GMF ↔ Ryu et al., 2000 P1158A IC, JM, TM15 LTC4 ↓↓ Letourneau et al., 2007 E2-17βG ↔ MTX ↔ Table 1. continued on next page Mutant Predicted location Substrate Activity changes Reference I1173F DJ IC, TM15-16 LTC4 No act Keitel et al., 2003 E2-17βG No act R1210A EC, JC, TM16 GMF ↓↓ Ryu et al., 2000 R1230A TM16 GMF ↔ R1257A JC, TM17 GMF ↓↓ W1254A JC, TM17 E2-17βG ↓↓ Ito et al., 2001a W1254C ↓↓ W1254F ↔ W1254Y ↔ W1254A JC, TM17 LTC4 ↓↓ Ito et al., 2001b W1254C ↓↓↓ W1254F ↓↓ W1254Y ↓↓ W1254A JC, TM17 MTX ↓↓ Ito et al., 2001a W1254C ↓↓ W1254F ↓↓ W1254Y ↓↓↓ A1450T NBD2 E2-17βG ↓↓ Hirouchi et al., 2004 LTC4 ↓↓ DNP-SG ↓↓ Rat Mrp2 K308M IC, JM, TM6 TLC-S ↔ Ito et al., 2001b DNP-G ↑ LTC4 ↓ E3040G ↔ K320M TM6 TLC-S ↑ DNP-G ↑ LTC4 ↓ E3040G ↑ K325M TM6 TLC-S ↓* DNP-G ↓↓↓* LTC4 ↓↓↓* E3040G ↓ D329N TM6 TLC-S ↔ DNP-G ↓ LTC4 ↓↓↓* E3040G ↓ R586L TM11 TLC-S ↓ DNP-G ↓↓* LTC4 ↓↓* E3040G ↔ R1019M IC, JM, TM13 TLC-S ↔ DNP-G ↑* LTC4 ↔ E3040G ↔ R1096L TM14 TLC-S ↑ DNP-G ↑ LTC4 ↔ E3040G ↔ EC, extracellular; IC, intracellular; JC, near the cytosol in the membrane; JM, juxtamembrane; TLC-S, tauro-litocholate-sulfate; GMF, glutathione- methyl-fluorescein; ↑, activity over control>1.2; ↔, 1.2>activity over control>0.8; ↓, 0.8>activity over control>0.5; ↓↓, 0.5>activity over control>0.1; ↓↓↓, 0.1>activity over control.
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ABCC2 p.Lys324Ala 20082599:97:173
status: NEW
PMID: 12130697
[PubMed]
Gerk PM et al: "Regulation of expression of the multidrug resistance-associated protein 2 (MRP2) and its role in drug disposition."
No.
Sentence
Comment
49
Thirteen basic residues (His, Arg, Lys) in these regions were substituted with alanine; four mutants (K324A in TM6, K483A in TM9, R1210A in TM16 and R1257A in TM17) were all delivered appropriately to the cell surface when expressed in COS-7 cells yet showed decreased efflux of the substrate (Ryu et al., 2000).
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ABCC2 p.Lys324Ala 12130697:49:102
status: NEW
PMID: 10978330
[PubMed]
Ryu S et al: "Identification of basic residues involved in drug export function of human multidrug resistance-associated protein 2."
No.
Sentence
Comment
3
Four mutants, K324A (TM6), K483A (TM9), R1210A (TM16), and R1257A (TM17), showed decreased transport activity, and another mutant, K578A (TM11), showed decreased protein expression.
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ABCC2 p.Lys324Ala 10978330:3:14
status: NEW42 Site-directed Mutagenesis-The seven mutants of MRP2, K316A, K324A, K329A, H439A, K483A, K578A, and R590A, were generated by the overlapping polymerase chain reaction method.
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ABCC2 p.Lys324Ala 10978330:42:60
status: NEW117 In K324A and K483A mutants, the excretion of GS-MF decreased about 40% compared with MRP2V.
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ABCC2 p.Lys324Ala 10978330:117:3
status: NEW163 In K324A and K483A mutants, GS-MF excretion also moderately decreased (Fig. 8).
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ABCC2 p.Lys324Ala 10978330:163:3
status: NEW