ABCB1 p.His61Arg
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PMID: 10331089
[PubMed]
Ambudkar SV et al: "Biochemical, cellular, and pharmacological aspects of the multidrug transporter."
No.
Sentence
Comment
47
Table 1 List of mutations in human, mouse, and hamster P-glycoproteins that affect substrate specificitya aa mutation Region Sourceb Reference H61R, F, K, M, W, Y TM 1 Human MDR1 149, 150 ABC20c G64R TM 1 Human MDR1 150 L65R TM 1 Human MDR1 150 aa78-97 EC 1 Human MDR1 151 Q128Hd TM 2 Mouse mdr3 152 R138H IC 1 Mouse mdr3 152 Q139H, R IC 1 Mouse mdr3 152 Q141V IC 1 Human MDR1 15319, Q145H IC 1 Mouse mdr3 152 E155G, K IC 1 Mouse mdr3 152 F159I IC 1 Mouse mdr3 152 D174G IC 1 Mouse mdr3 152 S176G, P IC 1 Mouse mdr3 152 K177I IC 1 Mouse mdr3 152 N179S IC 1 Mouse mdr3 152 N183S/G185V IC 1 Human MDR1 154 G183D IC 1 Mouse mdr3 152 G185V IC 1 Human MDR1 155-157 G187V IC 1 Human MDR1 153 A192T TM 3 Mouse mdr3 152 F204S EC 2 Mouse mdr3 152 W208G EC 2 Mouse mdr3 152 K209E EC 2 Mouse mdr3 152 L210I TM 4 Mouse mdr3 152 T211P TM 4 Mouse mdr3 152 I214T TM 4 Mouse mdr3 152 P223A TM 4 Human MDR1 158 G288V IC 2 Human MDR1 153 I299M, T319S, L322I, TM 5, EC3, Human MDR1 159 G324K, S351N IC 3 F335A TM 6 Human MDR1 19 F335 TM 6 Human MDR1 160 V338A TM 6 Human MDR1 161 G338A, A339P TM 6 Hamster PGY1 162, 163 A339P TM 6 Hamster PGY1 163 G341V TM 6 Human MDR1 161 K536R, Q N-NBD Human MDR1 164 ERGA → DKGT N-NBD Mouse mdr3 165 aa 522-525 T578C N-NBD Mouse mdr3 165 (Continued) G830V IC 4 Human MDR1 P866A TM 10 Human MDR1 158 F934A TM 11 Mouse mdr3 166 G935A TM 11 Mouse mdr3 166 I936A TM 11 Mouse mdr3 166 F938A TM 11 Mouse mdr3 166 S939A TM 11 Mouse mdr3 166 S939F TM 11 Mouse mdr3 167, 168 S941F TM 11 Mouse mdr1 167, 168 T941A TM 11 Mouse mdr3 166 Q942A TM 11 Mouse mdr3 166 A943G TM 11 Mouse mdr3 166 Y946A TM 11 Mouse mdr3 166 S948A TM 11 Mouse mdr3 166 Y949A TM 11 Mouse mdr3 166 C952A TM 11 Mouse mdr3 166 F953A TM 11 Mouse mdr3 166 F983A TM 12 Human MDR1 169 L975A, V981A, F983A TM 12 Human MDR1 169 M986A, V988A, Q990A, TM 12 Human MDR1 169 V991A V981A, F983A TM 12 Human MDR1 169 L975A, F983A TM 12 Human MDR1 169 L975A, V981A TM 12 Human MDR1 169 F978A TM 12 Human MDR1 19 a aa,amino acid; EC, extracellular loop; IC, intracellular loop; TM,transmembrane domain; NBD, nucleotide binding/utilization domain.
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ABCB1 p.His61Arg 10331089:47:143
status: NEW
PMID: 9220975
[PubMed]
Taguchi Y et al: "Alteration of substrate specificity by mutations at the His61 position in predicted transmembrane domain 1 of human MDR1/P-glycoprotein."
No.
Sentence
Comment
92
The replacement of His61 by Lys or Arg, which have a bulkier and basic side chain, reduced resistance to Vbl and Adr and increased resistance to Col and VP16, resulting in a resistance order of Col > VP16 ≈ Vbl > Adr.
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ABCB1 p.His61Arg 9220975:92:19
status: NEW136 The ability to confer resistance to Adr of mutant P-glycoproteins showed a characteristic dependence on the nature of the amino acids: although cells expressing mutants in which His61 was replaced by amino acids with side chains larger than His showed higher (more than 2-fold than that of the wild-type) resistance to Adr, cells expressing mutants in which His61 was replaced by Lys or Arg showed markedly lower resistance to Adr.
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ABCB1 p.His61Arg 9220975:136:358
status: NEW
PMID: 16545467
[PubMed]
Shilling RA et al: "New light on multidrug binding by an ATP-binding-cassette transporter."
No.
Sentence
Comment
48
The only exception is the introduction of a positively charged residue at position 61 (H61R), which decreases resistance to daunomycin.
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ABCB1 p.His61Arg 16545467:48:87
status: NEW47 The only exception is the introduction of a positively charged residue at position 61 (H61R), which decreases resistance to daunomycin.
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ABCB1 p.His61Arg 16545467:47:87
status: NEW
PMID: 9287132
[PubMed]
Taguchi Y et al: "Amino acid substitutions in the first transmembrane domain (TM1) of P-glycoprotein that alter substrate specificity."
No.
Sentence
Comment
50
In the previous study, we showed that the replacements of His61 by Arg changed the substrate specificity of P-glycoprotein drastically [13].
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ABCB1 p.His61Arg 9287132:50:58
status: NEW55 From cells transfected with the wild type and He60 -> Arg, His61 -> Arg, Ala63 -> Arg, Gly64 -> Arg, or Leu65 -> Arg mutant cDNA, both Vbl- and Col-resistant colonies were obtained (Fig. 1).
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ABCB1 p.His61Arg 9287132:55:59
status: NEW57 In contrast, cells transfected with mutants His61 -> Arg slightly more resistant colonies in the presence of Col than in the presence of Vbl.
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ABCB1 p.His61Arg 9287132:57:44
status: NEW
PMID: 22232552
[PubMed]
Iram SH et al: "Mutation of Glu521 or Glu535 in cytoplasmic loop 5 causes differential misfolding in multiple domains of multidrug and organic anion transporter MRP1 (ABCC1)."
No.
Sentence
Comment
261
Thus, the P-glycoprotein processing mutant G251V/T55R is not rescued by any drug substrates, whereas another mutant G251V/H61R can be rescued by only a single substrate (cyclosporine A) (39).
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ABCB1 p.His61Arg 22232552:261:122
status: NEW