ABCB1 p.Asn839Ile

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PMID: 12223492 [PubMed] Loo TW et al: "Location of the rhodamine-binding site in the human multidrug resistance P-glycoprotein."
No. Sentence Comment
186 Mutations in TM9 (I837L and N839I) or in TM6 (G388A and A339P) resulted in similar drug resistance profiles with four structurally different drugs (increased resistance to vincristine or actinomycin D but decreased resistance to colchicine or daunorubicin relative to wild-type P-gp).
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ABCB1 p.Asn839Ile 12223492:186:28
status: NEW
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PMID: 16545467 [PubMed] Shilling RA et al: "New light on multidrug binding by an ATP-binding-cassette transporter."
No. Sentence Comment
58 Although mutation of only one of these residues (L975A, V981A and F983A) has no effect on the phenotype of the protein [20], double mutations either completely inhibit (V981A/F983A and L975A/V981A) or cause 50% inhibition (L975A/F983A) of Table 1.
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ABCB1 p.Asn839Ile 16545467:58:696
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59 Published mutations in human and murine P-glycoprotein that alter drug transport in cells Location of mutation Mutation Refs Mutation Refs Mutation Refs Transmembrane helices H61A and others [14] I214L [60] L868W [59] G64R [15] P223A [65] I936A [21] L65R [15] S224P [60] F938A [21] Q139[H/P/R] [60] I306R [18] S939[A/C/T/Y/W/D/F] [21,22] G141V [17] F335A [16] T941A [21] G185V [61,62] V338A [66] Q942A [21] I186N [61] G338A [67,68] A943G [21] G187V [17] A339P [67,68] Y946A [21] G187E [60] G341A [66] S948A [21] A192T [60] S344[A/T/C/Y] [66] Y949A [21] F200L [60] N350I [19] C952A [21] F204S [60] P709A [65] F953A [21] R206L [60] G830V [17] L975A [20] W208G [60] I837L [23] F978A [16] K209E [60] N839I [23] V981A [20] L210I [60] I862F [19] F983A [20] T211P [60] L865F [19] F978A [16] V213A [60] P866A [65] N988D [59] Intracellular domain T169I [60] K177I [60] G288V [17] R170L [60] E180G [60] A931T [19] L171P [60] G181R [60] F934A [21] T172P [60] G183D [60] G935A [21] S176P [60] D184N [60] NBD D555N [63] K1076M [69] E1197Q [64] D558N [64] D1093N [64] D1203N [64] D592N [64] E1125Q [64] D1237N [64] E604Q [64] S1173A [70] E1249Q [64] Review TRENDS in Pharmacological Sciences Vol.27 No.
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ABCB1 p.Asn839Ile 16545467:59:696
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67 Hotspot IIB Change-in-specificity mutations also occur as a result of spontaneous mutations (I837L and N839I) in TMH9 [23].
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ABCB1 p.Asn839Ile 16545467:67:103
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65 Hotspot IIB Change-in-specificity mutations also occur as a result of spontaneous mutations (I837L and N839I) in TMH9 [23].
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ABCB1 p.Asn839Ile 16545467:65:103
status: NEW
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