Looking-glass synergistic pharmacological chaperones: DGJ and L-DGJ from the enantiomers of tagatose

Sarah F. Jenkinson; George W.J. Fleet; Robert J. Nash; Yuriko Koike; Isao Adachi; Akihide Yoshihara; Kenji Morimoto; Ken Izumori; Atsushi Kato

doi:10.1021/ol201552q

Looking-glass synergistic pharmacological chaperones: DGJ and L-DGJ from the enantiomers of tagatose

Sarah F. Jenkinson, George W.J. Fleet^*, Robert J. Nash, Yuriko Koike, Isao Adachi, Akihide Yoshihara, Kenji Morimoto, Ken Izumori, Atsushi Kato

^*この論文の責任著者

薬剤部

研究成果: ジャーナルへの寄稿 › 学術論文 › 査読

56 被引用数 (Scopus)

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The enantiomers of tagatose are converted to l-DGJ [a noncompetitive inhibitor of human lysosome α-galactosidase A (α-Gal A), K _i 38.5 μM] and DGJ [a competitive inhibitor of α-Gal A, K _i 15.1 nM] in 66% yield. l-DGJ and DGJ provide the first examples of pharmacological chaperones that (a) are enantiomeric iminosugars and (b) have synergistic activity with implications for the treatment of lysosomal storage disorders and other protein deficiencies.

本文言語	英語
ページ（範囲）	4064-4067
ページ数	4
ジャーナル	Organic Letters
巻	13
号	15
DOI	https://doi.org/10.1021/ol201552q
出版ステータス	出版済み - 2011/08/05

ASJC Scopus 主題領域

生化学
物理化学および理論化学
有機化学

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10.1021/ol201552q

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title = "Looking-glass synergistic pharmacological chaperones: DGJ and L-DGJ from the enantiomers of tagatose",

abstract = "The enantiomers of tagatose are converted to l-DGJ [a noncompetitive inhibitor of human lysosome α-galactosidase A (α-Gal A), K i 38.5 μM] and DGJ [a competitive inhibitor of α-Gal A, K i 15.1 nM] in 66% yield. l-DGJ and DGJ provide the first examples of pharmacological chaperones that (a) are enantiomeric iminosugars and (b) have synergistic activity with implications for the treatment of lysosomal storage disorders and other protein deficiencies.",

author = "Jenkinson, {Sarah F.} and Fleet, {George W.J.} and Nash, {Robert J.} and Yuriko Koike and Isao Adachi and Akihide Yoshihara and Kenji Morimoto and Ken Izumori and Atsushi Kato",

year = "2011",

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doi = "10.1021/ol201552q",

language = "英語",

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T1 - Looking-glass synergistic pharmacological chaperones

T2 - DGJ and L-DGJ from the enantiomers of tagatose

AU - Jenkinson, Sarah F.

AU - Fleet, George W.J.

AU - Nash, Robert J.

AU - Koike, Yuriko

AU - Adachi, Isao

AU - Yoshihara, Akihide

AU - Morimoto, Kenji

AU - Izumori, Ken

AU - Kato, Atsushi

PY - 2011/8/5

Y1 - 2011/8/5

N2 - The enantiomers of tagatose are converted to l-DGJ [a noncompetitive inhibitor of human lysosome α-galactosidase A (α-Gal A), K i 38.5 μM] and DGJ [a competitive inhibitor of α-Gal A, K i 15.1 nM] in 66% yield. l-DGJ and DGJ provide the first examples of pharmacological chaperones that (a) are enantiomeric iminosugars and (b) have synergistic activity with implications for the treatment of lysosomal storage disorders and other protein deficiencies.

AB - The enantiomers of tagatose are converted to l-DGJ [a noncompetitive inhibitor of human lysosome α-galactosidase A (α-Gal A), K i 38.5 μM] and DGJ [a competitive inhibitor of α-Gal A, K i 15.1 nM] in 66% yield. l-DGJ and DGJ provide the first examples of pharmacological chaperones that (a) are enantiomeric iminosugars and (b) have synergistic activity with implications for the treatment of lysosomal storage disorders and other protein deficiencies.

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U2 - 10.1021/ol201552q

DO - 10.1021/ol201552q

M3 - 学術論文

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AN - SCOPUS:79961042765

SN - 1523-7060

VL - 13

SP - 4064

EP - 4067

JO - Organic Letters

JF - Organic Letters

IS - 15

ER -

Looking-glass synergistic pharmacological chaperones: DGJ and L-DGJ from the enantiomers of tagatose

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