Looking-glass synergistic pharmacological chaperones: DGJ and L-DGJ from the enantiomers of tagatose |
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| Authors: | Jenkinson Sarah F Fleet George W J Nash Robert J Koike Yuriko Adachi Isao Yoshihara Akihide Morimoto Kenji Izumori Ken Kato Atsushi |
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| Affiliation: | Chemistry Research Laboratory, Department of Chemistry, University of Oxford, Mansfield Road, OX1 3TA, United Kingdom. |
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| 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. |
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