Methods and Compositions for Modulating Glycosylation
First Claim
Patent Images
1. An isolated compound set forth as compound 4, or a derivative, analog, or variant thereof;
- compound 5, or a derivative, analog, or variant thereof;
compound 6, or a derivative, analog, or variant thereof;
compound 7, or a derivative, analog, or variant thereof;
compound 8, or a derivative, analog, or variant thereof;
compound 9, or a derivative, analog, or variant thereof;
compound 10, or a derivative, analog, or variant thereof;
compound 11, or a derivative, analog, or variant thereof;
compound 12, or a derivative, analog, or variant thereof;
compound 13, or a derivative, analog, or variant thereof;
or compound 14, or a derivative, analog, or variant thereof.
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Accused Products
Abstract
The invention relates to methods and products for modulating glycosylation of proteins. The invention is useful for treating glycosylation-associated disorders such as neurodegeneration, diabetes, including complications of diabetes such as insulin resistance, nephropathy, microvascular damage, and endothelial dysfunction. The invention also relates in part to assays that are useful for identifying and testing candidate compounds for modulating glycosylation of proteins.
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Citations
59 Claims
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1. An isolated compound set forth as compound 4, or a derivative, analog, or variant thereof;
- compound 5, or a derivative, analog, or variant thereof;
compound 6, or a derivative, analog, or variant thereof;
compound 7, or a derivative, analog, or variant thereof;
compound 8, or a derivative, analog, or variant thereof;
compound 9, or a derivative, analog, or variant thereof;
compound 10, or a derivative, analog, or variant thereof;
compound 11, or a derivative, analog, or variant thereof;
compound 12, or a derivative, analog, or variant thereof;
compound 13, or a derivative, analog, or variant thereof;
or compound 14, or a derivative, analog, or variant thereof. - View Dependent Claims (2)
- compound 5, or a derivative, analog, or variant thereof;
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3. (canceled)
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4. A method for treating an OGT-associated disease or condition in a subject, comprising:
administering to a subject in need of such treatment an effective amount of an OGT-inhibiting compound to treat the OGT-associated disease or condition. - View Dependent Claims (5, 16, 17, 18, 19, 20, 21)
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6-15. -15. (canceled)
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22. A method of evaluating the effect of a candidate compound on OGT activity, comprising:
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contacting OGT bound to a probe with a candidate compound and determining the displacement of the probe from the OGT, wherein the displacement of the probe from the OGT indicates that the candidate compound inhibits OGT activity. - View Dependent Claims (23, 24)
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25-41. -41. (canceled)
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42. A method for inhibiting OGT activity in a cell or tissue, comprising:
- contacting the cell or tissue with an effective amount of an OGT-inhibiting compound to inhibit OGT activity in the cell, or tissue.
- View Dependent Claims (43, 54)
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44-53. -53. (canceled)
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55. An isolated nucleic acid molecule comprising the nucleotide sequence set forth as SEQ ID NO:
- 1.
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56. An isolated protein encoded by the nucleotide sequence set forth as SEQ ID NO:
- 1.
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57. An isolated polypeptide comprising the amino acid sequence set forth as SEQ ID NO:
- 2.
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58. A method for confirming the effect of a candidate compound as an inhibitor of OGT activity, the method comprising,
(a) contacting a sample containing the candidate compound with (i) an OGT substrate polypeptide, (ii) a UDP-GlcNAc probe comprising detectably labeled GlcNAc, and (iii) OGT; - and
(b) determining the amount of transfer of the labeled GlcNAc to the OGT substrate polypeptide in the sample, wherein a lower amount of GlcNAc transferred to the OGT substrate in the sample compared to a control amount of GlcNAc transfer to the OGT substrate confirms the effect of the candidate compound as an inhibitor of OGT activity.
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59-68. -68. (canceled)
Specification