Abstract: Provided herein are O-GlcNAc transferase (OGT) inhibitor compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., diabetes and complications thereof, neurodegenerative diseases, proliferative diseases such as cancers, autoimmune diseases, and inflammatory diseases) in a subject. Provided are methods of inhibiting OGT in a subject or biological sample.

Abstract: The present invention provides moenomycin-based probe compounds of Formula (I) for use in screening inhibitors of bacterial glycosyltransferases. The present invention also provides bacterial glycosyltransferase screening assays using compounds of Formula (I).

Abstract: Described herein are compounds of Formula (I?), Formula (IA), Formulae (I)-(VII), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The invention also provides pharmaceutical compositions of the compounds for human and veterinary use. Compounds of the present invention are useful for inhibiting bacterial growth and therefore are useful in treating and/or preventing bacterial infections. Methods of using the compounds for treating and/or preventing a bacterial infection in a subject are also described.

Abstract: The present invention provides methods of synthesizing moenomycin analogs of Formula (I). The present invention also provides compositions comprising a compound of Formula (I) and kits for synthesizing compounds of Formula (I).

Abstract: The present invention provides inhibitors of O-GlcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, metabolic diseases, neurodegenerative diseases, proliferative diseases (e.g., cancers), autoimmune diseases, and inflammatory diseases.

Abstract: The methods and compositions described herein relate to the identification, isolation, and characterization of genes which encode proteins useful for the biosynthesis of transglycosylase inhibitors such as moes. The methods and compositions also relate to the production of such proteins, and their use in the synthesis of moes, the expression of moes, and the production of modified moes.

Abstract: The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions.

Abstract: The present invention provides compounds of Formula (I): or a pharmaceutically acceptable form thereof; wherein R1, R2, R3, R 6, R7, R12, RXX, Ra, and Rb are as defined herein, and G is a group of Formula (a), (b), or (c): wherein X1, X2, X3, X4, X5, X6, X7, Y, Rc, Rd, Rz, a, d, e, x, n, and m are as defined herein. The present invention further provides pharmaceutical compositions comprising a compound of Formula (I), kits comprising such compositions, methods of use and treatment, and preparative methods.

Abstract: The present invention provides compounds of Formula (I); or a pharmaceutically acceptable form thereof; wherein R1,R2,R3,R6,R7,R12,Ra, and Rb are as defined herein, and G is a group of Formula (a), (b), or (c): Formula (II), wherein X1; X2, X3, X4, X5, X6, X7, Y, RC, Rd, Rz, a, d, e, x, n, and m are as defined herein. The present invention further provides pharmaceutical compositions comprising a compound of Formula (I), kits comprising such compositions, methods of use and treatment, and preparative methods.

Abstract: The methods and compositions described herein relate to the identification, isolation, and characterization of genes which encode proteins useful for the biosynthesis of transglycosylase inhibitors such as moes. The methods and compositions also relate to the production of such proteins, and their use in the synthesis of moes, the expression of moes, and the production of modified moes.

Abstract: The present invention provides novel moenomycin analogs as well as pharmaceutical compositions thereof, methods of synthesis, and methods of use in treating an infection by administering an inventive compound to a subject in need thereof. The moenomycin analogs may be prepared synthetically, biosynthetically, or semi-synthetically. The analogs are particularly useful in treating or preventing infections caused by Gram-positive organisms. Certain inventive compounds may have a broader spectrum of coverage, which includes Gram-negative organisms.

Abstract: The present invention provides compounds of Formula (I); or a pharmaceutically acceptable form thereof; wherein R1,R2,R3,R6,R7,R12,Ra, and Rb are as defined herein, and G is a group of Formula (a), (b), or (c): Formula (II), wherein X1; X2, X3, X4, X5, X6, X7, Y, RC, Rd, Rz, a, d, e, x, n, and m are as defined herein. The present invention further provides pharmaceutical compositions comprising a compound of Formula (I), kits comprising such compositions, methods of use and treatment, and preparative methods.

Abstract: The present invention provides methods of synthesizing moenomycin analogs of Formula (I). The present invention also provides compositions comprising a compound of Formula (I) and kits for synthesizing compounds of Formula (I).

Abstract: The invention relates to methods and products for modulating glycosylation of proteins. The invention is useful for identifying therapeutic compounds to treat glycosylation-associated disorders such as neurodegeneration, diabetes, including complications of diabetes such as insulin resistance, nephropathy, microvascular damage, and endothelial dysfunction. The invention is also useful for identifying therapeutic compounds to treat de-glycosylation-associated disorders such as ischemic damage and traumatic injury. The invention also relates in part to assays that are useful for identifying and testing candidate compounds for modulating glycosylation of proteins and also relates in part to compounds to treat glycosylation-associated diseases and disorders.

Abstract: The present invention provides moenomycin-based probe compounds of Formula (I) for use in screening inhibitors of bacterial glycosyltransferases. The present invention also provides bacterial glycosyltransferase screening assays using compounds of Formula (I).

Abstract: The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases.

Abstract: The invention relates to methods and products for modulating glycosylation of proteins. The invention is useful for identifying therapeutic compounds to treat glycosylation-associated disorders such as neurodegeneration, diabetes, including complications of diabetes such as insulin resistance, nephropathy, microvascular damage, and endothelial dysfunction. The invention is also useful for identifying therapeutic compounds to treat de-glycosylation-associated disorders such as ischemic damage and traumatic injury. The invention also relates in part to assays that are useful for identifying and testing candidate compounds for modulating glycosylation of proteins and also relates in part to compounds to treat glycosylation-associated diseases and disorders.

Abstract: The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions.

Abstract: The present invention provides novel moenomycin analogs as well as pharmaceutical compositions thereof, methods of synthesis, and methods of use in treating an infection by administering an inventive compound to a subject in need thereof. The moenomycin analogs may be prepared synthetically, biosynthetically, or semi-synthetically. The analogs are particularly useful in treating or preventing infections caused by Gram-positive organisms. Certain inventive compounds may have a broader spectrum of coverage, which includes Gram-negative organisms.

Abstract: The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant Staphylococcus aureus (MRSA). The invention further provides procedures for the syntheses of Wall Teichoic Acid biosynthesis inhibitors. The invention also provides methods for the identification of antibacterial therapeutic agents.