Abstract: Disclosed herein are, inter alia, compounds modulating MT1 and MT2 receptors' activity and methods of use thereof for treating MT1 and MT2 receptor-related conditions.

Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Abstract: The present application provides a colloid drug aggregate composition and methods of use and manufacture thereof. While the formation of colloidal aggregates leads to artifacts in early drug discovery, their composition makes them attractive as nanoparticle formulations for targeted drug delivery. The present application provides an acid-responsive composition comprising: a colloidal aggregate of one or more drugs and a stabilizing agent, wherein the colloidal aggregate disrupts, dissolves or disassembles when the acid-responsive composition is in an acid environment having a pH of less than 7.4. The colloidal aggregate of the composition will disassemble upon contact with acid or upon introduction to an acidic environment, such as is found in the endosomes of cells. This approach makes this composition an attractive vehicle for drug delivery to a target site in a subject or to cells.

Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Abstract: Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Abstract: Compounds and salts thereof which inhibit microbial growth or attenuate the virulence of pathogenic microorganisms and which inhibit UDP-galactopyranose mutase (UGM). Compounds of the invention include triazolothiadiazines, particularly 3, 6, 7-substituted-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, and 4-(1H-pyrrol-3-yl) thiazoles, particularly 4-(1,2,5-substituted-1H-pyrrol-3-yl)-2-substituted thiazoles, and salts thereof. Methods for inhibiting growth or attenuating virulence of microbial pathogens including mycobacterium, for example, M. tuberculosis and M. smegmatis and Klebsiella, for example, Klebsiella pneumoniae. Methods for inhibiting eukaryotic human and animal pathogens, and fungi and nematodes in particular. Methods for treatment of infections by prokaryotic and eukaryotic pathogens employing compounds of the invention.

Abstract: Compounds and salts thereof which inhibit microbial growth or attenuate the virulence of pathogenic microorganisms and which inhibit UDP-galactopyranose mutase (UGM). Compounds of the invention include triazolothiadiazines, particularly 3, 6, 7-substituted-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, and 4-(1H-pyrrol-3-yl) thiazoles, particularly 4-(1,2,5-substituted-1H-pyrrol-3-yl)-2-substituted thiazoles, and salts thereof. Methods for inhibiting growth or attenuating virulence of microbial pathogens including mycobacterium, for example, M. tuberculosis and M. smegmatis and Klebsiella, for example, Klebsiella pneumoniae. Methods for inhibiting eukaryotic human and animal pathogens, and fungi and nematodes in particular. Methods for treatment of infections by prokaryotic and eukaryotic pathogens employing compounds of the invention.

Abstract: Compounds and salts thereof which inhibit microbial growth or attenuate the virulence of pathogenic microorganisms and which inhibit UDP-galactopyranose mutase (UGM). Compounds of the invention include triazolothiadiazines, particularly 3,6,7-substituted-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, and 4-(1H-pyrrol-3-yl) thiazoles, particularly 4-(1,2,5-substituted-1H-pyrrol-3-yl)-2-substituted thiazoles, and salts thereof. Methods for inhibiting growth or attenuating virulence of microbial pathogens including mycobacterium, for example, M. tuberculosis and M. smegmatis and Klebsiella, for example, Klebsiella pneumoniae. Methods for inhibiting eukaryotic human and animal pathogens, and fungi and nematodes in particular. Methods for treatment of infections by prokaryotic and eukaryotic pathogens employing compounds of the invention.

Abstract: Disclosed herein inter alia are Boron containing compounds and methods for treating infections related to antibiotic resistant microorganisms.

Abstract: Compounds and salts thereof which inhibit microbial growth or attenuate the virulence of pathogenic microorganisms and which inhibit UDP-galactopyranose mutase (UGM). Compounds of the invention include triazolothiadiazines, particularly 3,6,7 -substituted-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, and 4-(1H-pyrrol-3-yl) thiazoles, particularly 4-(1,2,5-substituted-1H-pyrrol-3-yl)-2-substituted thiazoles, and salts thereof. Methods for inhibiting growth or attenuating virulence of microbial pathogens including mycobacterium, for example, M. tuberculosis and M. smegmatis and Klebsiella, for example, Klebsiella pneumoniae. Methods for inhibiting eukaryotic human and animal pathogens, and fungi and nematodes in particular. Methods for treatment of infections by prokaryotic and eukaryotic pathogens employing compounds of the invention.

Abstract: Disclosed herein inter alia are Boron containing compounds and methods for treating infections related to antibiotic resistant microorganisms.

Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.

Abstract: ?-lactamases are the most widespread resistance mechanism to ?-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also ?-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.

Abstract: ?-lactamases are the most widespread resistance mechanism to ?-lactam antibiotics, such as penicillins and cephalosporins. In response to these enzymes, inhibitors have been introduced. Unfortunately, these inhibitors are also ?-lactams, and resistance to them has developed rapidly. Consequently, the present invention provides a novel structure-based approach to inhibitors of these enzymes.

Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.

Abstract: The present invention provides methods of identifying compounds that non-specifically inhibit biological reactions. The present invention further includes kits that facilitate this identification. In addition, complications of compounds for use in high throughput drug screening that have been evaluated by the disclosed methodology are also part of the present invention. Further, the invention provides methods for identifying a false positive compound previously identified as positive in a screening assay by measuring the activity of at least one biological activity in the presence and absence of a small molecule compound capable of inhibiting aggregate formation, e.g., digitonin.