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Mutants of Rhizobium trifolii strain 7012 defective in C(4)-dicarboxylate transport were isolated by using a selective procedure based on pH indicator media. The mutant strains CR7098 and CR7099 failed to grow on or transport succinate, fumarate, or malate, but grew at wild-type rates on several other carbon sources. The C(4)-dicarboxylate transport system(More)
4-Thiazolidinones were synthesized and evaluated for their ability to inhibit the bacterial enzyme MurB. Selected 4-thiazolidinones displayed activity against the enzyme in vitro. This activity, coupled with the design principles of the thiazolidinones, supports the postulate that 4-thiazolidinones may be recognized as diphosphate mimics by a biological(More)
We have used the Sydney University Stellar Interferometer (SUSI) to measure the angular diameter of β Hydri. This star is a nearby G2 subgiant whose mean density was recently measured with high precision using asteroseismology. We determine the radius and effective temperature of the star to be 1.814 ± 0.017 R ⊙ (0.9%) and 5872 ± 44 K (0.7%) respectively.(More)
The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats. These findings, combined with a favorable ADME profile, have prompted clinical evaluation of dapagliflozin for the treatment of type 2(More)
Efforts to further elucidate structure-activity relationships (SAR) within our previously disclosed series of beta-quaternary amino acid linked l-cis-4,5-methanoprolinenitrile dipeptidyl peptidase IV (DPP-IV) inhibitors led to the investigation of vinyl substitution at the beta-position of alpha-cycloalkyl-substituted glycines. Despite poor systemic(More)
Inhibition of sodium-dependent glucose transporter 2 (SGLT2), the transporter that is responsible for renal re-uptake of glucose, leads to glucosuria in animals. SGLT-mediated glucosuria provides a mechanism to shed excess plasma glucose to ameliorate diabetes-related hyperglycemia and associated complications. The current study demonstrates that the proper(More)
Low-temperature dehydration and embedding techniques have been used to preserve the transverse structure of corneal collagen fibrils for study using electron microscopy. The diameters of the fibrils, which were found to be about 45% larger than those determined previously for specimens prepared for electron microscopy using conventional dehydration and(More)
Enzymes offer unique opportunities for drug design that are not available to cell surface receptors, nuclear hormone receptors, ion channels, transporters, and DNA. Here, we review the variety of inhibition mechanisms for enzyme-targeted drugs, and establish an enzyme target database for drugs currently marketed in the United States. From an analysis of the(More)