Abstract: The invention relates to FMS-like tyrosine kinase (FLT3), FLT3 binding pockets or FLT3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to FMS-like tyrosine kinase protein, complexes of FMS-like tyrosine kinase protein, homologues thereof, or FLT-3-like protein or protein complexes. The invention also relates to crystallizable compositions and crystals comprising an FMS-like tyrosine kinase cytoplasmic domain or homologues thereof. The invention also relates to methods of identifying inhibitors of the cytoplasmic domain of FMS-like tyrosine kinase protein.

Abstract: The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein R1 is NH2; R2 is NH2; R3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, and alkylamino; and R4 and R4? are each independently hydrogen or a substituted or unsubstituted, linear, branched, or cyclic, alkyl, alkenyl, alkynyl, aryl, acyl, aralkyl, or alkaryl group wherein one or more carbon or hydrogen atoms may be substituted by a substituent selected from amino, alkylamino, hydroxyl, alkoxyl, thio, halogen, nitro, and carbonyl; wherein NR4R4? incorporates a substituted or unsubstituted naphthyl group, wherein the substituents are selected from alkoxy, halogen, alkyl, and alkylene, and wherein said naphthyl group in NR4R4? is bonded to N through a substituted or unsubstituted alkylene moiety. These compounds have antibacterial properties based on their ability to bind and inhibit D-Ala-D-Ala ligase, a critical pathway enzyme in bacterial cell-wall synthesis, and are suitable for various antibacterial uses.

Abstract: The invention is based on the discovery of a new class of heterocyclic compounds having, for example, antibacterial properties. The D-Ala-D-Ala ligase enzyme is a critical pathway enzyme in the bacterial cell-wall synthesis. The compounds can bind to and inhibit the enzyme D-Ala-D-Ala ligase. The new compounds' activity combined with their ability to cross bacterial cell membranes makes them suitable for use as antibacterial drugs or other antibacterial applications.

Abstract: This invention relates to novel heterocyclic compounds and to their use in the medical treatment or prophylaxis of bacterial infections, or their use as antiseptics, sterilizants, or disinfectants.

Abstract: The invention is based on the discovery that certain small molecules can bind to the ATP binding site of D-Ala-D-Ala ligase, even in the absence of the enzyme's substrate, and can cause a conformational change in the enzyme structure similar to that which occurs upon binding of ATP and substrate to the enzyme. Without wishing to be bound by any theory, it is believed that such a conformational change is required for either activation or inhibition of the enzyme. The information obtained from this discovery has enabled identification of key interactions in the active site of the enzyme, as well as the design and opimization of inhibitors.

Abstract: An electronic database for identification of enzyme substrate and enzyme inhibitor structures that are structurally similar to a submitted chemical structure is provided. The enzyme substrate and enzyme inhibitor structures can be linked by numerous parameters, such as by Enzyme Classification Number. The database can be used to identify potential therapeutics for newly discovered enzymes or enzyme families.

Abstract: The present invention relates to the use of transferrin in controlling insulin levels. Transferrin can disrupt insulin:receptor interactions in mammalian cells, may be used in mammals to treat hypoglycemia, may also be used to inhibit production of insulin by mammalian cells, and can decrease the serum insulin levels in a mammal. The invention further provides methods for identifying compounds which modulate the effect of transferrin on insulin signal transduction. Pharmaceutical compositions containing transferrin are also disclosed.

Abstract: The present invention relates to the use of transferrin in controlling insulin levels. Transferrin can disrupt insulin:receptor interactions in mammalian cells, may be used in mammals to treat hypoglycemia, may also be used to inhibit production of insulin by mammalian cells, and can decrease the serum insulin levels in a mammal. The invention further provides methods for identifying compounds which modulate the effect of transferrin on insulin signal transduction. Pharmaceutical compositions containing transferrin are also disclosed.