Abstract: This invention contemplates improved methods of enzymatic production of carbohydrates especially fucosylated carbohydrates. Improved syntheses of glycosyl 1- or 2-phosphates using both chemical and enzymatic means are also contemplated. The phosphorylated glycosides are then used to produce sugar nucleotides that are in turn used as donor sugars for glycosylation of acceptor carbohydrates. Especially preferred herein is the use of a disclosed method for fucosylation.

Abstract: Compositions of purified biologically active Wnt proteins are provided. Wnt proteins are found to be hydrophobic and post-translationally modified by addition of a lipid moiety at a conserved cysteine residue. Methods for isolation of Wnt utilize detergents that maintain the solubility of the modified protein.

Abstract: The invention provides a composition for preventing or treating infectious diseases of a virus belonging to the Coronavirus family or Flavivirus family, the composition containing one or more substances selected from reduced glutathione or oxidized glutathione or pharmaceutically acceptable salts thereof and catechin, and a composition for preventing or treating infectious diseases of a virus belonging to the Coronavirus family or Flavivirus family, the composition containing reduced glutathione or oxidized glutathione or pharmaceutically acceptable salts thereof and catechin.

Abstract: A composition with a polypeptide including amino acid sequence LKKTET [SEQ ID NO:1] or a conservative variant thereof, the composition further including a carrier for application to a surface of a body.

Abstract: The present invention is directed to the improved synthesis of compounds of formula (I) an intermediate compound which is useful in the synthesis of the anticancer agents known as PSA conjugates.

Abstract: Thiol-linked polymeric prodrugs, methods of making and using the same are disclosed. The use of a sulfhydryl bond in combination with a benzyl elimination system results in the formation of prodrugs which can take advantage of plasma enzymes in vivo for regeneration of the parent molecule. A preferred prodrug in accordance with the invention is: where S-MP is 6-mercaptopurine.

Abstract: Inhibitors of bone calcium resorption are administered to allow high doses of vitamin D compounds or mimetics to be given with the intent of treating non-calcium related diseases such as cancer, psoriasis, and autoimmune disease without the dangers of calcification of kidney, heart, and aorta. Inhibitors of bone calcium resorption include the bis-phosphonates, OPG (osteoprotegerin) or the soluble RANKL (receptor activator of NF-?B ligand) receptor known as sRANK (soluble RANK which is the protein expressed by the NF-?B gene), and function to block the availability of calcium from bone thereby preventing hypercalcemia and the resulting calcification of soft tissues. Thus, high doses of 1?,25-dihydroxyvitamin D3 (1,25-(OH)2D3), its analogs, prodrugs, or mimetics can be utilized with minimal risk to a patient. Specifically, alendronate is shown to block the bone calcium mobilization activity of both 1,25-(OH)2D3 and its very potent analog, 2-methylene -19-nor-(20S)-1?,25-dihydroxyvitamin D3.

Abstract: Synthetic methods and compounds involving amino amides, peptides and peptidomimetics. Amino amide derivatives are prepared via the one-step three-component reaction of a glyoxamide, an amine, and an organoboron derivative. Conversion of the product to another glyoxamide intermediate allows the iterative use of this chemistry for the synthesis of peptides and peptidomimetics.

Abstract: The present invention discloses a method of treating an ophthalmic infection by administering to a vertebrate inflicted with the ophthalmic infection an ophthalmologically effective amount of an antimicrobial peptide which is derived from alpha-melanocyte-stimulating hormone (?-MSH) and biologically functional equivalents thereof. Specifically, the antimicrobial peptides derived from alpha-melanocyte-stimulating hormone (?-MSH) include ?-MSH (1–13) which is SYSMEHFRWGKPV, ?-MSH (4–10) which is MEHFRWG, ?-MSH (6–13) which is HFRWGKPV, ?-MSH (11–13) which is KPV, and a KPV dimer. The ophthalmic infection can be caused by a microorganism which include a bacteria, a fungi or a virus. The vertebrate includes a bird and a mammal. The antimicrobial peptide has anti-bacterial, antifungal, and antiviral property and therefore can be administered at the onset of the ophthalmic infection before the microorganism causing the infection is determined as well as thereafter.

Abstract: The present invention provides novel complexes consisting of certain GLP-1 molecules associated with a divalent metal cation that is capable of co-precipitating with a GLP-1 molecule. Pharmaceutical compositions and methods of using such complexes for enhancing the expression of insulin in B-type islet cells is claimed, as is a method for treating maturity onset diabetes mellitus in mammals, particularly humans.

Abstract: The present invention is directed to a prevention and treatment for dermatological disorders. One aspect of this invention involves a dermatological treatment comprising one or more polypeptides with an amino acid sequence including KPV (SEQ. ID. NO. 1), MEHFRWGKPV (SEQ. ID. NO. 2), HFRWGKPV (SEQ. ID. NO. 3), or SYSMEHFRWGKPV (SEQ. ID. NO. 4) for the treatment and prevention of dermatological disorders. The polypeptides are at a level to effectively treat the cutaneous inflammation and are carried by a carrier. The one or more polypeptides can also be a dimer formed from any of the amino acid sequence above.

Abstract: The present invention relates to sperm specific surface proteins, nucleic acid sequences encoding those proteins and antibodies raised against those proteins. Compositions comprising the sperm specific proteins or inhibitors of said proteins can be used in contraceptive applications.

Abstract: Methods for treating female sexual dysfunction are provided. A pharmaceutical composition containing a vasoactive agent selected from vasoactive intestinal potypeptide (VIP) and VIP agonists is administered to the vagina and/or vulvar region of the individual undergoing treatment. The formulations are also useful for improving vaginal muscle tone and tissue health, enhancing vaginal lubrication, and minimizing excess collagen deposition. Pharmaceutical formulations and kits are also provided.

Abstract: A method for production of lactic acid involving extracting protein from a natural renewable feedstock, preferably extracted from lignocellulose sources such as soybean hull, separating the feedstock into liquid and solid substrate feedstock, steam exploding the solid substrate feedstock by placing the solid feedstock in a pressure chamber, pressurizing the steam chamber with saturated steam, maintaining the pressure until the solid feedstock reaches temperatures in excess of the boiling point of water at atmospheric pressure, and explosively decompressing the pressure to a pressure no greater than atmospheric pressure. Hydrolyzing the steam-exploded feedstock by either acid hydrolysis or enzyme hydrolysis, and fermenting the resulting hydrolyzed feedstock to produce lactic acid. The hydrolyzing and fermenting steps may be carried out simultaneously, followed by recovering the lactate from the resultant material.

Abstract: The invention provides isolated agents having novel chemical structures and possessing superior activity as derepressors of IAP inhibited caspase. The invention further provides a method of derepressing an IAP-inhibited caspase. The invention further provides assay methods employing labeled compounds of the invention, especially fluorescent labeled compounds.

Abstract: Dipeptide, and tripeptide and tetrapeptide ester derivatives of bioactive agents are provided wherein the parent agents are substrates effluxed by the P-gp transporter. The derivatives are useful in treating the same condition as the bioactive agent. Also disclosed is a method for preparing a bioactive agent for targeted delivery by nutrient or peptide transporters comprising linking the agent to one or more groups of the formula —X—Y(n)-Z(n?)-Z?(n?)-R; wherein each X, Y, Z, and Z? is independently Met, Val, Thr, Tyr, Trp, Ser, Ala or Gly; R is independently H or an amino-protecting group; n=1, and each, n?, or n? is independently 0 or 1.

Abstract: The present invention relates to the use of proinsulin C-peptide or a variant, derivative or fragment thereof in the manufacture of a medicament for reducing the OTc interval and the use of proinsulin C-peptide or a variant, derivative or fragment thereof in the manufacture of a medicament for reducing the risk of sudden death or ‘dead in bed’ syndrome; particularly in patients suffering from IDDM.

Abstract: Imaging agents for magnetic resonance imaging are disclosed. Methods of monitoring angiogenesis and the growth and remission of tumor tissue are also disclosed. Methods of monitoring blood clot formation and dissolution are additionally disclosed. Methods of monitoring wound healing are further disclosed. A kit for obtaining an image of a biological structure is further disclosed.

Abstract: The invention relates to a formulation comprising a polypeptide selected from at least one of insulin, an insulin metabolite, an insulin analog, and an insulin derivative; at least one surfactant; optionally at least one preservative; and optionally at least one of an isotonicizing agent, a buffer or an excipient, wherein the formulation is free from or low in zinc. The invention also relates to the production of such insulin preparations and their use as pharmaceutical formulations.

Abstract: The invention relates to a formulation comprising a polypeptide selected from at least one of insulin, an insulin metabolite, an insulin analog, and an insulin derivative; at least one surfactant; optionally at least one preservative; and optionally at least one of an isotonicizing agent, a buffer or an excipient, wherein the formulation is free from or low in zinc. The invention also relates to the production of such insulin preparations and their use as pharmaceutical formulations.