Abstract: An adjuvant formulation includes a monophosphoryl Lipid A (MPLA) analogue, a Pam3CSK4 analogue, or a muramyldipeptide (MDP) analogue, or combinations thereof. The adjuvant may be formulated in soluble form or in a nanoparticle, such as polylactic glycolic acid nanoparticles. A vaccine formulation comprises the adjuvant formulation and an immunogen. Methods of vaccinating an animal include delivering the vaccine formulation to the animal.

Abstract: The present invention provides liposomal vaccines containing immunogenic lipopeptides that are capable of modulating the humoral and cellular immune responses in vivo.

Abstract: The present invention provides liposomal vaccines containing immunogenic lipopeptides that are capable of modulating the humoral and cellular immune responses in vivo.

Abstract: The present invention provides liposomal vaccines containing immunogenic lipopeptides that are capable of modulating the humoral and cellular immune responses in vivo.

Abstract: The present invention provides liposomal vaccines containing immunogenic lipopeptides that are capable of modulating the humoral and cellular immune responses in vivo.

Abstract: The core structure of pentaerythritol has been used as a replacement for one or both sugars in lipid A, leading to the generation of a series of lipid A analogs. These lipid A analogs may further differ from lipid A with respect to, e.g., the number, nature and location of negatively charged groups, and the number, nature and location of the lipid chains. The lipid A analogs may be lipid A agonists useful as immunostimulatory agents, or lipid A antagonists useful in the treatment of septic shock. In a like manner, a residue of pentaerythritylamine may be used as a replacement for an amino sugar residue in a carbohydrate ligand having a biological activity of interest, generating a series of ligand analogs. These are useful, e.g., as haptens, inhibitors of bacterial-host cell adhesion, etc.

Abstract: The core structure of pentaerythritol has been used as a replacement for one or both sugars in lipid A, leading to the generation of a series of lipid A analogs. These lipid A analogs may further differ from lipid A with respect to, e.g., the number, nature and location of negatively charged groups, and the number, nature and location of the lipid chains. The lipid A analogs may be lipid A agonists useful as immunostimulatory agents, or lipid A antagonists useful in the treatment of septic shock. In a like manner, a residue of pentaerythritylamine may be used as a replacement for an amino sugar residue in a carbohydrate ligand having a biological activity of interest, generating a series of ligand analogs. These are useful, e.g., as haptens, inhibitors of bacterial-host cell adhesion, etc.

Abstract: The core structure of pentaerythritol has been used as a replacement for one or both sugars in lipid A, leading to the generation of a series of lipid A analogs. These lipid A analogs may further differ from lipid A with respect to, e.g., the number, nature and location of negatively charged groups, and the number, nature and location of the lipid chains. The lipid A analogs may be lipid A agonists useful as immunostimulatory agents, or lipid A antagonists useful in the treatment of septic shock. In a like manner, a residue of pentaerythritylamine may be used as a replacement for an amino sugar residue in a carbohydrate ligand having a biological activity of interest, generating a series of ligand analogs. These are useful, e.g., as haptens, inhibitors of bacterial-host cell adhesion, etc.

Abstract: Covalently lipidated oligonucleotides comprising the CpG dinucleotide unit, or an analogue thereof, may be used as immunostimulatory agents to protect against a disease caused by a cancer cell or a pathogen, either alone or in conjunction with immunogens and/or non-immunological agents. Lipidated oligonucleotides with special backbones, lipidated oligonucleotides with fewer than eight nucleotides, and lipidated oligonucleotides comprising a plurality of CpG dinucleotide-containing segments connected by a long internucleoside linkage are of particular interest. These compounds are also novel per se.

Abstract: New synthetic Lipid-A analogs based on monosaccharide (1) and disaccharide (2) derivatives were designed and prepared in the present invention. Both structures (1) and (2) incorporate novel lipid structures (3) and (4) that are not found in nature. Also, novel disaccharide Lipid-A structures (2) that incorporate novel contingents of uniform lipids and where R1, R4 and R5 are the same substitution group of structure (III) were synthesized. Liposome formulations containing totally synthetic components such as synthetic Lipid-A and synthetic lipopeptide derived from tumor-associated MUC1 mucin are described along with their therapeutic utility. Comparative test results of immunostimulating properties and toxicity of Lipid-A analogs (1) and (2) are included.

Abstract: Covalently lipidated oligonucleotides comprising the CpG dinucleotide unit, or an analogue thereof, may be used as immunostimulatory agents to protect against a disease caused by a cancer cell or a pathogen, either alone or in conjunction with immunogens and/or non-immunological agents. Lipidated oligonucleotides with special backbones, lipidated oligonucleotides with fewer than eight nucleotides, and lipidated oligonucleotides comprising a plurality of CpG dinucleotide-containing segments connected by a long internucleoside linkage are of particular interest. These compounds are also novel per se.

Abstract: A conjugate of a plurality of carbohydrate haptens and an aggregate (multimer) of monomeric units of a carrier moiety is provided. The conjugate may be used to elicit an immune response. The conjugate is preferably a carbohydrate-substituted aggregate of KLH monomers, in particular, a dimeric, trimeric or tetrameric aggregated. An aggregated STn-KLH conjugate is of particular interest.

Abstract: Randomly generated glycopeptide combinatorial libraries are generated by randomly glycosylating a peptide having at least one glycosylation site with at least one glycosyl donor, optionally blocking unreacted glycosylation sites on the glycopeptides and optionally selectively removing one or more protecting groups on the carbohydrate groups introduced at the first level; whereby a first level library of glycopeptides is created; and then optionally randomly glycosylating said first level library of glycopeptides, or a combination of first level libraries of glycopeptides, with at least one glycosyl donor, and optionally selectively removing one or more designated protecting groups on the carbohydrate groups introduced at the second level; whereby a second level library of glycopeptides is created. Further iterations of the process result in higher level libraries of increased diversity. The glycopeptide libraries including, e.g.

Abstract: The present invention provides liposomal vaccines containing immunogenic lipopeptides that are capable of modulating the humoral and cellular immune responses in vivo.

Abstract: Randomly generated glycopeptide combinatorial libraries are generated by randomly glycosylating a peptide having at least one glycosylation site with at least one glycosyl donor, optionally blocking unreacted glycosylation sites on the glycopeptides and optionally selectively removing one or more protecting groups on the carbohydrate groups introduced at the first level; whereby a first level library of glycopeptides is created; and then optionally randomly glycosylating said first level library of glycopeptides, or a combination of first level libraries of glycopeptides, with at least one glycosyl donor, and optionally selectively removing one or more designated protecting groups on the carbohydrate groups introduced at the second level; whereby a second level library of glycopeptides is created. Further iterations of the process result in higher level libraries of increased diversity. The glycopeptide libraries including, e.g.

Abstract: Glycoconjugate antigens are prepared by preparing a hapten glycoside, especially an alpha glycoside prepared by the Fischer method, with an olefinic aglycon moiety, especially one having a non-terminal double bond, ozonolyzing the hapten glycoside with an olefinic aglycon moiety having a non-terminal double bond to form a hapten-glycoside derivative, preferably without producing Germaldehyde as a byproduct removing by-products of ozonolysis, and conjugating the hapten-glycoside derivative to a carrier.

Abstract: A stereodirected process for synthesizing .alpha.-N-acetylgalactosaminides from N-acetylgalactosamine which, in a preferred embodiment, comprises:reacting N-acetylgalactosamine with a dialkyl acetal of an aldehyde or ketone to form a 4,6-O-alkylidene derivative;reacting said 4,6-O-alkylidene derivative with a protecting group compound to attach a protecting group selectively to 3-OH of said derivative to form a 3-O-protected derivative;reacting said 3-O-protected derivative with an anomeric group to form a glycosyl donor;reacting said glycosyl donor with an alcohol to form an N-acetylgalactosaminide.

Abstract: Fluorocarbon chain-containing linking arms can be used to conjugate haptens to protein carriers such as BSA, HSA, or antibodies without recourse to harsh chemistry. In addition, .sup.19 F atoms serve as markers for quantitative estimation of bound haptens.