Abstract: This invention discloses the creation of a novel single ligand-targeted multi-stereoisomer peptide-polymer conjugate compounds comprising a group of different synthetic and chemically modified stereoisomer peptides that have been conjugated to a biocompatible polymer carrying a peptide ligand for targeted delivery and/or encapsulated in ligand targeted polymer nanoparticles. The unique physicochemical properties of the stereoisomer peptides provide therapeutic compounds with ideal biopharmaceutical properties. The stereoisomer peptides carried by the polymer are delivered to cells or tissues to inhibit, suppress, block, antagonize or disrupt, simultaneously and independently, the functional domain of different disease causing proteins.

Abstract: This invention discloses the creation of a novel single ligand-targeted multi-stereoisomer peptide-polymer conjugate compounds comprising a group of different synthetic and chemically modified stereoisomer peptides that have been conjugated to a biocompatible polymer carrying a peptide ligand for targeted delivery and/or encapsulated in ligand targeted polymer nanoparticles. The unique physicochemical properties of the stereoisomer peptides provide therapeutic compounds with ideal biopharmaceutical properties. The stereoisomer peptides carried by the polymer are delivered to cells or tissues to inhibit, suppress, block, antagonize or disrupt, simultaneously and independently, the functional domain of different disease causing proteins.

Abstract: This invention discloses ligand-targeted multi-stereoisomer peptide-polymer conjugate compounds comprising a plurality of different synthetic and chemically modified stereoisomer peptides that have been conjugated to a biocompatible polymer carrying a peptide ligand for targeted delivery or encapsulated in ligand targeted polymer nanoparticles. The unique physicochemical properties of the stereoisomer peptides provide therapeutic compounds with ideal biopharmaceutical properties. The stereoisomer peptides carried by the polymer are delivered to cells or tissues to inhibit, suppress, block, or disrupt, simultaneously and independently, the functional domain of a different disease causing protein.

Abstract: This invention discloses a group of 298 peptides from which several peptides are independently selected and synthesized in their stereoisomer and chemically modified forms, and conjugated to a polymer via linkers creating novel anti-HIV-1 multi-peptide-polymer conjugate compounds for the treatment and prevention of HIV-1 infection. The peptides mimic the domains of major HIV-1 proteins, and therefore, they function as inhibitors of the targeted HIV-1 proteins. The polymer is a useful delivery system for the stereoisomer peptides, and certain peptides are peptide-ligands for targeted delivery into the HIV infected cells.

Abstract: The invention provides compounds of the formula Poly-([SP-LI]n-PL-L2) including a collection of 152 peptides useful to create the compounds, and their uses thereof for the treatment of a variety of mammalian diseases. The compound, a novel ligand-targeted multi-stereoisomer peptide polymer conjugate, comprises two or more stereoisomer peptides and a peptide-ligand conjugated via linkers to a biocompatible hydrophilic polymer, preferably HPMA. The increased stability and solubility of the compound carrying the stereoisomer peptides and a peptide-ligand provide ideal pharmaceutical properties including the delivery by the polymer of the peptides into the target cells. The compounds of the invention are useful therapeutics for the treatment of a variety of mammalian diseases.

Abstract: This invention discloses ligand-targeted multi-stereoisomer peptide-polymer conjugate compounds comprising a plurality of different synthetic and chemically modified stereoisomer peptides that have been conjugated to a biocompatible polymer carrying a peptide ligand for targeted delivery or encapsulated in ligand targeted polymer nanoparticles. The unique physicochemical properties of the stereoisomer peptides provide therapeutic compounds with ideal biopharmaceutical properties. The stereoisomer peptides carried by the polymer are delivered to cells or tissues to inhibit, suppress, block, or disrupt, simultaneously and independently, the functional domain of a different disease causing protein.

Abstract: The invention provides compounds of the formula Poly-([SP-LI]n-PL-L2) including a collection of 152 peptides useful to create the compounds, and their uses thereof for the treatment of a variety of mammalian diseases. The compound, a novel ligand-targeted multi-stereoisomer peptide polymer conjugate, comprises two or more stereoisomer peptides and a peptide-ligand conjugated via linkers to a biocompatible hydrophilic polymer, preferably HPMA. The increased stability and solubility of the compound carrying the stereoisomer peptides and a peptide-ligand provide ideal pharmaceutical properties including the delivery by the polymer of the peptides into the target cells. The compounds of the invention are useful therapeutics for the treatment of a variety of mammalian diseases.

Abstract: The invention relates to a library of 298 peptides useful for formulating a novel therapeutic HIV vaccine. The peptide sequences were selected on the basis of calibration of molecular structure properties of HIV-1 or host cell proteins. A mixture of D- and L-amino acids or all D-amino acids are used to synthesize the stereoisomer peptides for the purpose of increasing their stability. The peptides are expected to have the ability to potently inhibit functioning of proteins important for HIV infection. A plural of the peptides are conjugated together with a biocompatible polymer, preferably HPMA to further increase stability and solubility, decrease drug toxicity, and potentially evade multidrug resistance and exert cooperative effect, since some peptides are the ligands for host proteins such as integrin, trombospondin, VEGFR and LEDGF which can bring the therapeutic peptides to the target cells and therefore help disrupt the interactions between the host proteins and the HIV proteins.

Abstract: This invention provides a method for solubilizing and recovering in bioactive form, a target polypeptide or protein that has been expressed from a host organism in insoluble form. The polypeptide is isolated from the host organism by standard procedures including disrupting the host cell to produce a lysate and recovering the precipitate from the lysate. The precipitate containing the polypeptide is solubilized in a non-denaturant and detergent free non-buffered solubilization solution containing sodium hydroxide between 8 and 10 mM, mannitol between 2 and 5 mM and lactose between 1 and 2 mM. The resultant solubilization preparation contains a biologically active target polypeptide between 1 and 4 mg per ml of solubilization solution. The solubilized polypeptide obtained in this particular manner constitutes the object of the invention.

Abstract: This invention entails a method for solubilizing and recovering, in bioactive and isolated form with retained native state configuration, a target peptide from a host organism in which the heterologous polypeptide is present in insoluble form. Broadly this method comprises (i) disrupting the host cell to produce a lysate (ii) recovering lysate precipitate containing the polypeptide (iii) resuspending the lysate precipitate in a denaturant-free, non-buffered solubilization solution to produce a solubilization preparation that comprises both sodium hydroxide between about 8 and about 10 mM and the target peptide between about 1 and about 4 mg peptide per ml solubilization solution, wherein the resultant solubilization preparation has a pH of between about 9 and about 11.2; (iv) recovering supernatant from the solubilization preparation containing non-denatured target peptide. Optionally, stabilizing compounds and detergents are employed.