Abstract: An antigen containing 3-methoxy-4-hydroxyphenylethylene glycol and represented by formula (I): ##STR1## (wherein R-NH is the residue of a polypeptide carrier R-NH.sub.2), and a method of producing an antibody to 3-methoxy-4-hydroxyphenylethylene glycol, characterized in that the method comprises immunizing an animal by using the antigen containing 3-methoxy-4-hydroxyphenylethylene glycol. The MHPG antigen of the present invention is capable of producing an MHPG antibody of high specificity. This antibody enables a precise determination of MHPG in specimens such as body fluid.

Abstract: A polyethylene glycol derivative of the formula ##STR1## wherein R represents a lower alkyl and n represents an optional positive integer which renders the average molecular weight of the polyethylene glycol moiety about 1,000 to 12,000, a peptide modified by said polyethylene glycol derivative and a method for production thereof. The polyethylene glycol derivative (I) is capable of modifying the guanidino groups in peptides. The peptides modified by the polyethylene glycol derivative (I) are extremely stable, are considerably delayed in biological clearance (i.e. the durability is extended) and exhibit their physiological activities effectively over the long period.

Abstract: The invention discloses novel series of silicone polyesters which are useful as delivery systems for a variety of hydroxyl containing active such as lanolin, cholesterol, dihydrocholesterol, Vitamin A, Vitamin D-2, Vitamin D-3, Vitamin D-4, Vitamin E, and Panthenol. Compounds of the invention by are prepared by the esterification of (a) a hydroxyl containing silicone compound selected from silanol and dimethicone copolyol (b) a diacid and (c) a hydroxyl functional active selected from lanolin, cholesterol, dihydrocholesterol, Vitamin A, Vitamin D-2, Vitamin D-3, Vitamin D-4, Vitamin E, and Panthenol; and optionally (d) a mono functional fatty acid. The polyesters of the present invention allow for the formulation of personal care products in which the "active" can be formulated into a variety of solvents without the loss of activity.

Abstract: The present invention relates to antitumor compounds of the formula I: ##STR1## wherein M is selected from the group consisting of an hydrogen atom, a peptide residue, and a protein residue linked to the carbon atom via the amino residue of .epsilon.-lysine present therein which can be an antibody used to target the anti-tumor agent to the malignant cells, and R can be an antitumor agent such as daunorubicin, doxorubicin, or an epirublicin derivative.

Abstract: A vaccine composition for inducing anti-tumor immunity comprising non-malignant cells, preferably syngeneic mon-malignant cells, coupled with adjuvant compounds. The nonmalignant immunizing cells of the present invention induce T-cell mediated cytoxicity which cross-reacts with tumor cells, providing in vivo protection against the tumor cells. Examples of turmors which may be treated by administration of the vaccine compositions include fibrosarcomas, glioblastomas, and all solid and lymphoid tumors.

Abstract: The invention pertains to terpyridine compounds having structure (I). These compounds form fluorescent lanthanide chelates with the appropriate metal ions. The fluorescent metal chelates are useful as probes in time-resolved fluorescence spectroscopy.

Abstract: The present invention provides digoxigenin derivatives of the formula: ##STR1## wherein n is a whole number of from 1 to 4 and Z is a carboxyl group or a functional derivative derived therefrom. The present invention also provides digoxigenin conjugates of the general formula: ##STR2## wherein the carrier is an immunogenic carrier material, a nucleic acid or a labelled immunocomponent of a labelled digoxigenin immunoconjugate for use in an immunoassay, m is a number from 1 to the number of coupling positions available on the carrier and Y is the group formed by the reaction of the carboxyl function Z of the digoxigenin derivative of general formula (I) with the reacting position of the carrier material. Also described are uses of these conjugates as nucleic acid probes, immunogens, and in immunoassay.

Abstract: A new method is described for eliciting IgG antibody response to proteins or synthetic peptides, particularly those that are weakly immunogenic, without the requirement for the use of adjuvants, thereby making it easier and safer to confer protection against pathogenic organisms. The antigen is coupled to a monoclonal antibody, specific for membrane determinants expressed on certain types of mammalian recipient cells, called antigen presenting cells. The monoclonal antibody acts as a "vector" or "delivery vehicle" for targeting foreign antigens onto such recipient cells. This targeting facilitates subsequent antigen recognition by helper T-cells, which are pivotal in helping the induction of antigen-specific IgG responses.

Abstract: Prolonged-action immunotoxin consisting of a conjugate in which an antibody or antibody fragment is coupled, by means of a covalent structure containing a disulfide group or a thioether group, with a glycoprotein which inactivates ribosomes and has a prolonged action obtained by the oxidation of its saccharide units which periodate ions.

Abstract: Polyethylene glycol derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl, m and n are the same or different and each represents a positive integer and p is 0 or a positive integer, peptides modified by the polyethylene glycol derivatives, methods for producing them and use of the modified peptides. The peptides modified by the polyethylene glycol derivatives (I) of the invention, as compared with the corresponding non-modified peptides, show decreased antigenicity, are considerably delayed in biological clearance, and exhibit their physiological activities effectively over a long period, rendering them very effective as pharmaceuticals as well as drugs for animals.

Abstract: Modified proteins for carrying hapten are provided. These carriers are prepared by blocking the amino groups of the original protein and then introducing amino groups into the carboxyl groups of the original protein. The blocking groups may be eliminated at the later stage to regenerate the amino groups of the original protein. The modified protein or polypeptide carrier have the three-dimensional structures different from the original proteins so that they are used in immunoassay while carrying low molecular weight haptens without the fear of forming antibodies for the original proteins. The modified protein carrier may also be used in the passive agglutination immunoassay without the need of absorbing the anti-hapten antibodies by the hapten-carrying carriers.

Abstract: "Iscom" adjuvant matrices, comprising a sterol, a glycoside, a solubilized water-insoluble antigen and, optionally, a phospholipid, may be formed without removing the solubilizing agent used for the antigen.The glycoside is preferably Quil A and the sterol is preferably cholesterol.

Abstract: An antigen/antibody complex is described wherein the antibody functions as an adjuvant. The antibody comprises an anti-lymphocyte antibody. The antigen comprises a hapten, peptide, protein, carbohydrate, virus, bacterium, parasite or other whole microorganism. The complex of antigen coupled to antibody may be used in immunizing a higher animal against an antigen.

Abstract: Polyethylene glycol serum immunoglobulin conjugates exhibit substantial rstance to degradation by intestinal enzyme while retaining their immuno-activity. Thus, PEG-IgG or PEG-IgA conjugates can be used as orally administered therapeutics to treat patients with gastrointestinal immunodeficiency to reconstitute secretory immunity. Preferred conjugates are made by reacting activated PEG and IgG in ratios of from 1:5 to 1:1000 such that less than about 27% of the IgG lysine residues are bonded to the PEG. The conjugates are advantageously formulated into a pharmaceutical composition comprising the conjugate and a pharmaceutically acceptable oral carrier. Particularly for administration to infants, a preferred oral carrier is milk.

Abstract: A modified pertussis toxin suitable as a pertussis vaccine having an essentially unmodified B-oligomer and a catalytic subunit which is inactivated by treatment with polyphosphate compounds, sulfhydryl reductants and mild detergents followed by modification of the activated --SH groups to inhibit ADP-ribosylating activity.

Abstract: This invention provides a method of preparing conjugates of bioactive compounds and site-specific compounds in which covalent bonding between the compounds is effected by interfacial condensation while protecting the active binding sites from the condensation reaction. This provides very high yields of the bioactive, site-specific conjugate, the products are homogeneous and it provides novel conjugate products. It is of particular advantage for monoclonal antibodies conjugated with cytotoxic agents.

Abstract: Methods are provided for the purification of interleukin-2 (IL-2) from a wide variety of sources, including synthetic mixtures, culture medium conditioned by natural IL-2 producing cells, and mammalian and bacterial recombinant IL-2 expression systems. The methods of the invention employ IL-2 receptor-affinity adsorbents in which soluble IL-2 receptors have been immobilized on solid supports. Through the use of these affinity adsorbents, highly purified IL-2 can be produced in a single step from bacterial extracts or conditioned medium. The IL-2 thus purified is largely free of aggregated forms, which are often present when other purification methods are used.

Abstract: Polypeptide compositions are provided having a binding site specific for a particular target ligand and further having an active functionality proximate the binding site. The active functionality may be a reporter molecule, in which case the polypeptide compositions are useful in performing assays for the target ligand. Alternatively, the active functionality may be a chemotherapeutic agent, in which case the polypeptide compositions are useful for therapeutic treatment of various diseased states. A novel method for preparing such polypeptides having active functionalities proximate their binding site comprises combining the polypeptide specific for the target ligand with an affinity label including ligand having a reactive group attached thereto. The reactive group is then covalently attached to an amino acid side chain proximate the binding site and cleaved from the substrate. The substrate is eluted, leaving a moiety of the reactive group covalently attached to the polypeptide.

Abstract: The present invention relates to an improved method for producing oligosaccharide conjugate vaccines. In an additional aspect of the invention, oligosaccharide vaccines are produced which elicit a monospecific and homogeneous immune response to capsular polysaccharide. A specific embodiment of the invention provides for vaccines which induce immunity to prevalent serotypes of Streptococcus pneumoniae.

Abstract: A process for solubilizing membrane receptor proteins which includes exposing an outer membrane having the desired protein to an oxidizing agent, treating the membrane with a detergent and treating with an inhibitory material lowering agent. This method maintains the activity of the membrane proteins after solubilization.

Abstract: Methods are provided for the purification of interleukin-2 (IL-2) and chimeric proteins containing an IL-2 moiety from a wide variety of sources, including synthetic mixtures, cell culture conditioned medium and mammalian and bacterial recombinant expression systems. The methods of the invention employ IL-2 receptor-affinity adsorbents in which soluble IL-2 receptors have been immobilized on solid supports. Through the use of these affinity adsorbents, highly purified IL-2 and chimeric proteins containing an IL-2 moiety can be produced in a single step from bacterial extracts or conditioned medium. The proteins thus purified are largely free of aggregated forms, which are often present when other purification methods are used.

Abstract: The present invention relates to conjugates in which a monovalent carboxylic ionophore is associated by means of a covalent bond with a macromolecule chosen from antibodies, fragments of antibodies, proteins such as peptide hormones or human proteins, and peptide ligands. It also relates to the activated inophores.These conjugates are suitable as immunotoxin potentiators.

Abstract: A method for controlling the release of durgs or other passenger molecules form carrier conjugates, and a class of conjugates that releases drugs when ingested by a cell or subjected to acidic conditions, are disclosed. These conjugates contain a passenger molecule which is attached to a spacer molecule through an acidic bonding group, such as carboxyl, that is in a "cis" configuration with another acidic group, and a carrier molecule that is bonded to the spacer molecule at another site. When subjected to a mild increase in acidity, such as occurs within a lysosome of a cell, the drug or other passenger molecule is hydrolyzed from the the conjugate and released in unmodified, active form.

Abstract: A conjugate of a protein carrier and an antigen is disclosed. The carrier protein is cationized and the conjugate has enhanced immunogenic properties over those of the antigen alone. Cationization can be accomplished by derivatization of native carboxyl groups on the protein with an aklyl diamine, e.g. ethylene diamine, resulting in the formation of side chain aminoalkylamide groups, e.g. aminoethylamide.

Abstract: The present invention relates to anti-tumor-conjugation agent-protein compounds of the general formula I: ##STR1## wherein, R.sub.1 and R.sub.2 are each independently selected from hydrogen atom, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-6 carboxyalkyl, phenyl, or phenyl substituted by at least one of hydroxy, halogen, lower alkyl, lower alkoxy, or nitro, with the proviso that R.sub.1 and R.sub.2 cannot be simultaneously a hydrogen, and when one of R.sub.1 or R.sub.2 is a hydrogen, the other one cannot be --CH.sub.2 COOH;A is the residue of an anti-tumor agent containing at least one amino group available to form an amide bound; andB is a free .epsilon.-lysine containing residue selected from a peptide or a protein.

Abstract: Undesired immune responses are suppressed by administering a nonimmunogenic material which comprises one or more haptens or epitopes corresponding to the antigen which causes the undesired immune response, the number and spacing of the haptens or epitopes being insufficient to trigger an immune response but sufficient to inhibit it. Also disclosed is an improved vaccine from which low molecular weight suppressive polymer has been removed.

Abstract: A protein conjugate or mixture useful in immunotherapy composed of a biological response modifier (BRM) and an allergen is disclosed. In use the protein conjugate or mixture is combined with a pharmaceutically acceptable carrier. Cytokines, bacterial, fungal and viral immunopotentiators and thymus hormones are disclosed as suitable BRM's for use in the invention.

Abstract: A method of potentiating immunotoxin action in an immunotoxin/target-cell stem in which Brefeldin A is utilized as an immunopotentiator. The Brefeldin A enhances the immunotoxin pathway while blocking or inhibiting the nonspecific pathway, thus being particularly useful in conjunction with immunotoxins made from holotoxins. The Brefeldin A is effective in small, nontoxic concentrations and therefore may be utilized with either in vivo or in vitro systems.

Abstract: Conjugates of transferrin or ceruloplasmin with anti-tumour agents. Such conjugates are useful in the treatment of tumours. Suitable anti-tumour agents include adriamycin, daunomycin, methotrexate, vincristin, 6-mercaptopurine, cytosine arabinoside and cyclophosphamide. Transferrin or ceruloplasmin in preferably coupled to the anti-tumour agent by means of glutaraldehyde.

Abstract: A polypeptide-labeled analyte analog for use in an immunoassay is prepared which is capable of binding with a polypeptide partner to provide enzymatic activity such as a ribonuclease or .beta.-galactosidase activity. The polypeptide analog provides a highly sensitive, immunoassay method for determining the amount of an analyte in a sample containing a known analyte in an unknown concentration. To carry out an immunoassay, there is brought together in a medium a sample, the polypeptide-labeled analog of the analyte, an antibody specific for said analyte, a polypeptide partner capable of non-covalently binding with the polypeptide-labeled analyte analog to form a complex having catalytic activity, and a substrate capable of being converted to a reporter molecule by the catalytic activity of said complex.

Abstract: A process for production of antibody conjugates which comprises modification of a part of the amino groups in an antibody or its fragment whose antigen-binding activity is lowered by the modification of its amino groups, with a reversible modifier for protein amino groups, reaction of the antibody or its fragment with a substance bearing a group reactive with the amino group and removal of the residues of the reversible modifier from the amino groups and, when necessary, the residues of the substance bearing a group reactive with the amino group in case they are introduced onto groups other than amino groups. The process according to the present invention gives antibody conjugates with retention of antigen-binding activity and these conjugates have a possibility of being used in affinity chromatography or as a diagnostic agent or a drug for cancer therapy.

Abstract: The present invention relates to a series of novel silicone proteins which are high substantive to fiber and hair. The compounds contain both a silicone portion and protein portion in a covalent bone one molecule. Since the compounds of the present invention are high molecular weight silicone polymers, they have a high degree of oxidative stability, even at elevated temperatures and are nonirritating to skin and eyes. The proteins of the present invention plate out on and form a film on the surface of hair skin and textile fibers. In addition, these compounds are non volatile and exhibit a inverse cloud point. These combination of properties makes these polymers ideally suited for use in personal care applications.The compounds of the invention having a pendant amphoteric group is represented by the following formula; ##STR1## wherein R is ##STR2## a is an integer from 0 to 200; b is an integer from 0 to 200;c is an integer from 1 to 200;R.sup.1 is selected from --(CH.sub.2).sub.n CH.sub.

Abstract: A substituted monoethylglycinexylidide or analogue is disclosed. The xylidide or analogue has the structure of FIG. 1 of the attached drawings where M is CH.sub.2 NHCH.sub.2 CH.sub.3, CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.3 or CH.sub.2 OCH.sub.2 CH.sub.3, one of Y.sup.1 and Y.sup.2 is H and the other is a protein or a fluorescein moiety chemcially bonded to the glycinexylidide or analogue moiety. Also disclosed is a method for carrying out immunoassays for MEGX, which has the structure of FIG. 3 of the attached drawings. The method for carrying out immunoassays involves using the foregoing compounds as tracers and immunogens.

Abstract: An immunogenic conjugate which is the reductive amination product of an immunogenic capsular polymer fragment having at least one reducing group and derived from a bacterial capsular polymer of a bacterial pathogen, and a bacterial toxin or toxoid. The invention also relates to methods for the preparation of the conjugates, a vaccine containing the conjugates which elicits effective levels of anti-capsular polymer antibodies in humans. Also disclosed are methods for inducing active immunization against systemic infection in young mammals caused by bacterial pathogens comprising the administration of an immunogenic amount of the abovedescribed conjugate. In a preferred embodiment, the capsular polymer fragment prior to conjugation has at least one aldehyde group at each end of the fragment. The final conjugate made with such capsular polymers has a lattice or network structure, and provides extremely high levels of anti-capsular polymer antibodies in infants.

Abstract: A polyethylene glycol derivative of the formula ##STR1## wherein R represents a lower alkyl and n represents an optional positive integer which renders the average molecular weight of the polyethylene glycol moiety about 1,000 to 12,000, a peptide modified by said polyethylene glycol derivative and a method for production thereof.The polyethylene glycol derivative (I) is capable of modifying the guanidino groups in peptides. The peptides modified by the polyethylene glycol derivative (I) are extremely stable, are considerably delayed in biological clearance (i.e. the durability is extended) and exhibit their physiological activities effectively over the long period.

Abstract: A new method is described for the preparation of a safe, immunogenic and efficacious vaccine for protection against the disease pertussis. In development of this vaccine, specific functional sites of pertussis toxin have been identified, and using this information, defined mutant holotoxins have been produced by site directed mutagenesis of the toxin gene. A number of these toxin analogues are detoxified, retain an immunodominant S1 epitope, are immunoganic and are protective in the standard pertussis vaccine potency test in mice.

Abstract: The present invention provides a chimeric protein IL4-PE40 which selectively kills IL4 receptor bearing cells. A mutant form of the protein is also provided.

Abstract: The present invention concerns novel immunogens. These immunogens comprise novel compounds which consist of an antigen or antigenic determinant couple dot an amphiphilic adjuvant molecule and optionally also free amphiphilic adjuvant molecules. An advantageous features of these novel immunogens is the presence of both an excellent immunogen activity as well as a pronounced adjuvant activity in a single complex.

Abstract: A fluorescence polarization immunoassay for detecting the presence of methadone in a test sample is provided, based upon competition between methadone and a fluorescently labeled tracer for the binding sites on an antibody specific for methadone. The concentration of methadone in the sample determines the amount of tracer that binds to the antibody. The amount of tracer-antibody complex formed can be quantitatively measured and is inversely proportional to the quantity of methadone in the sample. Tracers used as reagents and immunogens used to raise antibodies for use as reagents are also disclosed.

Abstract: A novel hyposensitization agent was prepared by covalently attaching a saccharide to a cedar pollen allergen having a partial amino acid sequence of Ala-Ile-Asn-Ile-Phe-Asn- beginning at its N-terminal. The hyposensitization agent, when compared with an intact cedar pollen allergen, extremely accelerates the production of immunoglobulin G and M antibodies which are specific to intact cedar pollen allergen, but extremely reduces the production of immunoglobulin E antibody which is specific to the allergen. Thus, the hyposensitization agent is administrable to cedar pollinosis patients with no anaphylaxis and allergy, and cuts hyposensitization period to about 1/3 to 1/200.

Abstract: Methods and composition for detecting the presence of human ras oncogene related malignancies are provided, where a biological sample is assayed for protein(s) specific to a DNA sequence. In the methods of this invention, the test reaction involves admixing a biological sample from cancer patients or control donors with labelled ras oncogene promoter DNA. The admixture is incubated under conditions favorable for promoting specific interactions between proteins and the labelled DNA. Thereafter, the admixture is separated by charge and size in an electrophoretic field and the protein-DNA interactions are identified depending on the method of label employed. Bands migrating at a slower rate than the uncomplexed DNA are indicative of a protein-DNA interaction (i.e. circulating serum protein(s) from cancer patients interacting specifically with a region(s) of the ras oncogene promoter DNA).

Abstract: The invention concerns antigens for the production of antibodies to Platelet Activating Factor (PAF). The antigens are PAF analogues of formula (I) ##STR1## wherein X comprises a high molecular weight group, R.sup.1 is a linking group and R.sup.2 to R.sup.5 are selected from C.sub.1 to C.sub.6 alkyl.Other aspects of the invention include PAF-antibodies produced using said antigens, labelled PAF analogues, intermediates for the preparation of PAF analogues and methods and a kit for the immunoassay of PAF.

Abstract: A method for conferring or increasing the antigenicity of a disulfide-crosslinked protein by treating the protein with an oxidizing agent, such as periodate, having an oxidation potential sufficient to cleave disulfide linkages. Excess oxidizing agent is then inactivated by addition of a reducing agent. The resulting protein exhibits an increase in its ability to be bound by select antibodies, particularly monoclonal antibodies directed to linear peptide epitopes in the protein.

Abstract: A protein containing at least one pendant sulfhydryl group is directly radiolabeled with a radiometal which binds tightly to sulfhydryl groups, using one or more pendant sulfhydral groups on the protein as endogenous ligands and optionally using an exogenous ligand which binds tightly to the radiometal ion to further stabilize the chelate.

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.

Abstract: Superior pharmaceutical compositions which comprise carriers coupled to epitope-bearing moieties are described. The carriers are crystalline or paracrystalline glycoproteins, especially those derived from S-layers of microbial cell walls. These conjugates are capable of eliciting the formation of antibodies as well as a T-cell response.

Abstract: An immunogenic complex comprising a peptide containing a hydrophobic tail, the peptide being adsorbed to hepatitis B virus surface antigen via the hydrophobic tail. Such complex in a immunogenically effective amount when administered with a physiologically acceptable diluent and an adjuvant can serve as a vaccine.

Abstract: The present invention relates to a novel glycoprotein, extracted from the seeds of Trichosanthes kirilowii, called: trichokirin, as well as to its modified derivatives containing a free or blocked SH group.It relates to a process for its preparation, to its use and to pharmaceutical compositions in which it is present.

Abstract: The present invention provides a hapten-protein conjugate, wherein a hapten is bound to the reducing end of a sugar which consists of up to 10 monosaccharide units and on a free CH.sub.2 OH group on the other end of the sugar, which is in the .alpha.-position to a hydroxyl group, is bound a protein.

Abstract: Hepatitis B PreS2+S antigen is isolated from plasma by adsorption on an affinity chromatography column, elution with a chaotropic agent and treatment with concentrated urea at an elevated temperature. The process retains all or substantially all of the preS2+S antigen.