Abstract: The present invention relates to the use of a compound of the following formula (I) for detecting a peptidase activity and/or a variation in pH: according to which: Y1 is a peptide, H or an alkyl; W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination thereof; n=0, 1 or 2; U and V are N, N+R or CZ4, R being H, alkyl, aralkyl, aryl, alkanoyl or alkylsulfonyl; Z1, Z2, Z3 and Z4 being independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulfonyl, including the carboxyl or sulfonyl esters or amides, and salts thereof.

Abstract: Synthetic antibody derivatives having at least two F regions covalently linked so as to enhance Fc activity for example effector recruitment. The use of such derivatives in the treatment of conditions where killing of cells is required for example cancer therapy. Methods for the preparation of derivatives are also described.

Abstract: Methods for reducing non-target retention of active moieties associated with immunoconjugates and their metabolites, and more specifically, for reducing renal retention of such active moieties, are disclosed. Methods of the present invention comprise administering an effective amount of a non-target reduction moiety, such as lysine, in addition to a therapeutically or diagnostically effective amount of an immunoconjugate. The non-target reduction moiety localizes in the kidneys and inhibits renal retention and reabsorption of active moieties associated with immunoconjugates and their metabolites.

Abstract: A method for preparing phycobiliprotein/amine-reactive dye conjugates is disclosed in which the conjugates so prepared overcome the energy transfer/fluorescent quenching dilemma encountered in the use of prior art conjugates. A phycobiliprotein, for example, phycoerythrin or allophycocyanin, is conjugated with an amine-reactive dye, for example, Texas Red or carboxyfluorescein succinimidyl ester, in the presence of a selective salt which causes a hydrophobic intramolecular rearrangement of the phycobiliprotein thereby exposing more hydrophobic sites for binding to the amine-reactive dye. The conjugates prepared according to the invention are useful in multiple color fluorescence assays without requiring the use of multiple exciting sources.

Abstract: To localize targets within the body (i.e., fixed intravascular antigens on emboli, neovascular endothelium, endothelium altered by regional inflammation) antibodies are linked via dextran spacer arms to rapidly cleared, Tc-99m labeled, microspheres. A micron-sized, albumin microsphere has been synthesized that is designed to enhance target surface interaction and to have a high antibody loading capacity. Stable, hydrophilic microspheres are produced from a pH dependent refolding of albumin followed by heat annealing. To couple dextran, the microspheres are derivatized with succinic anhydride and then linked via carbodiimide to succinic dihydrazide. After periodate oxidized dextran forms hydrazone linkages to the microspheres, additional dihydrazide coupled to the dextran spacer arm is used to link periodate oxidized IgG via its Fc domain carbohydrate. A milligram of the resulting 0.5-1.0 micron microspheres contains 50 to 350 ug of dextran and up to 10.sup.5 covalently bound IgG molecules per microsphere.

Abstract: A new series of bifunctional chelating agents useful for attaching metal ions to proteins, polypeptides and other polymers and methods for their preparation are described. These reagents are unique in their ability to bind a variety of metal ions and to yield a high metal ion concentration per protein molecule. Using these methods polymeric analogs of these bifunctional chelating agents called Starburst ligands can also be obtained. Protein metal chelates thus obtained will have useful radiophysical, chemical, fluorescent, photochemical and magnetic properties suitable for biomedical applications.

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: 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: Methods for rapidly labeling sulfhydryl-containing antibodies or fragments with technetium or rhenium radioisotopes are disclosed. The method generally involves combining an aqueous mixture of the radiometal in an oxidized form, a reducing agent and a water-soluble polyhydroxycarbonylic acid ligand to form a stable complex of the radiometal in its reduced state and contacting the mixture with the sulfhydryl-containing antibody or fragment to produce a radiometal-labeled antibody or fragment.

Abstract: Chimeric antibodies comprised of the variable region of an antibody chain contiguous with a polypeptide other than the constant region of that antibody chain are disclosed. Such chimeric antibodies can be comprised of the variable region of a chain of an immunoglobulin of selected specificity and an extrinsic polypeptide. In addition to the variable region of a chain of an immunoglobulin of selected specifity and an extrinsic polypeptide, the chimeric antibodies can include at least a portion of the constant region of an immunoglobFUNDING SOURCESThe work described herein was supported by grants from the National Institutes of Health, the American Cancer Society and the Damon Runyon--Walter Winchell Cancer Fund.

Abstract: The present invention relates to an immunotoxin. The invention further relates to a method of treating T cell leukemias and lymphomas, graft-versus-host diseases, and autoimmune diseases by administering an immunotoxin.

Abstract: The invention relates to compounds of formula: ##STR1## in which m, n, p and q are equal to 0 or 1, p being different from q and the sum m+n+p+q being equal to 2, A denotes a nonionic chain arrangement chosen from the groups:C.sub.2 H.sub.4 O.sub.r and/orC.sub.3 H.sub.5 (OH)O.sub.s,in which r denotes a number which can assume all integral values between 0 and 5 or a statistical average value between 0 and 20,s denotes a number which can assume all integral values between 0 and 5 or a statistical average value between 0 and 10,u is equal to 0 or 1, with the restriction that when u=0, s and r are also zero,R denotes(i) a linear or branched hydrocarbon radical which has 1 to 32 carbon atoms and can contain one or more oxygen atoms in the chain or bear one or more OH groups or(ii) a (C.sub.8 -C.sub.18 alkyl)phenyl radical.These compounds can be used for preparing stable chemical compounds, for conveying active substances or for forming vesicles.

Abstract: A polypeptide having amino acid sequence 172-192 of a Mycobacterium bovis BCG 64 kD polypeptide, said sequence having the formula ##STR1## as well as polypeptides derived therefrom, in the amino acid sequence of which sequence 172-179 and/or sequence 189-192 is (are) entirely or partially absent, were found to be useful as immunogens inducing resistance to auto-immune arthritis and similar auto-immune diseases.The invention relates to these polypeptides, to polypeptides showing sequential homology with these polypeptides, and to derivatives and multimers thereof. Also, microorganisms expressing the polypeptides either as such or as part of a fusion protein or as a multimer form part of the invention.Finally, the invention relates to pharmaceutical compositions, diagnostic compositions and test kits comprising a compound according to the invention.

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: Molecular conjugates which facilitate the attachment of macromolecular drugs onto cellular surfaces and their entry into cells are described. The molecular conjugates comprise a macromolecular drug linked to an "inactivated" membrane blending agent which inserts into the cellular plasma membrane. The membrane blending agent is inactivated by cleavable linkage to a blocking agent which, until released from the conjugate under appropriate conditions, blocks and ability of the membrane blending agent to insert into the cellular membrane. Upon release of the blocking agent, the membrane blending agent is "activated" and the conjugate can be inserted into a cellular plasma membrane. The membrane blending agents can be peptides such as fusogenic or ion channel forming peptides or long chain fatty acids. The blocking agents can be bulky or charged moieties which mask and prevent insertion of the membrane blending agent.

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: Described is a new class of polypeptide cell modulators characterized by being composed of two covalently linked cell modulators in a linear polypeptide sequence. Such dual function polypeptides have new and particularly useful activities when the component polypeptide cell modulators are interferons, lymphokines or cytotoxins which act through different and specific cell receptors to initiate complementary biological activities.

Abstract: The activity of cytotoxic agents on target cells is enhanced through administration of a sensitizing agent to a patient prior to or simultaneously with administration of the cytotoxic agent. One or both of the two types of agents are attached to antibodies specific for the desired target cells, thereby enhancing the cytotoxic effect on target cells compared to non-target cells. The sensitizer and/or the cytotoxic agent may be attached to monoclonal antibodies specific for cancer cells to selectively eradicate the cancer cells while minimizing toxicity toward normal tissues.

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: Methods and compositions are provided for concentrating particles in a minute area on a solid surface. The method permits the detection of small amounts of analytes by providing for an observable signal in relation to the concentration of particles in the area.