摘要:
A method for in-vivo targeting a functional moiety in a patient by administering a targeting moiety coupled to an affinity component, wherein the targeting moiety has affinity for binding sites in a target area, and administering a binding partner to the affinity component coupled to a functional moiety to localize the functional moiety in the target area. Preferably the targeting moiety is an antibody and the functional moiety is a radiometal when performing in vivo imaging or therapy. The affinity component may be a novel methotrexate analog. Preferably, the affinity component is thermo-stabilized.
摘要:
Site-specific heterobifunctional crosslinkers of the formula:X--COCH(NH.sub.2)--Y--Zwhere X is a carbonyl reactive group, Y is a variable length spacer, and Z is a thiol reactive group, are useful for the specific labelling of biomolecules or bioaffecting molecules.
摘要:
A modified human complement C3 protein (C3) is disclosed comprising a substitution of a portion of a human C3 protein, with a corresponding portion of a Cobra Venom Factor protein (CVF) which results in a human C3 protein with CVF functions, but with substantially reduced immunogenicity. Advantageously, the C3 protein can be manipulated to contain at least one of the following CVF functions: increased stability of the C3 convertase and increased resistance to the actions of factors H and/or I. A large number of hybrid C3 proteins containing substitutions in the C-terminal portion of the alpha chain of C3 are presented and tested for the above functions. Methods of treatment of diseases such as reperfusion injury, autoimmune diseases, and other diseases of increased complement activation are presented as well as methods of increasing the effectiveness of gene therapeutics and other therapeutics.
摘要:
Ligand-label conjugates which are an oligopeptide of 5 to 100 amino acid residues, bonded to a ligand or receptor, which contain a plurality of chemiluminescent or fluorescent labels and a plurality of polyoxoanions of sulfur or phosphorus are useful for immunoassays. Such conjugates are hydrophilic and exhibit very low nonspecific binding, thereby significantly increasing the signal to background ratio in immunoassays.
摘要:
A novel functionally active derivative of cobra venom factor is described in which the .beta.-chain has been cleaved by treatment with a protease. Gel electrophoretic analyses of the purified derivative revealed the absence of an intact .beta.-chain and a decrease of the molecular weight.
摘要:
A method for site-specific in-vivo activation of a prodrug in an animal using an activator-targeting moiety conjugate to localize an activator at a predetermined site of use and a prodrug compound that is converted to an active drug in the presence of the activator. In the preferred embodiment, the targeting moiety, the activator, and the prodrug demonstrate little or no immunogenicity in the animal being treated. The targeting moiety is relatively specific for binding to the target tissue than to non-target tissue. The activator is not found or present in only small amounts in circulation or in non-target tissue, does not have a substrate for its activity in circulation or in non-target tissue, can be linked to the targeting moiety, and is capable of converting the prodrug to an active drug. The prodrug is selected for its ability to exert a cytotoxic activity on the target tissue after conversion by the activator.