摘要:
Tubulysin analogs of the formula (I) where R1, R2 R3, R4, R5, R6, R7, and Y are as defined herein, are anti-mitotic agents that can be used in the treatment of cancer, especially when conjugated to a targeting moiety.
摘要:
The present invention concerns methods and compositions for making and using bioactive assemblies of defined compositions, which may have multiple functionalities and/or binding specificities. In particular embodiments, the bioactive assembly is formed using dock-and-lock (DNL) methodology, which takes advantage of the specific binding interaction between dimerization and docking domains (DDD) and anchoring domains (AD) to form the assembly. In various embodiments, one or more effectors may be attached to a DDD or AD sequence. Complementary AD or DDD sequences may be attached to an adaptor module that forms the core of the bioactive assembly, allowing formation of the assembly through the specific DDD/AD binding interactions. Such assemblies may be attached to a wide variety of effector moieties for treatment, detection and/or diagnosis of a disease, pathogen infection or other medical or veterinary condition.
摘要:
The present invention provides a novel anti-AIDS immunotoxin. The immunotoxin comprises a toxin chemically conjugated to a monoclonal antibody directed against viral reverse transcriptase. Also provided are various methods of using this novel immunotoxin including methods of treating various diseases.
摘要:
The present invention relates to a toxin conjugate in which a residue derived from a compound having an affinity for a target cell is bound to a toxin through a spacer comprising polyalkylene glycol and dipeptide.
摘要:
The present invention relates generally to methods and compositions for targeting the vasulature of solid tumors using immunologcially-based reagents. In particular aspects, antibodies carrying diagnostic or therapeutic agents are targeted to the vasculature of solid tumor masses through recognition of tumor vasculature-associated antigens, or through the specific induction of endothelial cell surface antigens on vascular endothelial cells in solid tumors.
摘要:
Therapeutic agents and methods for treating and diagnosing acute or chronic leukemia are provided. Such agents comprises monoclonal antibody M195, or a chimeric antibody containing the hypervariable region of M195, conjugated to a cytotoxic agent, e.g. a radioisotope.
摘要:
An antiviral protein having an amino acid sequence represented by sequence No. 8 of a Sequence Listing is disclosed. The protein is obtained such that cysteine residues in the basic protein (MAP) obtained from Mirabilis jalapa and having antiviral activity are substituted with serine residues. More specifically, a MAP gene in which codons encoding cysteines are substituted with codons encoding serines is prepared, and this gene is integrated in a MAP secretion vector. This vector is introduced into a host to express the gene, thereby obtaining the antiviral protein. This protein retains MAP advantages as a toxic protein and has higher protein synthesis inhibition activity than that of MAP, and almost equal to that of a lysine A chain.
摘要:
Disclosed is a novel recombinant human lyphotoxin (LT) mutein which combines with an antibody at an inactive site of an LT molecule and liberates the LT molecule easily from the antibody after incorporation of the mutein into tumor cells.The recombinant human LT mutein is prepared by introducing a polydeoxyribonucleic acid containing a nucleotide sequence coding for the particular amino acid sequence into a replicable vector, transforming a microorganism or a cell with the recombinant DNA thus obtained, and cultivating the resulting transformant to express genetic information of the polydeoxyribonucleic acid.The recombinant human LT mutein is useful for tumor-selective carcinostatics, and effective for increasing the actively of LT and reducing the side effects thereof.
摘要:
A cell-specific toxin molecule is prepared containing an enzymatically active toxin moiety coupled to a cell-specific binding ligand. The toxin moiety may be a diphtheria toxin, and has a non-naturally occurring cysteine residue encoded by a DNA sequence including a non-naturally occurring cysteine codon. The ligand may be a peptide hormone, proteinaceous growth factor, antibody of steroid hormone, and is derivatized with a sulfhydryl group reactive with the cysteine residue of the toxin moiety to couple the ligand to the toxin moiety via a disulfide bond. Derivatization of the ligand may be by providing the ligand with a non-naturally occurrring cysteine residue encoded by a DNA sequence including a non-naturally occurring cysteine codon. The toxin moiety exhibits cytotoxic activity but fails to exhibit generalized eukaryotic cell binding, and may be used to treat medical disorders.
摘要:
The invention relates to a method of detecting an inflammation site in an individual by administering to the individual a diagnostically effective amount of detectably labeled immunoglobulin or fragment thereof, wherein the immunoglobulin substantially accumulates at the site when the site is inflamed.