133 research outputs found
Antibody-targeted leucinostatin A.
This paper describes chemical modification of the toxic agent Leucinostatin A and its conjugation with a monoclonal antibody. The molecule, isolated from a culture filtrate of Paecilomyces marquandii (Massee) Hughes, is a nonapeptide antibiotic with cytotoxic and phytotoxic properties. To evaluate its toxicity, and to improve its specificity as an antitumor agent, the molecule was conjugated to the monoclonal antibody AR-3, specific to human colorectal and ovarian carcinomas. The targeting ability of AR-3, bearing different amounts of toxic agent, was tested on related and unrelated cell lines. Stability of the ester linkage between Leucinostatin A and AR-3 was also studied.
In this study we show that coupling of Leucinostatin A with a tumor-directed monoclonal antibody is a practical way to increase both the cytotoxicity and selectivity of the chemotherapeutic agent
3-carboxy-4-nitrophenyl-dithio-1,1',2-trisnorsqualene: a site-directed inactivator of yeast oxidosqualene cyclase
Biotyping of micelial fungus cultures by the killer system
Based on the occurrence of the yeast killer phenomenon in hyphomycetes, the toxic effect of 37 selected killer yeasts was studied on eleven strains of Pseudallescheria boydii, six strains of Aspergillus niger, 18 strains of Penicillium camemberti and nine strains of Sporothrix schenckii. The demonstration of different biotypes within the species of P. boydii and P. camemberti proves that the killer system also is a practical and effective method for epidemiological studies among hyphomycetes. Based on the system used, it was not possible to observe markedly different biotypes among the A. niger and S. schenckii strains studied. The first evidence that an isolated, concentrated (50X) and partially purified yeast killer toxin may display a lethal activity against mycelial fungus cultures is also given in this paper
In vitro metabolism of azasqualene derivatives and their effects on aminopyrine N-demethylase activity in rat liver microsomes
Toxin-targeted design for anticancer therapy - Part I. Synthesis and biological evaluation of new thioimidate heterobifunctional reagents
Toxin-targeted design for anticancer therapy - Part II. Preparation and biological comparison of different chemically linked gelonin-antibody CONJUGATES
Synthesis and biological activity of a squalenoid maleimide and other classes of squalene derivatives as irreversible inhibitors of 2,3-oxidosqualene cyclase
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