Bleomycins labelled

Wojcik A, Opalka B, Obe G (1999) Analysis of inversions and sister chromatide exchanges in chromosome 3 of human lymphocytes exposed to X-rays. Mutagenesis 14 633-637 Wojcik A, von Sonntag C, Obe G (2003) Application of the biotin-dUTP chromosome-labelling tech-nigue to study the role of 5-bromo-2 -deoxyuridine in the formation of UV-induced sister chromatid exchanges in CHO cells. J Photochem Photobiol B Biol 69 139-144 Wu JC, Kozarich JW, Stubbe J (1983) The mechanism of free base formation from DNA by bleomycin. J Biol Chem 258 4694-4697... 

Table III. Comparison of the Uptake of 57Co—Bleomycin, mIn—BLEDTA, and a Doubly Labeled Compound with mIn in the EDTA Moiety and 57Co Bound to the Bleomycin Moiety0...

Un 2.8 days (K, y) In(III)-bleomycin In(III)-oxine Tumor detection Labeled leukocytes (abscesses, infections, inflammations), labeled platelets (thrombosis, transplant rejection)... 

Haslett, C., Shen, A.S., Feldsien, D.C., Allen, D., Henson, P.M. and Cherniack, R.M. (1989b). " Indium-labelled neutrophil flux into the lungs of bleomycin-treated rabbits assessed non-invasively by external scintigraphy. Am. Rev. Respir. Dis. 140, 756-763. 

McGall, G. H., and J. Stubbe. Mechanistic studies of bleomycin-mediated DNA cleavage using isotope labeling. Nucl. Acids Mol. Biol. 2 (1989), 85-104. 

The spectral properties and conformational preferences of some 1 jB -thiadiazole macrocycles have been reported. In connection with thiazoles we find mention of a useful reagent for the spectro-photometric determination of cobalt, 4C labelling of a new B-adrenergic blocking agent, S-596, and synthesis of analogues of the cationic terminus of the antitumour agent Bleomycin A21 . Additionally, a polymer-supported thiazolium salt catalyst, as a model for the thiamine-dependent enzymes, has been prepared, and three 2-alkylbenzothiazole volatile flavour constituents... 

Bleomycin (Blm) is a natural product that is in regular use in combination chemotherapy. The left side of its structure contains a versatile metal-binding domain, probably composed of five labeled nitrogens (Figure 1). The right side includes a bithiazole moiety and a positively charged, variable R group, which can bind to DNA. A well-defined role for the disaccharide unit has yet to be established. 

Derivatization of samples with an equimolar mixture of labeled and unlabeled reagents to produce ion clusters has been applied recently to the characterization of the bleomycins by FD and FAB mass spectrometry. A variation of this technique utilizes a mixture of labeled and unlabeled reagent gases pyridine/[ Hs]pyridine, trimethylchlorosilane (TMCS)/ [ HsJTMCS, tetramethylsilane (TMS)/[ HizITMS," and NHa/N Ha in conjunction with Cl mass spectral analyses. The isotope cluster technique also may be exploited with the newer ionization methods of SIMS and FAB through the addition of appropriate counter-ions (for example, Ag " ). 

The major uses of lndlum-111 in medicine are listed in Table 2. Indium-111 labeled DTPA is the preferred agent for the study of cerebral spinal fluid kinetics (cisternography)( ). Indium-labeled bleomycin has been used for tumor scanning C2.), although citrate has achieved greater clinical use. It appears that indium bleomycin is in fact a weak chelate and the in vivo distribution is very similar to that of indium transferrin. 

C4 -hydrogen atom abstraction yields the alkaline-labile, oxidized abasic site (C4-AP). Isotopic labelling mled out bleomycin formation of C4-AP via an oxygen rebound-type mechanism, and instead oxidation of 44 and trap-ping of the carbocation (47) by H2O was invoked (Scheme 20). How-... 

A phase of epithelial cell proliferation, as measured by labelled nuclei in autoradiographs, was coincident with peak basement membrane degradative activity in Sprague-Dawley rats 2 weeks after intratracheal bleomycin (Bakowska and Adams 1998). 

The large kinetic isotope effect observed in the oxidation of d-[6- H] galactose by galactose oxidase has been exploited to increase its specific activity. As the unlabelled substrate is oxidised faster, incomplete oxidation leaves the starting material enriched in labelled component. In the Bleomycin-mediated oxidative degradation of DNA, 2 -deo qr-4 -pentulose is released. A mechanistic study with 0-labeIled O2 and H2O revealed that the solvent is the source of the 4 -carbonyl oxygen atom. ... 

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