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The Journal of Biological Chemistry Sep 1985Macromomycin, an antibiotic and antitumor protein obtained from Streptomyces macromomyceticus, displayed specific aminopeptidase activity. Pure macromomycin degraded the...
Macromomycin, an antibiotic and antitumor protein obtained from Streptomyces macromomyceticus, displayed specific aminopeptidase activity. Pure macromomycin degraded the beta-chain of insulin, a few synthetic di- and tripeptides, and a number of proteins of KB cell plasma membrane. The biological activity and the peptidase activity showed similar temperature-dependent patterns suggesting that one protein is responsible for both activities. The apoprotein contained the aminopeptidase activity while the chromophore, which displayed the antibiotic and antitumor activity, did not show any such activity.
Topics: Amino Acids; Anti-Bacterial Agents; Antibiotics, Antineoplastic; Apoproteins; Cell Line; Cell Membrane; Chromatography, High Pressure Liquid; Humans; Peptide Hydrolases; Peptides
PubMed: 3900063
DOI: No ID Found -
The Journal of Antibiotics Nov 1981Fredericamycin A is a novel antibiotic produced by a soil isolate of Streptomyces griseus (FCRC-48). In vitro, fredericamycin A exhibits antibacterial, antifungal, and...
Fredericamycin A is a novel antibiotic produced by a soil isolate of Streptomyces griseus (FCRC-48). In vitro, fredericamycin A exhibits antibacterial, antifungal, and cytotoxic activities. In vivo, fredericamycin A exhibits very good antitumor activity against P388 mouse leukemia as well as the CD8F mammary tumor and marginal activity against B16 melanoma. Fredericamycin A failed to demonstrate any interaction with DNA and inhibited protein and RNA synthesis preferentially to DNA synthesis in Bacillus subtilis and P388 cells.
Topics: Animals; Antibiotics, Antineoplastic; Bacteria; Chemical Phenomena; Chemistry; DNA; Isoquinolines; Mice; Microbial Sensitivity Tests; Mutagens; Neoplasms, Experimental; Spiro Compounds
PubMed: 7319903
DOI: 10.7164/antibiotics.34.1402 -
The Journal of Antibiotics Jun 1979The structure of nocamycin, a new antitumor antibiotic, has been elucidated with the aid of mass- and PMR-spectroscopic investigation of the antibiotic and its various...
The structure of nocamycin, a new antitumor antibiotic, has been elucidated with the aid of mass- and PMR-spectroscopic investigation of the antibiotic and its various chemical transformation products. Nocamycin is structurally related to tirandamycins.
Topics: Antibiotics, Antineoplastic; Chemical Phenomena; Chemistry; Magnetic Resonance Spectroscopy; Mass Spectrometry
PubMed: 468730
DOI: 10.7164/antibiotics.32.555 -
Cell Apr 1997The Hsp90 chaperone is required for the activation of several families of eukaryotic protein kinases and nuclear hormone receptors, many of which are protooncogenic and...
The Hsp90 chaperone is required for the activation of several families of eukaryotic protein kinases and nuclear hormone receptors, many of which are protooncogenic and play a prominent role in cancer. The geldanamycin antibiotic has antiproliferative and antitumor effects, as it binds to Hsp90, inhibits the Hsp90-mediated conformational maturation/refolding reaction, and results in the degradation of Hsp90 substrates. The structure of the geldanamycin-binding domain of Hsp90 (residues 9-232) reveals a pronounced pocket, 15 A deep, that is highly conserved across species. Geldanamycin binds inside this pocket, adopting a compact structure similar to that of a polypeptide chain in a turn conformation. This, and the pocket's similarity to substrate-binding sites, suggest that the pocket binds a portion of the polypeptide substrate and participates in the conformational maturation/refolding reaction.
Topics: Amino Acid Sequence; Animals; Antibiotics, Antineoplastic; Benzoquinones; Cattle; Conserved Sequence; Crystallography, X-Ray; HSP90 Heat-Shock Proteins; Humans; Lactams, Macrocyclic; Models, Molecular; Molecular Sequence Data; Protein Binding; Protein Conformation; Quinones; Sequence Alignment
PubMed: 9108479
DOI: 10.1016/s0092-8674(00)80203-2 -
The Journal of Antibiotics Sep 1989Phospholine, an antitumor antibiotic, has the molecular formula of C25H40NO8P and possesses a delta-lactone and a phosphoric acid ester as functional groups. Its...
Phospholine, an antitumor antibiotic, has the molecular formula of C25H40NO8P and possesses a delta-lactone and a phosphoric acid ester as functional groups. Its structure was determined based on interpretation of fast atom bombardment MS, 1H NMR, 13C NMR, 1H-1H correlation spectroscopy (COSY), 13C-1H COSY, heteronuclear multiple bond correlation spectroscopy, elemental analysis and chemical modifications.
Topics: Antibiotics, Antineoplastic; Chemical Phenomena; Chemistry; Lactones; Magnetic Resonance Spectroscopy; Organophosphorus Compounds
PubMed: 2793587
DOI: 10.7164/antibiotics.42.1339 -
The Journal of Antibiotics Jul 1981An antibiotic, identical with or closely related to xanthomycin A, was isolated from a soil Streptomyces. The antibiotic displayed significant therapeutic activity by...
An antibiotic, identical with or closely related to xanthomycin A, was isolated from a soil Streptomyces. The antibiotic displayed significant therapeutic activity by i.p. administration against i.p.-implanted mouse tumors: Ehrlich carcinoma, sarcoma 180 and P388 leukemia. Less therapeutic activity was observed by i.p. injection in mice bearing s.c. solid tumors of Ehrlich carcinoma and sarcoma 180. No significant activity was found against L1210 leukemia, B16 melanoma and Lewis lung carcinoma. In vitro the antibiotic exhibited a potent cytotoxicity to human leukemia K562 and mouse lymphoblastoma L5178Y cells. DNA strand scission of PM2 phage was caused by the antibiotic in the presence of dithiothreitol.
Topics: Animals; Antibiotics, Antineoplastic; Biguanides; Cell Survival; Cells, Cultured; DNA; Humans; Mice; Neoplasms, Experimental; Soil Microbiology; Streptomyces; Tetracyclines
PubMed: 7287588
DOI: 10.7164/antibiotics.34.856 -
The Journal of Antibiotics Oct 1988A new antitumor antibiotic porothramycin was produced by a new strain of Streptomyces albus. The antibiotic was isolated in two active forms, the natural free hydroxyl...
A new antitumor antibiotic porothramycin was produced by a new strain of Streptomyces albus. The antibiotic was isolated in two active forms, the natural free hydroxyl form (porothramycin A) or the crystalline methyl ether form (porothramycin B) depending upon the isolation process used. Structural studies established that porothramycin is a new member of the pyrrolo[1,4]benzodiazepine group antibiotics having only one substituent on the benzene ring. The antibiotic exhibited antimicrobial activity against Gram-positive bacteria and anaerobes and significantly prolonged the survival times of mice implanted with experimental tumors.
Topics: Animals; Anthramycin; Antibiotics, Antineoplastic; Benzodiazepinones; Chemical Phenomena; Chemistry; Gram-Positive Bacteria; Hydrolysis; Leukemia L1210; Leukemia P388; Magnetic Resonance Spectroscopy; Melanoma, Experimental; Mice; Microbial Sensitivity Tests; Streptomyces
PubMed: 3192492
DOI: 10.7164/antibiotics.41.1366 -
The Journal of Antibiotics Nov 1989Compounds AT2433-A1 (A1), AT2433-A2 (A2), AT2433-B1 (B1), and AT2433-B2 (B2) were isolated from the cultured broth of Actinomadura melliaura sp. nov. (SCC 1655)....
AT2433-A1, AT2433-A2, AT2433-B1, and AT2433-B2 novel antitumor antibiotic compounds produced by Actinomadura melliaura. Taxonomy, fermentation, isolation and biological properties.
Compounds AT2433-A1 (A1), AT2433-A2 (A2), AT2433-B1 (B1), and AT2433-B2 (B2) were isolated from the cultured broth of Actinomadura melliaura sp. nov. (SCC 1655). Structurally these materials are closely related to rebeccamycin (1), an indolocarbazole antitumor antibiotic. A1, A2, B1, and B2 were active against Staphylococcus aureus A9537, Streptococcus faecalis A20688, Streptococcus faecium (ATCC 9790), Micrococcus lutea (ATCC 9341), Bacillus subtilis (ATCC 6633). A1 and B1 were active against P388 leukemia in mice.
Topics: Aminoglycosides; Animals; Anti-Bacterial Agents; Antibiotics, Antineoplastic; Carbazoles; Chemical Phenomena; Chemistry, Physical; Chromatography, Gel; Chromatography, High Pressure Liquid; Fermentation; Indoles; Leukemia P388; Mice; Microbial Sensitivity Tests; Molecular Structure; Nocardiaceae; Soil Microbiology
PubMed: 2584136
DOI: 10.7164/antibiotics.42.1547 -
The Journal of Antibiotics Nov 1981A new antitumor antibiotic, fredericamycin A (FCRC-A48, NSC-305263), has been isolated from a strain of Streptomyces griseus (FCRC-48). Based on its unique...
A new antitumor antibiotic, fredericamycin A (FCRC-A48, NSC-305263), has been isolated from a strain of Streptomyces griseus (FCRC-48). Based on its unique ultraviolet-visible spectrum, infrared spectrum, proton and carbon-13 nuclear magnetic resonance spectra and mass spectra, it is judged to be a novel acid-base indicator type of compound. Its production, isolation and physicochemical properties are discussed. The isolation, ultraviolet-visible spectrum and some biological properties of two minor components, fredericamycin B and fredericamycin C, are also described.
Topics: Antibiotics, Antineoplastic; Chemical Phenomena; Chemistry, Physical; Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Fermentation; Isoquinolines; Spiro Compounds; Streptomyces griseus
PubMed: 6798004
DOI: 10.7164/antibiotics.34.1389 -
The Journal of Antibiotics Dec 1987The LL-D05139 complex, containing LL-D05139 beta and azaserine, was recovered from the fermentation filtrate of Glycomyces harbinensis (NRRL 15337). A chemically defined...
The LL-D05139 complex, containing LL-D05139 beta and azaserine, was recovered from the fermentation filtrate of Glycomyces harbinensis (NRRL 15337). A chemically defined medium was developed which favored the production of LL-D05139 beta. Antibiotic LL-D05139 beta was isolated from the fermentation filtrate by adsorption on granular carbon and further purified by chromatography on microcrystalline cellulose. Acid hydrolysis of LL-D05139 beta gave one molar equivalent each of alanine and serine. Both amino acids were found to have the L-configuration by GC analysis on a chiral column and alanine was assigned to be the N-terminal amino acid by Edman degradation. This information coupled with IR, UV, 1H NMR, 13C NMR and MS spectral data allowed us to assign the structure of LL-D05139 beta as alanylazaserine. LL-D05139 beta demonstrated greater antibacterial and biochemical induction assay activities than azaserine. The two drugs showed similar antitumor activities.
Topics: Antibiotics, Antineoplastic; Azaserine; DNA Damage; Fermentation; Fungi; Magnetic Resonance Spectroscopy; Microbial Sensitivity Tests; Soil Microbiology; Spectrophotometry, Infrared; Spectrophotometry, Ultraviolet
PubMed: 3429335
DOI: 10.7164/antibiotics.40.1657