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Methods in Enzymology 2009The myosin superfamily consists of more than 35 classes (each consisting of multiple isoforms) that have diverse cellular activities. The reaction pathway of the...
The myosin superfamily consists of more than 35 classes (each consisting of multiple isoforms) that have diverse cellular activities. The reaction pathway of the actin-activated myosin ATPase appears to be conserved for all myosin isoforms, but the rate and equilibrium constants that define the ATPase pathway vary significantly across the myosin superfamily, resulting in kinetic differences that that allow myosins to carry out diverse mechanical functions. Therefore, it is important to determine the lifetimes and relative populations of the key biochemical intermediates to obtain an understanding of a particular myosin's cellular function. This chapter provides procedures for determining the overall and individual rate and equilibrium constants of the actomyosin ATPase cycle, including actomyosin binding and dissociation, ATP binding, ATP hydrolysis, phosphate release, and ADP release and binding. Many of the methods described in the chapter are applicable to the characterization of other ATPase enzymes.
Topics: Animals; Computer Simulation; Dactinomycin; Enzyme Stability; Humans; Kinetics; Myosins; Protein Binding; Thermodynamics
PubMed: 19289206
DOI: 10.1016/S0076-6879(08)04206-7 -
Journal of Natural Products Oct 2016Four new Y-type actinomycin analogues named Y-Y (1-4) were isolated and characterized from the scale-up fermentation of the Streptomyces sp. strain Gö-GS12, as well as...
Four new Y-type actinomycin analogues named Y-Y (1-4) were isolated and characterized from the scale-up fermentation of the Streptomyces sp. strain Gö-GS12, as well as actinomycin Zp (5), which was, for the first time, isolated as a natural product. Structures of the new compounds were elucidated by the cumulative analyses of NMR spectroscopy and HRMS. The 4-hydroxythreonine on the β-ring of 1 uniquely undergoes both a rearrangement by a 2-fold acyl shift and an additional ring closure with the amino group of the phenoxazinone chromophore, and the α-rings of 4 and 5 contain a rare 5-methyl proline. Compounds 2-5 showed potent antibacterial activities against Gram-positive bacteria that correlated with cytotoxicity against representative human cell lines. The combination of a β-ring rearrangement and additional ring closure in 1 rendered this actinomycin significantly less potent relative to the nonrearranged comparator actinomycin Y and other actinomycins.
Topics: Anti-Bacterial Agents; Cell Survival; Dactinomycin; Fermentation; Humans; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Proline; Streptomyces; Threonine
PubMed: 27736087
DOI: 10.1021/acs.jnatprod.6b00742 -
International Journal of Molecular... Nov 2021() is a common pathogen that causes various serious diseases, including chronic infections. Discovering new antibacterial agents is an important aspect of the...
() is a common pathogen that causes various serious diseases, including chronic infections. Discovering new antibacterial agents is an important aspect of the pharmaceutical field because of the lack of effective antibacterial drugs. In our research, we found that one anti- substance is actinomycin D, originating from (); then, we further focused on the anti- ability and the omics profile of in response to actinomycin D. The results revealed that actinomycin D had a significant inhibitory activity on with a minimum inhibitory concentration (MIC) of 2 μg/mL and a minimum bactericidal concentration (MBC) of 64 μg/mL. Bacterial reactive oxygen species (ROS) increased 3.5-fold upon treatment with actinomycin D, as was measured with the oxidation-sensitive fluorescent probe DCFH-DA, and HO increased 3.5 times with treatment by actinomycin D. Proteomics and metabolomics, respectively, identified differentially expressed proteins in control and treatment groups, and the co-mapped correlation network of proteomics and metabolomics annotated five major pathways that were potentially related to disrupting the energy metabolism and oxidative stress of . All findings contributed to providing new insight into the mechanisms of the anti- effects of actinomycin D originating from
Topics: Anti-Bacterial Agents; Dactinomycin; Metabolomics; Proteomics; Reactive Oxygen Species; Staphylococcus aureus; Streptomyces
PubMed: 34830114
DOI: 10.3390/ijms222212231 -
Archives of Dermatology Jan 1967
Topics: Animals; Cryptococcosis; Dactinomycin; Epidermophyton; Fungi; Mice
PubMed: 6016301
DOI: No ID Found -
Journal of Veterinary Internal Medicine 1994Fifty dogs with advanced malignancies were treated with actinomycin D at doses ranging from 0.5 to 1.1 mg/m2 every 3 weeks. The greatest number of responses was noted in...
Fifty dogs with advanced malignancies were treated with actinomycin D at doses ranging from 0.5 to 1.1 mg/m2 every 3 weeks. The greatest number of responses was noted in dogs with lymphoma, including dogs that had received prior chemotherapy. Other responding tumor types included anal sac adenocarcinoma, perianal adenocarcinoma, squamous cell carcinoma, thyroid carcinoma, and transitional cell carcinoma. The median time to maximum response for dogs with lymphoma was 7 days, with a median duration of 42 days. Gastrointestinal toxicity was the most frequently observed side effect. A dose of 0.6 to 0.7 mg/m2 appears to be appropriate for treating various malignancies in dogs.
Topics: Animals; Carcinoma; Dactinomycin; Dog Diseases; Dogs; Female; Lymphoma; Male; Neoplasms; Treatment Outcome
PubMed: 8064663
DOI: 10.1111/j.1939-1676.1994.tb03224.x -
Proceedings of the Society For... Oct 1969
Topics: Animals; Cyclophosphamide; Dactinomycin; Erythrocytes; Female; Malaria; Mice; Plasmodium
PubMed: 5344828
DOI: 10.3181/00379727-132-34172 -
Journal of Medicinal Chemistry Dec 1975The synthesis and biological activity of three 7-substituted actinomycin D derivatives are reported. Three such derivatives, 7-nitro-, 7-amino-, and 7-hydroxyactinomycin...
The synthesis and biological activity of three 7-substituted actinomycin D derivatives are reported. Three such derivatives, 7-nitro-, 7-amino-, and 7-hydroxyactinomycin D, were synthesized via new methods which were first tested successfully with a chromophore model system. Of these, 7-nitro- and 7-aminoactinomycin D were assayed for growth inhibitory activity against mammalian cells (CCRF-CEM human lymphoblastic leukemia) in vitro and against the Ridgway osteogenic sarcoma and the L1210, P1534, and P388 murine leukemias in vivo. In these systems, the inhibitory activity of the 7-substituted analogs was comparable to actinomycin D. In two bacterial systems ( (L. casei and L. arabinosus) in vitro, on the other hand, these compounds showed inhibitory profiles which are distinctly different from actinomycin D. These studies demonstrate that substitution at the 7 position, which does not interfere with DNA binding, is capable of yielding experimental antitumor agents with significant activity against a variety of tumors.
Topics: Animals; Dactinomycin; Humans; Lactobacillus; Leukemia L1210; Leukemia, Experimental; Magnetic Resonance Spectroscopy; Mice; Mice, Inbred Strains; Osteosarcoma; Sarcoma, Experimental; Structure-Activity Relationship
PubMed: 1059773
DOI: 10.1021/jm00246a001 -
American Journal of Clinical Pathology Aug 1969
Topics: Animals; Antibiotics, Antineoplastic; Chemical Phenomena; Chemistry; Culture Techniques; DNA Replication; Dactinomycin; Humans; Models, Chemical; RNA
PubMed: 5798361
DOI: 10.1093/ajcp/52.2.130 -
Postepy Higieny I Medycyny... 2005For over 60 years, actinomycins, well-known antibacterial and anticancer antibiotics, have been the subject of the scientific research. These compounds exhibit high... (Review)
Review
For over 60 years, actinomycins, well-known antibacterial and anticancer antibiotics, have been the subject of the scientific research. These compounds exhibit high toxicity and therefore are not widely used in the chemotherapeutic treatment of antibacterial and antifungal diseases. However, actinomycin D, the best-known compound from the actinomycin group, has been introduced into clinical practice as an anticancer drug. Actinomycin D, together with 7-amino-actinomycin D, also became a useful tool in biochemistry and molecular biology. The isolation, production, chemistry, and biological and clinical use of the actinomycins have been thoroughly investigated. Many derivatives of actinomycins, differing in chemical structure as well as biological activity, have been isolated and synthesized and their modifications involved not only the chromphoric phenoxazone ring, but also two cyclic pentapeptide lacton rings. Modifications of the actinomycins' chromophore mainly concerned introducing an amino group in position 2 and a carbon atom in position 7, but also modifications in positions 4, 6, and 8 of the phenoxazone ring. The actinomycin peptide moiety was mainly modified by replacement of amino acids in the pentapeptide rings and also by the synthesis of actinomycin derivatives with open peptide lacton rings. These modifications enabled separating the elements in the actinomycin structure which are responsible for the biological activity of these compounds. That was key information for recognizing the performance of these compounds, and an important way of planning effective new chemotherapeutics.
Topics: Animals; Antibiotics, Antineoplastic; Dactinomycin; Humans; Structure-Activity Relationship
PubMed: 15995594
DOI: No ID Found -
Marine Drugs Dec 2021Actinomycins as clinical medicine have been extensively studied, while few investigations were conducted to discover the feasibility of actinomycins as antimicrobial...
Actinomycins as clinical medicine have been extensively studied, while few investigations were conducted to discover the feasibility of actinomycins as antimicrobial natural dye contributing to the medical value of the functional fabrics. This study was focused on the application of actinomycin X2 (Ac.X2), a peptide pigment cultured from marine-derived , in the dyeing and finishing of silk fabric. The dyeing potential of Ac.X2 with silk vs. cotton fabrics was assessed. As a result, the silk fabric exhibited greater uptake and color fastness with Ac.X2. Through Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), and X-ray diffraction (XRD) analyses, some changes of chemical property for the dyed fabric and Ac.X2 were studied. The silk fabric dyed with Ac.X2 exhibited good UV protection ability. The antibacterial properties of dyed and finished silk were also evaluated, which exhibited over 90% antibacterial activity even after 20 washing cycles. In addition, the brine shrimp assay was conducted to evaluate the general toxicity of the tested fabric, and the results indicated that the dyed silk fabrics had a good biological safety property.
Topics: Animals; Anti-Bacterial Agents; Aquatic Organisms; Artemia; Coloring Agents; Dactinomycin; Microbial Sensitivity Tests; Microscopy, Electron, Scanning; Silk; Spectroscopy, Fourier Transform Infrared; Staphylococcus aureus; Streptomyces
PubMed: 35049871
DOI: 10.3390/md20010016