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Distamycins (0):
Recent article
Distamycins
Biophysical Chemistry (149)1-2 2010
Abstract
We have examined the affinity and mode of Dst binding to DNA duplexes containing a conserved A/T core and variable terminal A/T regions by using circular dichroism spectroscopy. The observed circular dichroism spectra were analyzed by singular value decomposition and fitted to a two-step binding mod...
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PMID: 20395035
PDF is available here.
PDF is available here.
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Abstract
The study of DNA G-quadruplex stabilizers has enjoyed a great momentum in the late years due to their application as anticancer agents. The recognition of the grooves of these structural motifs is expected to result in a higher degree of selectivity over other DNA structures. Therefore, to achieve a...
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PMID: 20394365
PDF is available here.
PDF is available here.
Abstract
I and II at a concentration of 50 microM. The ethidium bromide assay showed that these compounds bind to plasmid pBR322, yet weaker than distamycin. Further investigations concerning the mechanism of cytotoxicity are now in progress, but the IC(50) values suggest that synthetic distamycin analogues...
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PMID: 19173336
PDF is available here.
PDF is available here.
Abstract
Derivatives of distamycin A modified at the C-terminal amidine moiety and tethered to bis-epoxyethyl moieties at the N-terminal position were tested for their ability to induce erythroid differentiation in the human erythroleukemic cell line K562. None of the compounds without bis-epoxyethyl moiety...
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PMID: 19082513
PDF is available here.
PDF is available here.
Abstract
We have reported a series of hybrid compounds characterized by the presence of a alpha-halogenocryloyl alkylating moiety of low chemical reactivity, linked to known antitumor agents or their active moieties. Among them, brostallicin (PNU-166196), was selected for clinical development and is now unde...
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PMID: 19149662
PDF is available here.
PDF is available here.
Abstract
Six new aromatic oligopeptides were synthesized and evaluated for their activity in the standard cell line of the mammalian tumor MCF-7 as well as in a cell-free system employing the topoisomerase I/II inhibition assay.
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PMID: 20050527
PDF is available here.
PDF is available here.
Bioconjugate Chemistry (19)12 2008
Abstract
We present the synthesis, photochemical, and DNA binding properties of three photoisomerizable azobenzene-distamycin conjugates in which two distamycin units were linked via electron-rich alkoxy or electron-withdrawing carboxamido moieties with the azobenzene core. Like parent distamycin A, these mo...
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PMID: 18991370
PDF is available here.
PDF is available here.
ChemBioChem (9)17 2008
Abstract
Our work has led to the discovery of synthetic tripyrrole-octa-arginine conjugates that are capable of targeting specific DNA sites that contain A-rich tracts with low nanomolar affinity; they simultaneously exhibit excellent membrane and nuclear translocation properties in living HeLa cells....
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PMID: 18942688
PDF is available here.
PDF is available here.
Abstract
Hydrolysis of DNA is of increasing importance in biotechnology and medicine. In this Letter, we present the DNA-cleavage potential of metal-free hydroxylamines and oximes as new members of nucleic acid cleavage agents.
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PMID: 18667311
PDF is available here.
PDF is available here.
Abstract
The use of small molecules that bind and stabilize G-quadruplex structures is emerging as a promising way to inhibit telomerase activity in tumor cells. In this paper, isothermal titration calorimetry (ITC) and 1H NMR studies have been conducted to examine the binding of distamycin A and its two car...
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PMID: 18420038
PDF is available here.
PDF is available here.
Molecular Microbiology (69)1 2008
Abstract
We evaluated this potential. Downregulation of EhMLBP using antisense technology resulted in trophozoites with impaired growth and cytopathic activity. This indicated that EhMLBP is an essential protein. With a view to identifying new antiamebic agents, we tested the effect of distamycin A, a drug w...
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PMID: 18484949
PDF is available here.
PDF is available here.
Abstract
We have examined the effects of local DNA sequence on the interaction of distamycin, Hoechst 33258, echinomycin, actinomycin and mithramycin with their preferred binding sites using a series of DNA fragments that contain every symmetrical hexanucleotide sequence. In several instances we find that th...
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PMID: 18226601
PDF is available here.
PDF is available here.
Journal of Biochemistry (143)6 2008
Abstract
We show that the sensitivity profiles of E. coli RecQ to a number of DNA-binding ligands are different to those observed for WRN and Bloom helicases. These observations may give insights into the differences in molecular mechanisms underlying efficient motor function of RecQ helicases....
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PMID: 18296713
PDF is available here.
PDF is available here.
FEBS Letters (582)5 2008
Abstract
We blunted the induction of hNOS2 by pro-inflammatory stimuli. Binding of HMGA1 in the region -3506 to -3375 of the hNOS2 promoter, a region not previously known to be involved in hNOS2 regulation, contributed to the induction of hNOS2 promoter in conjunction with upstream enhancer regions. We demon...
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PMID: 18279675
PDF is available here.
PDF is available here.
Abstract
We previously reported that distamycin A, a natural antibiotic known as a minor groove binder, could bind to DNA duplexes containing the (6-4) photoproduct formed at its target site, whereas the binding was not observed for duplexes containing the cis-syn cyclobutane pyrimidine dimer in the same seq...
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PMID: 17950611
PDF is available here.
PDF is available here.
Biochimica et Biophysica Acta (1779)1 2008
Abstract
Fragile sites are heritable specific chromosome loci that exhibit an increased frequency of gaps, poor staining, constrictions or breaks when chromosomes are exposed to partial DNA replication inhibition. They constitute areas of chromatin that fail to compact during mitosis. They are classified as...
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PMID: 18078840
PDF is available here.
PDF is available here.
Intervirology (51)3 2008
Abstract
In spite of the lower activity against ACV-resistant strains, DA may be used as an antiherpetic drug.
Copyright 2008 S. Karger AG, Basel....
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PMID: 18663321
PDF is available here.
PDF is available here.
Abstract
We have analyzed the NMR titration profile of a modified quadruplex, namely [d(TGGMeGGT)]4, and we have applied the recently developed differential frequency-saturation transfer difference (DF-STD) method, for assessing the ligand-DNA binding mode. The three-dimensional structure of the 4:1 distamyc...
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PMID: 18052170
PDF is available here.
PDF is available here.
Biochemistry (Washington) (46)42 2007
Abstract
I footprinting confirmed strict cognate site selectivity and demonstrated that affinity increased with linker length (f-ImPyIm-9 = f-ImPyIm-8 = f-ImPyIm-EG-8 > f-ImPyIm-7 > f-ImPyIm-6). The eight- and nine-linked derivatives bound at 100-fold lower concentrations at the cognate site relative to f-Im...
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PMID: 17910471
PDF is available here.
PDF is available here.
Abstract
A 3D-QSAR analysis has been carried out by comparative molecular field analysis (CoMFA) on a series of distamycin analogs that bind to the DNA of drug-resistant bacterial strains MRSA, PRSP and VSEF. The structures of the molecules were derived from the X-ray structure of distamycin bound to DNA and...
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PMID: 17690925
PDF is available here.
PDF is available here.
Mutation Research (623)1-2 2007
Abstract
An understanding of the mechanism by which minor groove binding agents interact with DNA has led to the design of agents that can reversibly bind with high selectivity to extended DNA target sequences. Simple compounds, such as the polypyrroles and the bis-benzimidazoles, have been used as carriers...
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PMID: 17507044
PDF is available here.
PDF is available here.
Abstract
In the context of the design and synthesis of minor groove binding and intercalating DNA ligands some new oligopyrrole carboxamides were synthesized. These hybrid molecules (combilexins) possess a variable and conformatively flexible spacer at the N-terminal end. As intercalating tricyclic systems a...
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PMID: 17433851
PDF is available here.
PDF is available here.
Abstract
We examined cytotoxic effect of Duo in the coexistence of Dist using human lung carcinoma (HLC-2) cells. The cytotoxicity of Duo to HLC-2 cells was enhanced 10 times by the addition of 0.5microg/ml Dist, which was much lower than the IC(50) value of 16microg/ml. Addition of Duo alone to HLC-2 cells...
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PMID: 17321782
PDF is available here.
PDF is available here.
Abstract
A DNA-binding affinity and the effect on restriction enzymes activity of seven carbocyclic mono- and bis-lexitropsins and two analogues of pentamidine with unsubstituted N-terminal amine group were investigated. DNA association constants (Kapp) show that DNA affinity of mono-compounds is much weaker...
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PMID: 17665860
PDF is available here.
PDF is available here.
Abstract
We plan to use them as templates for forthcoming virtual screening experiments to discover molecules with the same bioactivity and a different scaffold. In this proof of principle study, carried out with the software tool Catalyst, we present a model work for description of a ligand-DNA complex with...
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PMID: 17518460
PDF is available here.
PDF is available here.
Drug Delivery (14)1 2007
Abstract
We describe the production and characterization of specialized delivery systems for some distamycin derivatives (DD), namely liposomes and micellar dispersions. All the formulations were designed to increase the solubility of DD in an aqueous environment and to reduce the possible toxicity problems...
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PMID: 17107925
PDF is available here.
PDF is available here.
Abstract
The DNA minor groove is an attractive target for the design and development of molecules able to specifically recognize predetermined DNA sequences. The pyrrole-amide skeleton of distamycin A has been also used as DNA sequence selective vehicle for the delivery of alkylating functions to DNA targets...
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PMID: 17081759
PDF is available here.
PDF is available here.
Abstract
I footprinting, with compound 7 producing a footprint of 0.1 microM at the expected 5'-ACGCGT-3' site. SPR analysis of compound 7 binding to 5'-ACGCGT-3', 5'-ACCGGT-3', and 5'-AAATTT-3' produced binding affinities of 2.2x10(6), 3.3x10(5), and 1x10(5)M(-1), respectively, indicating a preference for i...
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PMID: 17035029
PDF is available here.
PDF is available here.
Abstract
I footprinting, SPR, and CD studies to bind as a stacked dimer to its cognate sequences: 5'-TACGAT-3' (5'-flank of the inverted CCAAT box-2 of the human topoisomerase IIalpha promoter) and 5'-ATCGAT-3'. A gel shift experiment provided evidence for f-PIP to inhibit protein-DNA interaction at the ICB2...
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PMID: 17011187
PDF is available here.
PDF is available here.
Journal of Biochemistry (140)6 2006
Abstract
We demonstrated that the limited digestion of full-length Dnmt1 with different proteases produced a common N-terminal fragment, which migrated along with Dnmt1 (1-248) in SDS-polyacrylamide gel electrophoresis. Digestion of the N-terminal domains larger than Dnmt1 (1-248) with chymotrypsin again pro...
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PMID: 17046852
PDF is available here.
PDF is available here.
Biochemistry (Washington) (45)45 2006
Abstract
We further characterize f-ImPyIm and f-PyImIm, and we report thermodynamic and structural differences between -ImPy- (f-ImPyIm) and -PyIm- (f-PyImIm) central pairings. DNase I footprinting studies confirmed that f-ImPyIm is a stronger binder than distamycin A and f-PyImIm and that f-ImPyIm preferent...
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PMID: 17087509
PDF is available here.
PDF is available here.
Abstract
A number of amide-linked oligopyrroles based on distamycin molecules have been synthesized by solid-state methods, and their interactions with a human intramolecular G-quadruplex have been measured by a melting procedure. Several of these molecules show an enhanced ratio of quadruplex vs. duplex DNA...
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PMID: 17036143
PDF is available here.
PDF is available here.
Biophysical Journal (91)4 2006
Abstract
Binding of a small molecule to a macromolecular target reduces its conformational freedom, resulting in a negative entropy change that opposes the binding. The goal of this study is to estimate the configurational entropy change of two minor-groove-binding ligands, netropsin and distamycin, upon bin...
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PMID: 16731550
PDF is available here.
PDF is available here.
Biochemical Pharmacology (72)3 2006
Abstract
These results indicate the amidine analogue of melphalan, AB4 represent multifunctional inhibitor of breast cancer cells growth and metabolism....
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PMID: 16730667
PDF is available here.
PDF is available here.
Abstract
We conclude that the binding affinity characteristics of these DNA binding molecules to the RNA conformations are vastly different and may serve as data for the development of RNA based antiviral drugs....
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PMID: 16202606
PDF is available here.
PDF is available here.
FEMS Microbiology Letters (147)1 2006
Abstract
We found a novel DNA curvature, which has changeable bending-center sites of an intrinsic curvature under temperature conditions (CIT) in the cyanobacterium strain Microcystis aeruginosa K-81. Circular permutation analyses (CPA) for CIT under different temperature conditions (4201350°C) revealed tha...
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PMID: 9037772
PDF is available here.
PDF is available here.
Abstract
We reported that distamycin A can bind to DNA containing the (6-4) photoproduct, one of the major UV lesions in DNA, by means of CD spectroscopy. Here, we have analyzed the structure of DNA containing the (6-4) photoproduct in complex with distamycin A by NMR. Broadening of NMR resonances and large...
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PMID: 17150905
PDF is available here.
PDF is available here.
Abstract
We analyzed the binding properties of distamycin A and compared the results with those of the DDB protein. Structural change of the DNA duplex was not observed for distamycin A in two types of experiments, whereas the protein induced a large bending of the helix. Although the substrate specificity w...
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PMID: 17150904
PDF is available here.
PDF is available here.
Nucleic Acids Research (34)1 2006
Abstract
We previously reported the chemical synthesis of oligonucleotides containing thymine glycol, a major form of oxidative DNA damage. In the preparation of the phosphoramidite building block, the predominant product of the osmium tetroxide oxidation of protected thymidine was (5R,6S)-thymidine glycol....
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PMID: 16401612
PDF is available here.
PDF is available here.
Chemotherapy (51)6 2005
Abstract
Tecogalan had no effect even on 639V tumour growth, where bFGF was unaffected. TNP-470 only had an effect on T24 tumours, delaying tumour appearance and growth and lowering VEGF; these effects were augmented by adding minocycline. PNU153429 had no effect on 639V tumours, and a slight effect on T24 t...
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PMID: 16224178
PDF is available here.
PDF is available here.
Journal of Mass Spectrometry (40)10 2005
Abstract
The charge state-dependent dissociation of various DNA duplexes and drug/duplex complexes has been investigated using collisionally activated dissociation (CAD) in a quadrupole ion trap mass spectrometer (QIT-MS). Several non-self-complementary 14-residue oligonucleotides were employed, in addition...
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PMID: 16220501
PDF is available here.
PDF is available here.
Abstract
Sugar-oligoamides have been designed and synthesized as structurally simple carbohydrate-based ligands to study carbohydrate-DNA interactions. The general design of the ligands 1-3 has been done as to favor the bound conformation of Distamycin-type gamma-linked covalent dimers which is a hairpin con...
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PMID: 15984879
PDF is available here.
PDF is available here.
Abstract
We used the combinatorial selection method restriction endonuclease protection, selection, and amplification (REPSA) to determine the DNA-binding specificity of the semisynthetic covalent DNA-binding polyamide tallimustine, which contains a benzoic acid nitrogen mustard appended to the minor groove...
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PMID: 15709763
PDF is available here.
PDF is available here.
Biophysical Journal (88)1 2005
Abstract
We compared the effects of the minor groove binder distamycin-A, a major groove binding alpha-helical peptide, the intercalators ethidium bromide, YO-1, and daunomycin as well as the bisintercalator YOYO-1 on lambda-DNA. Binding of molecules to the minor and major groove of dsDNA induces distinct ch...
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PMID: 15516529
PDF is available here.
PDF is available here.
Annals of Botany (95)2 2005
Abstract
The remarkable variation in chromosome size and number and rDNA sites shows that dramatic karyological changes have occurred during the evolution of the genus at the diploid level. These data further suggest that the two putative basic numbers of the genus, x=9 and x=10, may have arisen two or more...
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PMID: 15567808
PDF is available here.
PDF is available here.
Nucleic Acids Research (33)2 2005
Abstract
Molecular dynamics simulations have been performed on netropsin in two different charge states and on distamycin binding to the minor groove of the DNA duplex d(CGCGAAAAACGCG).d(CGCGTTTTTCGCG). The relative free energy of binding of the two non-covalently interacting ligands was calculated using the...
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PMID: 15687382
PDF is available here.
PDF is available here.
Biophysical Chemistry (111)3 2004
Abstract
We have used DNase I footprinting and fluorescence melting studies to study the interaction of the hairpin polyamide Im-Py-Py-Py-(R)H2Ngamma-Im-Py-Py-Py-beta-Dp with its preferred binding sites (5'-WGWWCW; W=A or T) and other sequences. DNase I footprinting confirmed that the ligand binds to the seq...
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PMID: 15501563
PDF is available here.
PDF is available here.
Abstract
Positive and negative ion electrospray ionization (ESI) mass spectra of complexes of positively charged small molecules (distamycin, Hoechst 33258, [Ru(phen)2dpq]Cl2 and [Ru(phen)2dpqC]Cl2) have been compared. [Ru(phen)2dpq]Cl2 and [Ru(phen)2dpqC]Cl2 bind to DNA by intercalation. Negative ion ESI ma...
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PMID: 15465350
PDF is available here.
PDF is available here.
Journal of Immunology (173)6 2004
Abstract
We and others have previously shown that AT-rich regions of DNA surrounding transcription factor binding sites in the NOS2 promoter are critical for NOS2 induction by inflammatory stimuli in vitro. Therefore, we hypothesized that Dist A would attenuate NOS2 up-regulation in vivo during endotoxemia a...
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PMID: 15356165
PDF is available here.
PDF is available here.
Abstract
We have found that distamycin A can bind to DNA duplexes containing the (6-4) photoproduct, one of the major UV lesions in DNA, despite the changes, caused by photoproduct formation, in both the chemical structure of the base moiety and the local tertiary structure of the helix. A 20-mer duplex cont...
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PMID: 15339187
PDF is available here.
PDF is available here.
Journal of Molecular Biology (342)1 2004
Abstract
Our results reveal several unprecedented ligand-DNA binding features. DST binds to the neighboring 5'-AAGTT-3' and 5'-ATATA-3' sites of D#1 statistically in a 2:1 binding mode. By contrast, its association to D#2 appears to be a 2:1 binding event only at the DST/D#2 molar ratios between 0 and 2 whil...
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PMID: 15313608
PDF is available here.
PDF is available here.
Abstract
We describe an efficient access to a focused library of new analogues yielding compounds with improved activity in a mouse peritonitis model. The most potent molecules (14 and 19) exhibit efficacy against MRSA at ED50 values of approximately 1 and approximately 5 mg/kg, respectively, and display exc...
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PMID: 15317448
PDF is available here.
PDF is available here.
Abstract
Our preliminary results indicated that the compounds of this series have a pattern of alkylation similar to that of tallimustine, but they seem to be less reactive overall in alkylating naked DNA....
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PMID: 15210158
PDF is available here.
PDF is available here.
Abstract
We now report and discuss the synthesis, the in vitro and in vivo activities, and some mechanistic features of alpha-halogenoacrylamido derivatives of distamycin A. The final result of this work was the selection of brostallicin 17 (PNU-166196). Brostallicin, presently in phase II clinical trials, s...
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PMID: 15115402
PDF is available here.
PDF is available here.
Abstract
Abstract
Forty-eight heterocyclic amino acid trimers, analogues of distamycin, with a number of features that enhance lipophilicity are described. They contain alkyl or cycloalkyl groups larger than methyl; some are N-terminated by acetamide or methoxybenzamide and are C-terminated by dimethylaminopropyl or...
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PMID: 15056010
PDF is available here.
PDF is available here.
Journal of Virology (78)4 2004
Abstract
We show here that distamycin is a potent inhibitor of vaccinia virus replication. Pulse-labeling experiments showed that most major late proteins failed to accumulate in the presence of the antibiotic. We characterized the effect of distamycin on vaccinia virus nucleic acid biosynthesis with the goa...
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PMID: 14747579
PDF is available here.
PDF is available here.
Biochemical Pharmacology (67)3 2004
Abstract
We found that these hybrids bind to TAR-RNA and inhibit TAR/protein(s) interactions. The anti-proliferative activity of the hybrids has been tested in vitro on HL3T1 cells and compared to the anti-proliferative effects of the natural product distamycin A and PBD. The effects on HIV-1 LTR directed tr...
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PMID: 15037192
PDF is available here.
PDF is available here.
Abstract
The polyamides based on 4-amino-1-methylpyrrol-2-carboxylic acid, 4-amino-1-methylimidazole-2-carboxylic acid, and beta-alanine that stabilize oligonucleotide duplexes consisting of G x C pairs through parallel packing in the minor groove were studied. The initial duplex TTGCGCp x GCGCAA melts at 28...
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PMID: 15562979
PDF is available here.
PDF is available here.
Drug Delivery (11)2 2004
Abstract
This article describes the production and characterization of two liposome formulations containing antitumor drugs, namely distamycin A (Dist) and a new alkyl derivative of distamycin A (C16-Dist). Egg-PC/cholesterol liposomes (4:1 mol/mol) were prepared by reverse phase evaporation technique follow...
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PMID: 15200006
PDF is available here.
PDF is available here.