TY - JOUR. T1 - Molecular and cellular toxicological profiling of DNA bis-intercalator, quinoxaline compounds. T2 - echinomycin as the versatile lead. AU - Park, Yoon Sun. AU - Shin, Woon Seob. AU - Kim, Cheol Su. AU - Ahn, Chan Mug. AU - Qi, Xu Feng. AU - Kim, Soo-Ki. PY - 2018/1/1. Y1 - 2018/1/1. N2 - Of quinoxaline compounds, echinomycin is classically known as an antitumor agent which binds to DNA via a mechanism of bis-intercalation. In addition to intercalation, quinoxaline compounds such as echinomycin, echinomycin derivatives or analogues might control anomalous cellular proliferation in eukaryotes via specifically triggering cellular signaling pathways in mitochondria, as well as under hypoxia. Further, since echinomycin was proven to be a specific inhibitor of HIF-1α, these novel mechanisms could be clinically applied in the development of therapeutics against cancer, infection, obesity, fibrosis, and autoimmune disease. Herein, this review focuses on the current toxicological ...
A Hoogsteen base pair is a variation of base-pairing in nucleic acids such as the A•T pair. In this manner, two nucleobases, one on each strand, can be held together by hydrogen bonds in the major groove. A Hoogsteen base pair applies the N7 position of the purine base (as a hydrogen bond acceptor) and C6 amino group (as a donor), which bind the Watson-Crick (N3-N4) face of the pyrimidine base. Ten years after James Watson and Francis Crick published their model of the DNA double helix, Karst Hoogsteen reported a crystal structure of a complex in which analogues of A and T formed a base pair that had a different geometry from that described by Watson and Crick. Similarly, an alternative base-pairing geometry can occur for G•C pairs. Hoogsteen pointed out that if the alternative hydrogen-bonding patterns were present in DNA, then the double helix would have to assume a quite different shape. Hoogsteen base pairs are, however, rarely observed. Hoogsteen pairs have quite different properties ...
In the paper by Waring and Makoff, "Breakdown of Pulse-Labeled Ribonucleic Acid and Polysomes in Bacillus megaterium: Actions of Streptolydigin, Echinomycin, and Triostins," Vol. 10, No. 2, March 1974, pp. 214-224, Figs. 1 and 3 were transposed. The legends are correct on the pages where they stand, but the illustration printed as Fig. 1 should appear on p. 219 and the one printed as Fig. 3 should appear on p. 217.. ...
Hossain, MB and Helm, Dick Van der and Olsen, Richard K and Jones, Peter G and Sheldrick, George M and Egert, Ernst and Kennard, Olga and Waring, Michael J and Viswamitra, MA (1982) Crystal and molecular structure of the quinoxaline antibiotic analog TANDEM (des-N-tetramethyltriostin A). In: Journal of the American Chemical Society, 104 (12). pp. 3401-3408. Viswamitra, MA and Shakked, Zippora and Jones, PG and Sheldrick, GM and Salisbury, SA and Kennard, Olga (1982) Structure of the Deoxytetranucleotide d-pApTpApT and a Sequence-Dependent Model for Poly(dA-dT). In: Biopolymers, 21 (3). pp. 513-533. Klug, A and Jack, A and Viswamitra, MA and Kennard, Olga and Shakked, Z and Steitz, TA (1979) A hypothesis on a specific sequence-dependent conformation of DNA and its relation to the binding of the lac-repressor protein. In: Journal of Molecular Biology, 131 (4). pp. 669-680. Viswamitrata, MA and Seshadri, TP and Post, ML and Kennard, Olga (1975) Molecular structures of cytidine-5-diphosphate and ...
Hoogsteen (HG) base pairs (bps) provide an alternative pairing geometry to Watson-Crick (WC) bps and can play unique functional roles in duplex DNA. Here, we use structural features unique to HG bps (syn purine base, HG hydrogen bonds and constricted C1-C1 distance across the bp) to search for HG bps in X-ray structures of DNA duplexes in the Protein Data Bank. The survey identifies 106 A•T and 34 G•C HG bps in DNA duplexes, many of which are undocumented in the literature. It also uncovers HG-like bps with syn purines lacking HG hydrogen bonds or constricted C1-C1 distances that are analogous to conformations that have been proposed to populate the WC-to-HG transition pathway. The survey reveals HG preferences similar to those observed for transient HG bps in solution by nuclear magnetic resonance, including stronger preferences for A•T versus G•C bps, TA versus GG steps, and also suggests enrichment at terminal ends with a preference for 5-purine. HG bps induce small local ...
Left: Watson-Crick base pair; Right: Hoogsteen base pair (A = Adenine, U = Uracil, found in RNA).. Were all familiar with the double helix form of DNA. However, thats not the only shape DNA ever takes. Hashim Al-Hashimi led a team from the University of Michigan in identifying and observing an alternate form of DNA.. Normally, the DNA bases adenine (A), thymine (T), guanine (G) and cytosine (C) pair up in a specific way to create whats known as a Watson-Crick double helix. By using modified nuclear magnetic resonance (NMR), the team was able to observe a different kind of pairing called Hoogsteen base pairs. Although this structure had been observed before, Hoogsteen base pairs were thought to occur only in DNA that is damaged or bound to certain proteins or drugs. Al-Hashimi and his team showed that this is not the case, in fact, DNA can spontaneously, though briefly, flip into the alternative orientation. The changes were too ephemeral to have been seen by conventional NMR. Al-Hashimis ...
Mutations in the evolutionarily conserved codons of the p53 tumor suppressor gene are common in diverse types of human cancer. The p53 mutational spectrum differs among cancers of the colon, lung, esophagus, breast, liver, brain, reticuloendothelial tissues, and hemopoietic tissues. Analysis of these mutations can provide clues to the etiology of these diverse tumors and to the function of specific regions of p53. Transitions predominate in colon, brain, and lymphoid malignancies, whereas G:C to T:A transversions are the most frequent substitutions observed in cancers of the lung and liver. Mutations at A:T base pairs are seen more frequently in esophageal carcinomas than in other solid tumors. Most transitions in colorectal carcinomas, brain tumors, leukemias, and lymphomas are at CpG dinucleotide mutational hot spots. G to T transversions in lung, breast, and esophageal carcinomas are dispersed among numerous codons. In liver tumors in persons from geographic areas in which both aflatoxin B1 ...
Present in northwestern region, central-western region, Sierra Nevada foothills, Sacramento Valley (Sutter Buttes), western Transverse Ranges, and possibly south coast, to 1000m. Inhabits grassland, chaparral, oak woodland, summer dry pasture, coastal bluffs and terraces, riverbanks, and other disturbed places (1).Very common along the coast, and even more so inland. A major understory component in oak woodlands (so is somewhat shade-tolerant), and in almost all grasslands in the N. Coast Ranges and along the coast (2). Roadsides, fields, grassland, chaparral, oak woodland, summer dry pasture, coastal bluffs and terraces, riverbanks, other disturbed places.. ...
120Figure 8. A, B. Heliopyge helios (Richter & Richter, 1926) from the Ermitage Member of the Moulin Liénaux Formation at Loc018, Nismes. Incomplete pygidium, IRSNB a13166, in dorsal view (A). Fragment of left side of a pygidium, IRSNB a13167, in dorsal view (B). C. Heliopyge cf. helios from the Bovesse Formation at Loc096, Ligny. Partially exfoliated pygidium, IRSNB a13188, in dorsal view. D-J, L. Bradocryphaeus mosanus (Richter & Richter, 1926) from the Ermitage Member of the Moulin Liénaux Formation at Loc088, Marloie. Cephalon, IRSNB a13208, in dorsal (D), oblique lateral (E) and anterior (G) views. Cephalon, IRSNB a13209, in dorsal (F) and anterior (H) views. Pygidium, IRSNB a13210, in dorsal (I) and posterior (L) views. Pygidium, IRSNB a13211, in dorsal view (J). K, M-Q. Bradocryphaeus echinatus sp. nov. from the Ermitage Member of the Moulin Liénaux Formation at Loc120, Hotton. Holotype pygidium, IRSNB a13215, in dorsal (N), lateral (O) and close-up of right pleural field (Q) views. ...
Conservation of information between prokaryotic and eukaryotic regulatory proteins and their cognate binding sites on DNA and RNA (operators and response elements) has been observed and is proposed as a basis for site-specific recognition. We present anal
A printed wire board has lamp socket holes and switch contact pairs adjacent the holes on the top surface of the board and lamp socket contacts adjacent the holes on its bottom surface. An insulating spacer sheet is adhered to the board and has apertures which are congruent with the switch contact pairs. A membrane, adhered to the top surface of the spacer, has lamp holes and short circuiting contacts on its bottom surface for being flexed through the apertures to bridge gaps between the contact pairs on the board. An apertured rigid plate is superposed over and spaced from the membrane. Combination light channel and switch operating plunger elements fit in the plate apertures and contact the membrane. A film on which switch operating touch zones are delineated is adhered to the plate.
53066-83-4 - XXLSSFGQENJRJJ-UHFFFAOYSA-N - Quinoxaline, 2-(4-((3-methylbutyl)thio)phenyl)- - Similar structures search, synonyms, formulas, resource links, and other chemical information.
Basepairs involving Hoogsteen(H) edge of Adenine and WatsonCrick(W) edge of Guanine is shown. Highlighted examples are found from RNA crystal structures obtained from PDB. Base pairs stabilized by N-H...N/O type hydrogen bonds ...
0063] Specific examples of the above and other classes of drugs and therapeutic agents deliverable by the invention are set forth below, by way of example only. Each named drug should be understood to include the neutral form of the drug, pharmaceutically acceptable salts, as well as prodrugs. Specific examples of antihypertensives include prazosin, nifedipine, trimazosin and doxazosin; a specific example of an antianxiety agent is hydroxyzine; a specific example of a blood glucose-lowering agent is glipizide; a specific example of an anti-impotence agent is sildenafil citrate; specific examples of antineoplastics include chlorambucil, lomustine and echinomycin; a specific example of an imidazole-type antineoplastic is tubulazole; specific examples of anti-inflammatory agents include betamethasone, prednisolone, aspirin, flurbiprofen and (+)-N-{4-[3-(4-fluorophenoxy)phenoxy]-2-cyclopenten-1-yl}-N-hydroxyurea; a specific example of a barbiturate is phenobarbital; specific examples of antivirals ...
The synthesis of a new bifunctional compound in which two aminoacridine chromophores are linked by the bicyclic depsipeptidic backbone of des-N-tetramethylTriostin A is described. The molecule, bis-[(9-acridinyl)-D-seryl-L-alanyl-L-cysteinyl-L-valine] dilactone disulphide, structurally analogous to the antibiotic anti-tumour drug Triostin A, is shown to possess a high affinity to DNA and to act as a bis-intercalator on the basis of spectroscopic, viscosimetric and thermal-denaturation studies. This model constitutes the first attempt of a synergic association between a peptidic moiety that mimics a naturally occurring drug and aminoacridine, the two parts themselves each exhibiting a high affinity for the DNA target. ...
Eckers research interests are in several areas of optimization including geometric programming, multiple objective linear programming, algorithm development and evaluation in nonlinear programming, and applications of mathematical programming. Mathematical programming deals with the problem of optimizing a function of several variables subject to inequality and equality constraints on other functions of several variables. Recent areas of application include the development of an optimization model of locating protein binding sites on DNA strands and the development of a linear programming model for managing consumer credit delinquency. He is also very interested in developing studio courses in which students are actively engaged in the learning process. Much of his current efforts have focused on developing materials for the Studio Calculus course at Rensselaer. In addition, Ecker has focused on optimization problems involving several objective functions that are to be optimized. These multiple ...
The compound 3, which exists in tautomeric equilibria between enamine (form A) and methylene imine (form B), was prepared by addition of ethoxycarbonylmethyl chloride 2 (1.23g, 0.01 mol) to a solution of 3-(ethoxycarbonylmethylene)-2-oxo quinoxaline, 1 [1] (2.32 g, 0.01 mol) in 60 ml DMF, K2CO3 (1.38g, 0.01mol) and triethylbenzylammonium chloride (0.001 mol).[...]
NMR investigations of the PmrA-DNA complex.The overlaid two-dimensional (2D) 1H, 15N TROSY-HSQC spectra (a) and 2D 1H, 13C HSQC spectra, showing the methyl re
Pharmacologically, phenyl pyrazolo benzothiazolo quinoxaline derivatives are known to exhibit important biological activities like antimicrobial1, ant..
The Adam fig tree is one of the oldest figs you can get. They have big green leaves which hide the fruit. They tend to ripen late in the growing season.
Number of consecutive base pairs required in 3 end. How many consecutive 3 end base pairs in the primer that MUST be present for priming/mispriming to occur. This option is included since 3 terminal base pairs are known to be essential for priming to occur ...
Abstract: Proteins are known to locate their specific targets on DNA up to two orders of magnitude faster than predicted by the Smoluchowski three-dimensional diffusion rate. One of the mechanisms proposed to resolve this discrepancy is termed "intersegment transfer." Many proteins have two DNA binding sites and can transfer from one DNA segment to another without dissociation to water. We calculate the target search rate for such proteins in a dense globular DNA, taking into account intersegment transfer working in conjunction with DNA motion and protein sliding along DNA. We show that intersegment transfer plays a very important role in cases where the protein spends most of its time adsorbed on DNA. ...
Heterocyclic compounds particularly five and six membered ring compounds have occupied a prominent place among various classes of organic compounds for their diverse biological activities.[...]
Grade: Biotech Appearance Fine, white homogeneous powder Moisture content ≤10% Gel Strength 1.5% ≥1,120 g/cm2 Gelling Point 34.5 - 37.5°C Electroendosmosis-Mr 0.09-0.13 Sulfate ≤0.15% DNase , RNase and protease None detected ...
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SW-163C: cyclic depsipeptide having 3-hydroxyquinaldic acid as a chromophore and a sulfur-containing intramolecular cross linkage