Synthesis and spectroscopic studies of the aminoglycoside (neomycin)--perylene conjugate binding to human telomeric DNA.


:Synthesis of a novel perylene-neomycin conjugate (3) and the properties of its binding to human telomeric G-quadruplex DNA, 5'-d[AG3(T2AG3)3] (4), are reported. Various spectroscopic techniques were employed to characterize the binding of conjugate 3 to 4. A competition dialysis assay revealed that 3 preferentially binds to 4, in the presence of other nucleic acids, including DNA, RNA, DNA-RNA hybrids, and other higher-order structures (single strands, duplexes, triplexes, other G-quadruplexes, and the i-motif). UV thermal denaturation studies showed that thermal stabilization of 4 increases as a function of the increasing concentration of 3. The fluorescence intercalator displacement (FID) assay displayed a significantly tighter binding of 3 with 4 as compared to its parent constituents [220-fold stronger than neomycin (1) and 4.5-fold stronger than perylene diamine (2), respectively]. The binding of 3 with 4 resulted in pronounced changes in the molar ellipticity of the DNA absorption region as confirmed by circular dichroism. The UV-vis absorption studies of the binding of 3 to 4 resulted in a red shift in the spectrum of 3 as well as a marked hypochromic change in the perylene absorption region, suggesting that the ligand-quadruplex interaction involves stacking of the perylene moiety. Docking studies suggest that the perylene moiety serves as a bridge that end stacks on 4, making contacts with two thymine bases in the loop, while the two neomycin moieties branch into the grooves of 4.






Xue L,Ranjan N,Arya DP




Has Abstract


2011-04-12 00:00:00












  • Thermodynamic characterization of the binding interaction between the histone demethylase LSD1/KDM1 and CoREST.

    abstract::Flavin-dependent histone demethylases catalyze the posttranslational oxidative demethylation of mono- and dimethylated lysine residues, producing formaldehyde and hydrogen peroxide in addition to the corresponding demethylated protein. In vivo, histone demethylase LSD1 (KDM1; BCH110) is a component of the multiprotein...


    pub_type: 杂志文章


    authors: Hwang S,Schmitt AA,Luteran AE,Toone EJ,McCafferty DG

    更新日期:2011-02-01 00:00:00

  • Expression and In Vivo Characterization of the Antimicrobial Peptide Oncocin and Variants Binding to Ribosomes.

    abstract::Peptides have important biomedical applications, but poor correlation between in vitro and in vivo activities can limit their development for clinical use. The ability to generate peptides and monitor their expression with new mass spectrometric methods and biological activities in vivo would be an advantage for the d...


    pub_type: 杂志文章


    authors: Muthunayake NS,Islam R,Inutan ED,Colangelo W,Trimpin S,Cunningham PR,Chow CS

    更新日期:2020-09-15 00:00:00

  • Dissection of the pH dependence of inhibitor binding energetics for an aspartic protease: direct measurement of the protonation states of the catalytic aspartic acid residues.

    abstract::The catalytic activity and inhibitor binding energetics of enzymes are often pH-dependent properties. Aspartic proteases comprise an important class of enzyme targets for structure-based drug design. We have performed a complete thermodynamic study of pepstatin binding to plasmepsin II, an aspartic proteinase found in...


    pub_type: 杂志文章


    authors: Xie D,Gulnik S,Collins L,Gustchina E,Suvorov L,Erickson JW

    更新日期:1997-12-23 00:00:00

  • The thermodynamic and structural differences among the catalytically active complexes of phosphoglucomutase: metal ion effects.

    abstract::When the identity of the metal ion activator, M, is changed within the series, Zn2+, Co2+, Mg2+, Ni2+, Mn2+, and Cd2+, the equilibrium distribution among the central complexes in the phosphoglucomutase system is markedly altered. (The central complexes are Ep-M-Glc-6-P, ED-M-Glc-1,6-P2, and Ep-M-Glc-1-P, where Ep and ...


    pub_type: 杂志文章


    authors: Ray WJ Jr,Long JW

    更新日期:1976-09-07 00:00:00

  • Effects of select histidine to cysteine mutations on transcriptional regulation by Escherichia coli RcnR.

    abstract::The RcnR metalloregulator represses the transcription of the Co(II) and Ni(II) exporter, RcnAB. Previous studies have shown that Co(II) and Ni(II) bind to RcnR in six-coordinate sites, resulting in derepression. Here, the roles of His60, His64, and His67 in specific metal recognition are examined. His60 and His64 corr...


    pub_type: 杂志文章


    authors: Higgins KA,Hu HQ,Chivers PT,Maroney MJ

    更新日期:2013-01-08 00:00:00

  • Characterization and purification of the monoamine transporter of bovine chromaffin granules.

    abstract::The monoamine transporter of the chromaffin granule membranes can be specifically labeled by the photoaffinity reagent 7-azido-8-[125I]iodoketanserin. The characteristics of the labeled protein have been investigated. Two-dimensional gel electrophoresis of the labeled membranes indicated a MW of about 70,000 and an is...


    pub_type: 杂志文章


    authors: Isambert MF,Gasnier B,Botton D,Henry JP

    更新日期:1992-02-25 00:00:00

  • Turkey ovomucoid third domain inhibits eight different serine proteinases of varied specificity on the same ...Leu18-Glu19 ... reactive site.

    abstract::We show that eight different serine proteinases--bovine chymotrypsins A and B, porcine pancreatic elastase I, proteinase K, Streptomyces griseus proteinases A and B, and subtilisins BPN' and Carlsberg--interact with turkey ovomucoid third domain at the same Leu18-Glu19 peptide bond, the reactive site of the inhibitor....


    pub_type: 杂志文章


    authors: Ardelt W,Laskowski M Jr

    更新日期:1985-09-24 00:00:00

  • N-ethylmaleimide inhibits Ncd motor function by modification of a cysteine in the stalk domain.

    abstract::N-Ethylmaleimide (NEM), which reacts readily with exposed sulfhydryl groups, has been shown to inhibit the activity of the microtubule (MT) motors kinesin, Ncd, and dynein. Currently, the mechanism of inhibition is not known for any of these proteins. To investigate the mechanism by which NEM inhibits Ncd, the recombi...


    pub_type: 杂志文章


    authors: Phelps KK,Walker RA

    更新日期:1999-08-17 00:00:00

  • Role of mitochondrial and cytoplasmic serine hydroxymethyltransferase isozymes in de novo purine synthesis in Saccharomyces cerevisiae.

    abstract::One-carbon units are essential to a variety of anabolic processes which yield necessary cellular components including purines, pyrimidines, amino acids, and lipids. Serine hydroxymethyltransferase (SHMT) is the major provider of one-carbon units in the cell. The other product of this reaction is glycine. Both of these...


    pub_type: 杂志文章


    authors: Kastanos EK,Woldman YY,Appling DR

    更新日期:1997-12-02 00:00:00

  • Mössbauer characterization of an unusual high-spin side-on peroxo-Fe3+ species in the active site of superoxide reductase from Desulfoarculus Baarsii. Density functional calculations on related models.

    abstract::Superoxide reductase (SOR) is an Fe protein that catalyzes the reduction of superoxide to give H(2)O(2). Recently, the mutation of the Glu47 residue into alanine (E47A) in the active site of SOR from Desulfoarculus baarsii has allowed the stabilization of an iron-peroxo species when quickly reacted with H(2)O(2) [Math...


    pub_type: 杂志文章


    authors: Horner O,Mouesca JM,Oddou JL,Jeandey C,Nivière V,Mattioli TA,Mathé C,Fontecave M,Maldivi P,Bonville P,Halfen JA,Latour JM

    更新日期:2004-07-13 00:00:00

  • Changes in protein conformation and stability accompany complex formation between human C1 inhibitor and C1-s.

    abstract::The fluorescence spectrum of C1 inhibitor (C1-Inh) in aqueous buffer has a maximum at 324 nm which shifts to 358 nm in 6.0 M guanidinium chloride (GdmC1), indicating that fluorescent tryptophans are buried in the native protein. When titrated with GdmC1, the fluorescence intensity, polarization, and emission maximum o...


    pub_type: 杂志文章


    authors: Lennick M,Brew SA,Ingham KC

    更新日期:1985-05-07 00:00:00

  • Librational motion of an "immobilized" spin label: hemoglobin spin labeled by a maleimide derivative.

    abstract::The spin label Tempo-maleimide, when "immobilized" in hemoglobin, is shown to exhibit motional fluctuation whose amplitude and/or frequency depend on temperature and solution conditions. These motional fluctuations are observable by several electron spin resonance techniques. For desalted hemoglobin the fluctuations a...


    pub_type: 杂志文章


    authors: Johnson ME

    更新日期:1978-04-04 00:00:00

  • Occurrence of a reduced nicotinamide adenine dinucleotide oxidase activity linked to a cytochrome system in renal brush border membranes.

    abstract::NADH oxidase activity has been detected in luminal membrane derived from the proximal tubules of rat kidney (brush border membranes). The cytochromes associated with these membranes [García, M.L., Benavides, J., Valdivieso, F., Mayor, F., & Giménez-Gallego, G. (1978) Biochem. Biophys. Res. Commun. 82, 738-744] were re...


    pub_type: 杂志文章


    authors: Giménez-Gallego G,Benavides J,García ML,Valdivieso F

    更新日期:1980-10-14 00:00:00

  • Thrombin inactivates acidic fibroblast growth factor but not basic fibroblast growth factor.

    abstract::Incubation of bovine brain derived acidic fibroblast growth factor (aFGF) with bovine or human thrombin, 0.5 NIH unit/mL, for 24 h at 37 degrees C results in cleavage of the mitogen, generating a 14-kilodalton fragment which has significantly reduced affinity for immobilized heparin as compared to aFGF, and is at leas...


    pub_type: 杂志文章


    authors: Lobb RR

    更新日期:1988-04-05 00:00:00

  • Inhibition of peptidyl-prolyl cis/trans isomerase activity by substrate analog structures: thioxo tetrapeptide-4-nitroanilides.

    abstract::The ubiquitous cyclophilins belong to peptidyl-prolyl cis/trans isomerases (PPIases; EC They are able to catalyze the cis/trans isomerization about peptidyl-prolyl amide bonds. The mode of action of human cytosolic cyclophilin (Cyp18cy) has been studied on substrate analog tetrapeptide-4-nitroanilides contai...


    pub_type: 杂志文章


    authors: Schutkowski M,Wöllner S,Fischer G

    更新日期:1995-10-10 00:00:00

  • A Cyclic Mimic of HIV Tat Differentiates Similar TAR RNAs on the Basis of Distinct Dynamic Behaviors.

    abstract::Efforts toward the development of RNA-based drug leads have been challenging because of the complexity and dynamic nature of RNA structures as therapeutic targets. The transactivation response (TAR) RNA and cognate Tat protein of HIV have long been recognized as promising antiviral targets, and recent works have ident...


    pub_type: 杂志文章


    authors: Lu J,Nguyen L,Zhao L,Xia T,Qi X

    更新日期:2015-06-16 00:00:00

  • Long-range structural and dynamical changes induced by cofactor binding in DNA methyltransferase M.HhaI.

    abstract::The bacterial DNA cytosine methyltransferase M.HhaI sequence-specifically modifies DNA in an S-adenosylmethionine dependent reaction. The enzyme stabilizes the target cytosine (GCGC) into an extrahelical position, with a concomitant large movement of an active site loop involving residues 80-99. We used multidimension...


    pub_type: 杂志文章


    authors: Zhou H,Shatz W,Purdy MM,Fera N,Dahlquist FW,Reich NO

    更新日期:2007-06-19 00:00:00

  • The amino- and carboxyl-terminal fragments of the Bacillus thuringensis Cyt1Aa toxin have differential roles in toxin oligomerization and pore formation.

    abstract::The Cyt toxins produced by the bacteria Bacillus thuringiensis show insecticidal activity against some insects, mainly dipteran larvae, being able to kill mosquitoes and black flies. However, they also possess a general cytolytic activity in vitro, showing hemolytic activity in red blood cells. These proteins are comp...


    pub_type: 杂志文章


    authors: Rodriguez-Almazan C,Ruiz de Escudero I,Cantón PE,Muñoz-Garay C,Pérez C,Gill SS,Soberón M,Bravo A

    更新日期:2011-01-25 00:00:00

  • Location of sites in human lipocortin I that are phosphorylated by protein tyrosine kinases and protein kinases A and C.

    abstract::Lipocortin I is a 39-kilodalton membrane-associated protein that in A431 cells is phosphorylated on tyrosine in response to epidermal growth factor (EGF). We have used recombinant human lipocortin I as a substrate for several protein kinases and identified phosphorylated residues by a combination of peptide mapping an...


    pub_type: 杂志文章


    authors: Varticovski L,Chahwala SB,Whitman M,Cantley L,Schindler D,Chow EP,Sinclair LK,Pepinsky RB

    更新日期:1988-05-17 00:00:00

  • Properties of overlapping EREs: synergistic activation of transcription and cooperative binding of ER.

    abstract::We have designed a novel estrogen-responsive unit, overERE, which consists of two overlapping ERE separated by 5 bp (center-to-center). In gel retardation assays, this sequence forms a low-mobility complex that migrates like an estrogen receptor tetramer. The receptor-overERE complex was specific and was supershifted ...


    pub_type: 杂志文章


    authors: Massaad C,Coumoul X,Sabbah M,Garlatti M,Redeuilh G,Barouki R

    更新日期:1998-04-28 00:00:00

  • Forming the phosphate layer in reconstituted horse spleen ferritin and the role of phosphate in promoting core surface redox reactions.

    abstract::Apo horse spleen ferritin (apo HoSF) was reconstituted to various core sizes (100-3500 Fe3+/HoSF) by depositing Fe(OH)3 within the hollow HoSF interior by air oxidation of Fe2+. Fe2+ and phosphate (Pi) were then added anaerobically at a 1:4 ratio, and both Fe2+ and Pi were incorporated into the HoSF cores. The resulti...


    pub_type: 杂志文章


    authors: Johnson JL,Cannon M,Watt RK,Frankel RB,Watt GD

    更新日期:1999-05-18 00:00:00

  • Electrostatic Constituents of the Interaction of Cardiolipin with Site A of Cytochrome c.

    abstract::Cytochrome c binds to cardiolipin (CL) on the inner mitochondrial membrane during the initial stages of apoptosis where it oxidizes CL, promoting its release into the cytoplasm where it initiates apoptosis. Previous work has identified interaction sites on cytochrome c involved in the cytochrome c-CL interaction. The ...


    pub_type: 杂志文章


    authors: Elmer-Dixon MM,Bowler BE

    更新日期:2018-10-02 00:00:00

  • DNA polymerase beta fidelity: halomethylene-modified leaving groups in pre-steady-state kinetic analysis reveal differences at the chemical transition state.

    abstract::The mechanism of DNA polymerase beta-catalyzed nucleotidyl transfer consists of chemical steps involving primer 3' OH deprotonation, nucleophilic attack, and pyrophosphate leaving-group elimination, preceded by dNTP binding which induces a large-amplitude conformational change for Watson-Crick nascent base pairs. Ambi...


    pub_type: 杂志文章


    authors: Sucato CA,Upton TG,Kashemirov BA,Osuna J,Oertell K,Beard WA,Wilson SH,Florián J,Warshel A,McKenna CE,Goodman MF

    更新日期:2008-01-22 00:00:00

  • Mechanism of adenylate kinase. Structural and functional roles of the conserved arginine-97 and arginine-132.

    abstract::The structural and functional roles of two conserved active site residues, Arg-97 and Arg-132, in chicken muscle adenylate kinase (AK) were evaluated by site-directed mutagenesis in conjunction with one- and two-dimensional proton nuclear magnetic resonance (NMR), kinetics, and guanidine hydrochloride-induced denatura...


    pub_type: 杂志文章


    authors: Dahnke T,Shi Z,Yan H,Jiang RT,Tsai MD

    更新日期:1992-07-14 00:00:00

  • Structural Basis for Substrate and Oxygen Activation in Homoprotocatechuate 2,3-Dioxygenase: Roles of Conserved Active Site Histidine 200.

    abstract::Kinetic and spectroscopic studies have shown that the conserved active site residue His200 of the extradiol ring-cleaving homoprotocatechuate 2,3-dioxygenase (FeHPCD) from Brevibacterium fuscum is critical for efficient catalysis. The roles played by this residue are probed here by analysis of the steady-state kinetic...


    pub_type: 杂志文章


    authors: Kovaleva EG,Rogers MS,Lipscomb JD

    更新日期:2015-09-01 00:00:00

  • Chloroplast biogenesis: [4-vinyl] chlorophyllide a reductase is a divinyl chlorophyllide a-specific, NADPH-dependent enzyme.

    abstract::Some properties of [4-vinyl] chlorophyllide a reductase are described. This enzyme converts divinyl chlorophyllide a to monovinyl chlorophyllide a. The latter is the immediate precursor of monovinyl chlorophyll a, the main chlorophyll in green plants. [4-Vinyl] chlorophyllide a reductase plays an important role in day...


    pub_type: 杂志文章


    authors: Parham R,Rebeiz CA

    更新日期:1992-09-15 00:00:00

  • Ligand-dependent aggregation and cooperativity: a critique.

    abstract::Ligand-dependent site-site (or subunit-subunit) interactions provide the basis for explaining cooperativity in chemical reactions. Even in the simplest possible nonaggregating system, interpretation of the interactions in terms of structural details requires an explicit assumption (or model) for the binding of the lig...


    pub_type: 杂志文章,评审


    authors: Saroff HA

    更新日期:1991-10-22 00:00:00

  • Structural studies of P22 phage, precursor particles, and proteins by laser Raman spectroscopy.

    abstract::For the study of the protein--protein and protein--nucleic acid interactions in the assembly of virus particles, laser Raman spectra have been obtained in H2O and D2O solutions and as a function of temperature for the following Salmonella phage P22 components: mature phage particles, isolated mature phage DNA, mature ...


    pub_type: 杂志文章


    authors: Thomas GJ Jr,Li Y,Fuller MT,King J

    更新日期:1982-08-03 00:00:00

  • Pre-steady-state kinetic analysis of enzyme-monitored turnover during cystathionine β-synthase-catalyzed H(2)S generation.

    abstract::Cystathionine β-synthase (CBS) catalyzes the first step in the transsulfuration pathway in mammals, i.e., the condensation of serine and homocysteine to produce cystathionine and water. Recently, we have reported a steady-state kinetic analysis of the three hydrogen sulfide (H(2)S)-generating reactions that are cataly...


    pub_type: 杂志文章


    authors: Singh S,Ballou DP,Banerjee R

    更新日期:2011-01-25 00:00:00

  • Calcium binding to calmodulin mutants having domain-specific effects on the regulation of ion channels.

    abstract::Calmodulin (CaM) is an essential, eukaryotic protein comprised of two highly homologous domains (N and C). CaM binds four calcium ions cooperatively, regulating a wide array of target proteins. A genetic screen of Paramecia by Kung [Kung, C. et al. (1992) Cell Calcium 13, 413-425] demonstrated that the domains of CaM ...


    pub_type: 杂志文章


    authors: VanScyoc WS,Newman RA,Sorensen BR,Shea MA

    更新日期:2006-12-05 00:00:00