Groove binder

Design of DNA minor-groove binders as new antitumor agents 99F15. 

Figure 9 summarizes the electrode responses toward a variety of DNA-binding substrates [14c]. For intercalators (quinacrine, acridine orange, and safranin) and groove binders (spermine and spermidine), a steep rise followed by a saturation of the concentration response curve is commonly observed. If one compares the specific concentration which gives a 50% response in the increment of the cathodic peak current (A/p ) for each substrate, a selectivity order of quinacrine acridine orange > spermine > spermidine > safranin can be estimated. The binding constants measured in aqueous media for the affinity reaction with ds DNA are as follows quinacrine, 1.5 x 10 (38 mM NaCl)... 

Escude C, Sun J-S (2005) DNA Major Groove Binders Triple Helix-Forming Oligonucleotides, Triple Helix-Specific DNA Ligands and Cleaving Agents. 253 109-148 Evans SV, see Schuman B (2007) 272 217-258 Van der Eycken E, see Appukkuttan P (2006) 266 1-47... 

The DNA minor groove binder brostallicin (PNU-166196, 24), currently in Phase 2 clinical trials for the treatment of soft-tissue sarcoma, exhibited potent... 

D.A. Kulesh, R.O. Baker, B.M. Loveless, D. Norwood, S.H. Zwiers, E. Mucker, C. Hartmann, R. Herrera, D. Miller, D. Christensen, L.P. Wasieloski Jr., J. Huggins and P.B. Jahrling, Smallpox and pan-orthopox virus detection by real-time 3 -minor groove binder TaqMan assays on the Roche lightcycler and the Cepheid smart cycler platforms, J. Clin. Microbiol., 42 (2004) 601-609. 

Attempts have been made to prepare carborane-containing DNA binders by adding carborane units to representative DNA intercalators (acridine, ethidium) and a DNA groove binder (distamysine), which have high binding affinity with DNA (Scheme 2.2-8). The intercalators insert themselves into a gap between the base pairs of double-helical DNA [32, 33]. 

Other compounds with strong affinity to DNA are groove binders such as ne-... 

Scheme 2.2-9. C2Bio-containing DNA minor groove binders. 

Keywords Nucleosome, Chromosome, Intercalators, Groove-binders, DNA-cleaving agents. 

Minor groove binders. Minor groove binders are typically composed... 

Major groove binders. Mainly proteins recognize the major... 

Woynarowski JM, Beerman TA (1997) Effects of bizelesin (U-77,779), a bifunctional alkylating minor groove binder, on repUcation of genomic and simian virus 40 DNA in BSC-1 cells. Biochim Biophys Acta 1353 50-60... 

RNA, (ii) the screening for antiviral compounds that do not bind to RNA but bind specifically to target RNA polymerases, (hi) the evaluation of the binding of aminoglycosides to RNA, and (iv) the evaluation of the binding of DNA intercalators and minor groove binders to RNA. 

De Pauw, E. Determination of binding constants of oligonucleotide complexes with minor groove binders by electrospray ionization mass spectrometry. Comparison with fluorescence titration data. Adv. Mass Spectrom. 2001, 15, 795-796. 

AGE — agarose gel electrophoresis, BAL = bronchoalveolar fluid, FAM = 6-carboxyfluorescein label, MGB = minor groove binder, n.s. - not specified, RAPD = randomly amplified polymorphic DNA, RT-PCR = reverse transcription PCR, TAMRA = 6-carboxytetramethylrhodamine label. 

Carteau S, Mouscadet JF, Goulaouic H, Subra F, Auclair C. Inhibition of the in vitro integration of Moloney murine leukemia virus DNA by the DNA minor groove binder netropsin. Biochem Pharmacol... 

Electrochemical transduction of the hybridisation event can be classified into two categories label-based and label-free approaches. The label-based approach can be further subdivided into intercalator/groove binder, non-intercalating marker, and NP. The label-free approach is based on the intrinsic electroactivity of the DNA purine bases or the change in interfacial properties (e.g., capacitance and electron transfer resistance) upon hybridisation [49],... 

Matsuzawa, Y. and Yoshikawa, K. (1994) Change of the higher-order structure in a giant DNA induced by 4 ,6-diamidino-2-phenylindole as a minor groove binder and ethidium bromide as an intercalator. Nucleosides Nucleotides, 13, 1415-1423. 

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