Minor-groove binders

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

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. 

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

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

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... 

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. 

Yoshikawa, K., Matsuzawa, Y., Minagawa, K., Doi, M. and Matsumoto, M. (1992) Opposite effect between inteicalator and minor groove binder drug on the higher order structure of DNA as is visualised by fluorescence microscopy. Biochem. Biophys. Res. Commun., 188, 1274-1279. 

The two grooves, major and minor, in a DNA double helix are structural features that can be readily recognized by many compounds. Typically, major groove binders share distinct traits from minor groove binders. 

L. J., Clark, G.R., Martin, R.F., White, J. Structures of m-iodo Hoechst-DNA complexes in crystals with reduced solvent content implications for minor groove binder dmg design. Nucleic Acids Res. 2000, 28, 1252-1258 (b) 1QV8, 1QV4 Martin, R. F., Broadhurst, S., Reum,... 

Shaikh, S. A., Ahmed, S. R., and Jayaram, B., A molecular thermodynamic view of DNA-drug interactions a case study of 25 minor-groove binders. Arch. Biochem. Biophys. 429, 81-99 (2004). 

SNP analysis with genomic DNA Monolabeled uniprobes F at the 5 -end - - free minor groove binder F FRET 34... 

The fluorescence lifetimes of the four natural DNA bases within the femtosecond range are too short to be useful as spectroscopic probes to characterize the solvation dynamics of DNA (31). The minor groove binder Hoechst 33258, the fluorescent adenine analog 2-Aminopurine (2Ap), and the base pair mimic coumarine 102-abasic site are better probes because they exhibit longer lifetimes and better solvatochromic properties. Of the two base pair analogs, the coumarine 102-abasic site base pair mimic disrupts the native DNA structure more than the adenine analog 2Ap. However, the spectroscopic characteristics of the former are superior to those of 2Ap for probing solvation dynamics. 

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