The tripeptide ImPImP containing alternating imidazole and pyrrole carboxamides specifically binds the designated six base pair site 5’-d(A,T)GCGC(A,T)-3’ in the minor groove of DNA. Quantitative footprint titration experiments demonstrate that ImPImP binds the sites 5’-AGCGCT-3’ and 5’-TGCGCA-3’ with apparent first order binding affinities of 3.8 x lo5 M-I and 3.6 x lo5 M-I, respectively (25 m...

The designed peptide pyridine-2-carboxamidonetropsin (2-PyN) binds to the minor groove of double-helical DNA at two very different sequences, 5’-TTTTT-3’ and 5’-TGTCA-3’, with comparable energetics but quite different structures. 2-PyN likely binds the 5’-TTTTT-3’ site as a 1:l complex, whereas 2-PyN binds 5’-TGTCA-3’ sites as a 2:l complex. In order to enhance the binding affinity of 2-PyN for...

A new upper limit of binding site size is defined for the hairpin polyamide-DNA motif. Ten-ring hairpin polyamides containing pyrrole (Py) and imidazole (Im) amino acids were designed for recognition of seven base pair (bp) sequences in the minor groove of DNA. The DNA binding properties of two polyamides, ImPyPyPyPyγ-ImPyPyPyPy-â-Dp, and ImImPyPyPy-γ-ImPyPyPyPy-â-Dp were analyzed by footprinti...

Our recent study has revealed that 12,14-dichlorodehydroabietic acid (diCl-DHAA), which is synthetically derived from a natural product, abietic acid, is a potent opener of large conductance Ca -activated K (BK) channel. Here, we examined, by using a channel expression system in human embryonic kidney 293 cells, the mechanisms underlying the BK channel opening action of diCl-DHAA and which subu...

Arene C(sp2)-H bond borylation offers direct and efficient access to aryl boronic esters. Using in situ catalyst activation photoirradiation, the iron-catalysed reaction of carboarenes, pyrroles, indoles has been developed using only bench-stable pre-catalysts reagents. Good functional group tolerance was observed including those not reported previous methods (ArNH2, ArOH, ArSiR3, ArP(O)(OR)2, ...

Department of Advanced Materials Engin Kyung Hee University, Yongin, Gyeonggi-do 4 Department of Applied Chemistry & Depa University, Ansan, Gyeonggi-do 426-791, Ko Department of Material and Life Science, University, ALCA, Japan Science and Tech 0871, Japan. E-mail: [email protected] † Electronic supplementary information ( the syntheses of the Pt(II) catalysts; Fig. spectra, femtoand nanose...

Pyrrole-imidazole (Py-Im) polyamides can bind to the predetermined base pairs in the minor groove of double-helical DNA with high affinity. These synthetic small molecules can interfere with transcription factor-DNA interaction and inhibit or activate the transcription of corresponding genes. In the present study, we designed and synthesized a Py-Im polyamide to target 545 to 539 base pairs of ...

Selective placement of an aliphatic â-alanine (â) residue paired side-by-side with either a pyrrole (Py) or imidazole (Im) aromatic amino acid is found to compensate for sequence composition effects for recognition of the minor groove of DNA by hairpin pyrrole-imidazole polyamides. A series of polyamides were prepared which contain pyrrole and imidazole aromatic amino acids, as well as γ-aminob...