AI Article Synopsis
- The manuscript examines how hairpin polyamides with a specific thiazole unit (Nt) bind to double-stranded DNA (dsDNA) compared to those with an imidazole unit (Im).
- Polyamides with the Nt unit show stronger binding to dsDNA and better stability, but they sacrifice selectivity for guanine (G) bases compared to the Im versions.
- Structural studies reveal that the Nt polyamides cause more compression in the DNA's major groove, indicating a different interaction pattern than the Im-containing polyamides.
Article Abstract
This manuscript reports the molecular basis for double-stranded DNA (dsDNA) binding of hairpin polyamides incorporating a 5-alkyl thiazole (Nt) unit. Hairpin polyamides containing an N-terminal Nt unit induce higher melting stabilisation of target dsDNA sequences relative to an archetypical hairpin polyamide incorporating an N-terminal imidazole (Im) unit. However, modification of the N-terminus from Im to Nt-building blocks results in an increase in dsDNA binding affinity but lower G-selectivity. A general G-selectivity trend is observed for Nt-containing polyamide analogues. G-selectivity increases as the steric bulk in the Nt 5-position increases. Solution-based NMR structural studies reveal differences in the modulation of the target DNA duplex of Nt-containing hairpin polyamides relative to the Im-containing archetype. A structural hallmark of an Nt polyamide•dsDNA complex is a more significant degree of major groove compression of the target dsDNA sequence relative to the Im-containing hairpin polyamide.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5758887 | PMC |
| http://dx.doi.org/10.1093/nar/gkx1211 | DOI Listing |
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