Groove specificity. Pyrrole-imidazole polyamides are well-known for their specific interactions with the minor groove of DNA. Here we demonstrate that polyamides do not similarly bind duplex RNA, and offer a structural rationale for the molecular-level discrimination of nucleic acid duplexes by minor groove binding ligands.

Blood compatibility of polyamides has been improved by introducing amido-amine groups in polymer backbone. Polyamide block-copolymer are synthesized by reacting amine end-capped polyamides with N,N'-methylene-bisacrylamide. Polyamide block-copolymers, thus produced found to have the ability of absorbing heparin. Heparinized polyamide block-copolymers have shown significant improvement in blood ...

The sequence-specific recognition of the minor groove of DNA by pyrrole-imidazole polyamides has been extended to 9-13 base pairs (bp). Four polyamides, ImPyPy-Py-PyPyPy-Dp, ImPyPy-G-PyPyPy-Dp, ImPyPyâ-PyPyPy-Dp, and ImPyPy-γ-PyPyPy-Dp (Im ) N-methylimidazole, Py ) N-methylpyrrole, Dp ) N,Ndimethylaminopropylamide, G ) glycine, â ) â-alanine, and γ ) γ-aminobutyric acid), were synthesized and c...

We report a preclinical study of a pyrrole-imidazole (PI) polyamide that targets the human transforming growth factor (hTGF)-β1 gene as a novel transcriptional gene silencer in a common marmoset primate model. We designed and then synthesized PI polyamides to target the hTGF-β1 promoter. We examined effects of seven PI polyamides (GB1101-1107) on the expression of hTGF-β1 mRNA stimulated with p...

The gene-specific transcription factor IIIA (TFIIIA) binds to the internal promoter element of the 5 S rRNA gene through nine zinc fingers which make specific DNA contacts. Seven of the nine TFIIIA zinc fingers participate in major groove DNA contacts while two fingers, 4 and 6, have been proposed to bind in or across the minor groove. Pyrrole-imidazole polyamides are minor groove binding ligan...

Inside Cover: In article number 2100408 by C. Remzi Becer and co-workers, N-substituted polyamides with high biomass content tunable physical properties, such as glass transition temperature hydrophobicity, are prepared via an efficient catalyst-free Ugi 4-component reaction polymerization in optimized solvent system. The obtained polyamides, which show excellent thermal stability near-room tra...

When targeted to sequences adjacent to a TATA element, pyrrole-imidazole (Py-Im) polyamides inhibit the DNA binding activity of TATA box binding protein (TBP) and basal transcription by RNA polymerase II. In the present study, we scanned the human immunodeficiency virus type 1 promoter for polyamide inhibition of TBP binding and transcription using a series of DNA constructs in which a polyamid...

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-terminu...

A new aromatic diamine monomer containing ether linkage based on the phenanthrimidazole ring, ‎1,1´-(4,4´- oxy bis(1,4-phenylene))bis(2-(4-aminophenyl)-1H-phenanthro[9,10-d]imidazole) was synthesized through four-‎components condensation of 4,4´-diamino diphenyl ether, 4-nitrobenzaldehyde, phenanthrene-9,10-dione and ammonium ‎acetate in presence of acetic acid, followed by palladi...

Pyrrole-imidazole polyamides targeted to the androgen response element were cytotoxic in multiple cell lines, independent of intact androgen receptor signaling. Polyamide treatment induced accumulation of S-phase cells and of PCNA replication/repair foci. Activation of a cell cycle checkpoint response was evidenced by autophosphorylation of ATR, the S-phase checkpoint kinase, and by recruitment...