Recognition of the four Watson-Crick base pairs in the DNA minor groove by synthetic ligands
Article Abstract:
It has been possible to identify the DNA-binding affinities of three eight-ring hairpin polyamides containing pairings of Im/Py, Py/Im opposite G.C, C.G and either Py/Py, Hp/Py or Py/Hp at a common single point opposite T.A and A.T. A new aromatic acid, 3-hydroxypyrrole (Hp), was added to test for pairings that discriminate A.T from T.A. It was found that replacing a single hydrogen atom with a hydroxy group in a Hp/Py pairing regulates affinity and specificity by an order of magnitude.
Publication Name: Nature
Subject: Zoology and wildlife conservation
ISSN: 0028-0836
Year: 1998
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Regulation of gene expression by small molecules
Article Abstract:
Genetic research shows eight-ring pyrrole-imidazole polyamides are capable of inhibiting transcription in genetic expression. They bind with the factor TFIIIA binding site of Xenopus kidney cells to inhibit the express of the 5S ribonucleic acid gene. Further research is required to establish which genes can be affected by polyamide treatment. Researchers believe polyamides could be used to improve genetic transcription in the development of clinical treatments.
Publication Name: Nature
Subject: Zoology and wildlife conservation
ISSN: 0028-0836
Year: 1997
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Recognition of DNA by designed ligands at subnanomolar concentrations
Article Abstract:
The binding affinities of two synthetic eight-ring hairpin polyamides of pyrrole and imidazole show selective binding to six base pair DNA target site. The DNA-binding affinity and specificity of these polyamides is similar to that of natural DNA-binding proteins. The polyamides differ from each other by a single amino acid residue. The DNA recognition by small synthetic molecules may help in gene-specific regulation in vivo.
Publication Name: Nature
Subject: Zoology and wildlife conservation
ISSN: 0028-0836
Year: 1996
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