Artikel ; Online: Drug design and DNA structural research inspired by the Neidle laboratory: DNA minor groove binding and transcription factor inhibition by thiophene diamidines.
Bioorganic & medicinal chemistry
2022 Band 68, Seite(n) 116861
Abstract: The understanding of sequence-specific DNA minor groove interactions has recently made major steps forward and as a result, the goal of development of compounds that target the minor groove is an active research area. In an effort to develop biologically ...
| Abstract | The understanding of sequence-specific DNA minor groove interactions has recently made major steps forward and as a result, the goal of development of compounds that target the minor groove is an active research area. In an effort to develop biologically active minor groove agents, we are preparing and exploring the DNA interactions of diverse diamidine derivatives with a 5'-GAATTC-3' binding site using a powerful array of methods including, biosensor-SPR methods, and X-ray crystallography. The benzimidazole-thiophene module provides an excellent minor groove recognition component. A central thiophene in a benzimidazole-thiophene-phenyl aromatic system provides essentially optimum curvature for matching the shape of the minor groove. Comparison of that structure to one with the benzimidazole replaced with an indole shows that the two structures are very similar, but have some interesting and important differences in electrostatic potential maps, the DNA minor groove binding structure based on x-ray crystallographic analysis, and inhibition of the major groove binding PU.1 transcription factor complex. The binding K |
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| Mesh-Begriff(e) | Benzimidazoles/chemistry ; Binding Sites ; DNA/chemistry ; Drug Design ; Indoles/pharmacology ; Models, Molecular ; Nucleic Acid Conformation ; Pentamidine/chemistry ; Surface Plasmon Resonance ; Thiophenes/chemistry ; Thiophenes/pharmacology ; Transcription Factors | |||||
| Chemische Substanzen | Benzimidazoles ; Indoles ; Thiophenes ; Transcription Factors ; Pentamidine (673LC5J4LQ) ; DNA (9007-49-2) | |||||
| Sprache | Englisch | |||||
| Erscheinungsdatum | 2022-05-31 | |||||
| Erscheinungsland | England | |||||
| Dokumenttyp | Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S. ; Research Support, N.I.H., Extramural | |||||
| ZDB-ID | 1161284-8 | |||||
| ISSN | 1464-3391 ; 0968-0896 | |||||
| ISSN (online) | 1464-3391 | |||||
| ISSN | 0968-0896 | |||||
| DOI | 10.1016/j.bmc.2022.116861 | |||||
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| Datenquelle | MEDical Literature Analysis and Retrieval System OnLINE |
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