ArticleProceedings of the National Academy of Sciences of the United States of America2009
Allosteric modulation of DNA by small molecules.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 79 papers.
What it found
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Who cites it
79 citing papers in PubMed.
- Article
- Novel therapeutic strategy targeting STMN1 using chlorambucil-conjugated pyrrole-imidazole polyamide in small cell lung cancer.International journal of cancer · 2026Article
- Structural Studies of a Complex of a CAG/CTG Repeat Sequence-Specific Binding Molecule and A-A-Mismatch-Containing DNA.JACS Au · 2024Article
- Using synthetic genome readers/regulators to interrogate chromatin processes: A brief review.Methods (San Diego, Calif.) · 2024Review
- Targeting MYC with modular synthetic transcriptional repressors derived from bHLH DNA-binding domains.Nature biotechnology · 2023Article
- The roles of ETS transcription factors in liver fibrosis.Human cell · 2023Review
- Potentiometric Determination of Acid Dissociation Constants (pACS medicinal chemistry letters · 2022Article
- RNA polymerase II trapped on a molecular treadmill: Structural basis of persistent transcriptional arrest by a minor groove DNA binder.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Telomere-specific chromatin capture using a pyrrole-imidazole polyamide probe for the identification of proteins and non-coding RNAs.Epigenetics & chromatin · 2021Article
- Low-frequency vibrational modes in G-quadruplexes reveal the mechanical properties of nucleic acids.Physical chemistry chemical physics : PCCP · 2021Article
- Natural and Synthetic Oligoarylamides: Privileged Structures for Medical Applications.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Review
- Targeting the mutant PIK3CA gene by DNA-alkylating pyrrole-imidazole polyamide in cervical cancer.Cancer science · 2021Article
- Cooperative Heteroligand Interaction with G-Quadruplexes Shows Evidence of Allosteric Binding.Biochemistry · 2020Article
- From Interaction to Function in DNA-Templated Supramolecular Self-Assemblies.ChemistryOpen · 2020Review
- Single position substitution of hairpin pyrrole-imidazole polyamides imparts distinct DNA-binding profiles across the human genome.PloS one · 2020Article
- Modulating DNA by polyamides to regulate transcription factor PU.1-DNA binding interactions.Biochimie · 2019Article
- Structural and Kinetic Profiling of Allosteric Modulation of Duplex DNA Induced by DNA-Binding Polyamide Analogues.Chemistry (Weinheim an der Bergstrasse, Germany) · 2019Article
- Experimental Measurement of Surface Charge Effects on the Stability of a Surface-Bound Biopolymer.Langmuir : the ACS journal of surfaces and colloids · 2018Article
- Allosterism and signal transfer in DNA.Nucleic acids research · 2018Article
- A survey of recent unusual high-resolution DNA structures provoked by mismatches, repeats and ligand binding.Nucleic acids research · 2018Review
19 more citing papers are in PubMed but not listed here.
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Authors and funding
2 authors.
Funding
Abstract
Many human diseases are caused by dysregulated gene expression. The oversupply of transcription factors may be required for the growth and metastatic behavior of human cancers. Cell permeable small molecules that can be programmed to disrupt transcription factor-DNA interfaces could silence aberrant gene expression pathways. Pyrrole-imidazole polyamides are DNA minor-groove binding molecules that are programmable for a large repertoire of DNA motifs. A high resolution X-ray crystal structure of an 8-ring cyclic Py/Im polyamide bound to the central 6 bp of the sequence d(5'-CCAGGCCTGG-3')2 reveals a 4 A widening of the minor groove and compression of the major groove along with a >18 degrees bend in the helix axis toward the major groove. This allosteric perturbation of the DNA helix provides a molecular basis for disruption of transcription factor-DNA interfaces by small molecules, a minimum step in chemical control of gene networks.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.