In this paper, we report studies concerning four variants of the G-quadruplex forming anti-HIV-integrase aptamer T30923, in which specific 2'-deoxyguanosines have been singly replaced by 8-methyl-2'-deoxyguanosine residues, with the aim to exploit the methyl group positioned in the G-quadruplex grooves as a steric probe to investigate the interaction aptamer/target. Although, the various modified aptamers differ in the localization of the methyl group, NMR, circular dichroism (CD), electrophoretic and molecular modeling data suggest that all of them preserve the ability to fold in a stable dimeric parallel G-quadruplex complex resembling that of their natural counterpart T30923. However, the biological data have shown that the T30923 variants are characterized by different efficiencies in inhibiting the HIV-integrase, thus suggesting the involvement of the G-quadruplex grooves in the aptamer/target interaction.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7460552 | PMC |
| http://dx.doi.org/10.3390/ijms21165637 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Selective Recognition of Oncogene Promoter C-Myc G-Quadruplex: Design, Synthesis, and In Vitro Evaluation of Naphthalimide and Imidazo[1,2-]pyrazines for Their Anticancer Activity.
ACS Appl Bio Mater
January 2025
Department of Chemistry and Biochemistry, Thapar Institute of Engineering and Technology, Patiala 147001, India.
c-Myc is a transcription factor that is overexpressed in most human cancers. Despite its challenging nature, we have developed a series of naphthalimide-imidazopyrazine conjugates to target c-Myc. The library of synthesized derivatives was tested for their anticancer activity against a nine-panel of cancer cell lines.
View Article and Find Full Text PDFTopology-selective photo-crosslinking of G-quadruplexes dual G-quartet and groove recognition.
Chem Commun (Camb)
November 2024
Department of Biotechnology and Life Science, Tokyo University of Agriculture and Technology, 2-24-16 Naka-cho, Koganei city, Tokyo 184-8588, Japan.
The novel photo-crosslinking ligand 6OTD-Bp, bearing an alkylamine benzophenone (Bp) with macrocyclic hexaoxazole (6OTD), was shown to preferentially ligate with hybrid G4s through recognizing both G-quartets and their characteristic wide groove. Higher crosslinking yield was observed for hybrid G4 with wider grooves.
View Article and Find Full Text PDFRationally Designed G-Quadruplex Selective "Turn-On" NIR Fluorescent Probe with Large Stokes Shift for Nucleic Acid Research-Based Applications.
ACS Appl Bio Mater
November 2024
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow 226031, India.
Guanine-rich DNA/RNA sequences can form Hoogsteen bonds to adopt noncanonical secondary structures called G-quadruplexes, and these have been associated with diverse cellular processes. There has been considerable research interest in the design of G4-interacting ligands for cellular probing of the G4 structure and understanding its associated biological function. Most of the fluorescent G4 ligands either do not have significant selectivity over other nucleic acid structures, have high Stokes shift, or are not in the near-infrared (NIR) region, which limits its cellular visualization.
View Article and Find Full Text PDFHigher-order G-quadruplex structures and porphyrin ligands: Towards a non-ambiguous relationship.
Int J Biol Macromol
May 2024
Department of Pharmacy, University of Naples Federico II, via Domenico Montesano 49, 80131 Naples, Italy. Electronic address:
Herein, we evaluated the interaction of the tetracationic porphyrin HTCPPSpm4 with three distinct DNA G-quadruplex (G4) models, i.e., the tetramolecular G4 d(TGGGGT) (Q), the 5'-5' stacked G4-dimer [d(CGGAGGT)] (Q), and a mixture of 5'-5' stacked G-wires [d(5'-CGGT-3'-3'-GGC-5')] (Q).
View Article and Find Full Text PDFComprehensive analysis of intramolecular G-quadruplex structures: furthering the understanding of their formalism.
Nucleic Acids Res
April 2024
Chemistry and Modeling for the Biology of Cancer, CNRS UMR9187, INSERM U1196, Institut Curie, PSL Research University, Université Paris-Saclay, CS 90030, 91401 ORSAYCedex, France.
G-quadruplexes (G4) are helical structures found in guanine-rich DNA or RNA sequences. Generally, their formalism is based on a few dozen structures, which can produce some inconsistencies or incompleteness. Using the website ASC-G4, we analyzed the structures of 333 intramolecular G4s, of all types, which allowed us to clarify some key concepts and present new information.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!