Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

Javier Ramos-Soriano; Maisie Holbrow-Wilshaw; Eliza Hunt; Y Jennifer Jiang; Pablo Peñalver; Juan C Morales; M Carmen Galan

doi:10.1039/d4cc03106g

Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

Javier Ramos-Soriano^*, Maisie Holbrow-Wilshaw, Eliza Hunt, Y Jennifer Jiang, Pablo Peñalver, Juan C Morales^*, M Carmen Galan^*

^*Corresponding author for this work

School of Chemistry

Research output: Contribution to journal › Article (Academic Journal) › peer-review

6 Citations (Scopus)

Abstract

Novel strategies against parasitic infections are of great importance. Here, we describe a G4 DNA ligand with subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC₅₀ MRC-5/T. brucei) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.

Original language	English
Pages (from-to)	11520-11523
Number of pages	4
Journal	Chemical communications (Cambridge, England)
Volume	60
Issue number	81
Early online date	13 Sept 2024
DOIs	https://doi.org/10.1039/d4cc03106g
Publication status	Published - 8 Oct 2024

Bibliographical note

Publisher Copyright:
© 2024 The Royal Society of Chemistry.

Research Groups and Themes

Organic & Biological
Bristol BioDesign Institute

Keywords

Ligands
G-Quadruplexes/drug effects
Trypanosoma brucei brucei/drug effects
Azo Compounds/chemistry
Drug Design
Humans
Antiparasitic Agents/chemistry
Binding Sites
Molecular Structure

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title = "Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design",

abstract = "Novel strategies against parasitic infections are of great importance. Here, we describe a G4 DNA ligand with subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC50 MRC-5/T. brucei) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.",

keywords = "Ligands, G-Quadruplexes/drug effects, Trypanosoma brucei brucei/drug effects, Azo Compounds/chemistry, Drug Design, Humans, Antiparasitic Agents/chemistry, Binding Sites, Molecular Structure",

author = "Javier Ramos-Soriano and Maisie Holbrow-Wilshaw and Eliza Hunt and Jiang, \{Y Jennifer\} and Pablo Pe{\~n}alver and Morales, \{Juan C\} and Galan, \{M Carmen\}",

note = "Publisher Copyright: {\textcopyright} 2024 The Royal Society of Chemistry.",

year = "2024",

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day = "8",

doi = "10.1039/d4cc03106g",

language = "English",

volume = "60",

pages = "11520--11523",

journal = "Chemical communications (Cambridge, England)",

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publisher = "Royal Society of Chemistry",

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TY - JOUR

T1 - Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

AU - Ramos-Soriano, Javier

AU - Holbrow-Wilshaw, Maisie

AU - Hunt, Eliza

AU - Jiang, Y Jennifer

AU - Peñalver, Pablo

AU - Morales, Juan C

AU - Galan, M Carmen

PY - 2024/10/8

Y1 - 2024/10/8

N2 - Novel strategies against parasitic infections are of great importance. Here, we describe a G4 DNA ligand with subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC50 MRC-5/T. brucei) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.

AB - Novel strategies against parasitic infections are of great importance. Here, we describe a G4 DNA ligand with subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC50 MRC-5/T. brucei) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.

KW - Ligands

KW - G-Quadruplexes/drug effects

KW - Trypanosoma brucei brucei/drug effects

KW - Azo Compounds/chemistry

KW - Drug Design

KW - Humans

KW - Antiparasitic Agents/chemistry

KW - Binding Sites

KW - Molecular Structure

U2 - 10.1039/d4cc03106g

DO - 10.1039/d4cc03106g

M3 - Article (Academic Journal)

C2 - 39308448

SN - 1359-7345

VL - 60

SP - 11520

EP - 11523

JO - Chemical communications (Cambridge, England)

JF - Chemical communications (Cambridge, England)

IS - 81

ER -

Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design

Abstract

Bibliographical note

Research Groups and Themes

Keywords

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