G-quadruplex, Friend or Foe: The Role of the G-quartet in Anticancer Strategies

Josué Carvalho; Jean Louis Mergny; Gilmar F. Salgado; João A. Queiroz; Carla Cruz

doi:10.1016/j.molmed.2020.05.002

G-quadruplex, Friend or Foe: The Role of the G-quartet in Anticancer Strategies

Josué Carvalho
, Jean Louis Mergny
, Gilmar F. Salgado
, João A. Queiroz
, Carla Cruz

Universidade da Beira Interior
Univ. Bordeaux
of Sciences

Research output: Contribution to journal › Review article › peer-review

Abstract

The clinical applicability of G-quadruplexes (G4s) as anticancer drugs is currently being evaluated. Several G4 ligands and aptamers are undergoing clinical trials following the notable examples of quarfloxin and AS1411, respectively. In this review, we summarize the latest achievements and breakthroughs in the use of G4 nucleic acids as both therapeutic tools (‘friends’, as healing anticancer drugs) and targets (‘foes’, within the harmful cancer cell), particularly using aptamers and quadruplex-targeted ligands, respectively. We explore the recent research on synthetic G4 ligands toward the discovery of anticancer therapeutics and their mechanism of action. Additionally, we highlight recent advances in chemical and structural biology that enable the design of specific G4 aptamers to be used as novel anticancer agents.

Original language	English
Pages (from-to)	848-861
Number of pages	14
Journal	Trends in Molecular Medicine
Volume	26
Issue number	9
DOIs	https://doi.org/10.1016/j.molmed.2020.05.002
Publication status	Published - 1 Sept 2020
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

G-quadruplex
anticancer strategy
aptamers
cell regulation
drug discovery
ligands

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10.1016/j.molmed.2020.05.002

Cite this

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title = "G-quadruplex, Friend or Foe: The Role of the G-quartet in Anticancer Strategies",

abstract = "The clinical applicability of G-quadruplexes (G4s) as anticancer drugs is currently being evaluated. Several G4 ligands and aptamers are undergoing clinical trials following the notable examples of quarfloxin and AS1411, respectively. In this review, we summarize the latest achievements and breakthroughs in the use of G4 nucleic acids as both therapeutic tools ({\textquoteleft}friends{\textquoteright}, as healing anticancer drugs) and targets ({\textquoteleft}foes{\textquoteright}, within the harmful cancer cell), particularly using aptamers and quadruplex-targeted ligands, respectively. We explore the recent research on synthetic G4 ligands toward the discovery of anticancer therapeutics and their mechanism of action. Additionally, we highlight recent advances in chemical and structural biology that enable the design of specific G4 aptamers to be used as novel anticancer agents.",

keywords = "G-quadruplex, anticancer strategy, aptamers, cell regulation, drug discovery, ligands",

author = "Josu{\'e} Carvalho and Mergny, \{Jean Louis\} and Salgado, \{Gilmar F.\} and Queiroz, \{Jo{\~a}o A.\} and Carla Cruz",

note = "Publisher Copyright: {\textcopyright} 2020 Elsevier Ltd",

year = "2020",

month = sep,

day = "1",

doi = "10.1016/j.molmed.2020.05.002",

language = "English",

volume = "26",

pages = "848--861",

journal = "Trends in Molecular Medicine",

issn = "1471-4914",

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}

TY - JOUR

T1 - G-quadruplex, Friend or Foe

T2 - The Role of the G-quartet in Anticancer Strategies

AU - Carvalho, Josué

AU - Mergny, Jean Louis

AU - Salgado, Gilmar F.

AU - Queiroz, João A.

AU - Cruz, Carla

PY - 2020/9/1

Y1 - 2020/9/1

N2 - The clinical applicability of G-quadruplexes (G4s) as anticancer drugs is currently being evaluated. Several G4 ligands and aptamers are undergoing clinical trials following the notable examples of quarfloxin and AS1411, respectively. In this review, we summarize the latest achievements and breakthroughs in the use of G4 nucleic acids as both therapeutic tools (‘friends’, as healing anticancer drugs) and targets (‘foes’, within the harmful cancer cell), particularly using aptamers and quadruplex-targeted ligands, respectively. We explore the recent research on synthetic G4 ligands toward the discovery of anticancer therapeutics and their mechanism of action. Additionally, we highlight recent advances in chemical and structural biology that enable the design of specific G4 aptamers to be used as novel anticancer agents.

AB - The clinical applicability of G-quadruplexes (G4s) as anticancer drugs is currently being evaluated. Several G4 ligands and aptamers are undergoing clinical trials following the notable examples of quarfloxin and AS1411, respectively. In this review, we summarize the latest achievements and breakthroughs in the use of G4 nucleic acids as both therapeutic tools (‘friends’, as healing anticancer drugs) and targets (‘foes’, within the harmful cancer cell), particularly using aptamers and quadruplex-targeted ligands, respectively. We explore the recent research on synthetic G4 ligands toward the discovery of anticancer therapeutics and their mechanism of action. Additionally, we highlight recent advances in chemical and structural biology that enable the design of specific G4 aptamers to be used as novel anticancer agents.

KW - G-quadruplex

KW - anticancer strategy

KW - aptamers

KW - cell regulation

KW - drug discovery

KW - ligands

U2 - 10.1016/j.molmed.2020.05.002

DO - 10.1016/j.molmed.2020.05.002

M3 - Review article

C2 - 32467069

AN - SCOPUS:85085353394

SN - 1471-4914

VL - 26

SP - 848

EP - 861

JO - Trends in Molecular Medicine

JF - Trends in Molecular Medicine

IS - 9

ER -

G-quadruplex, Friend or Foe: The Role of the G-quartet in Anticancer Strategies

Abstract

UN SDGs

Keywords

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