Polymorphic and Higher-Order G-Quadruplexes as Possible Transcription Regulators: Novel Perspectives for Future Anticancer Therapeutic Applications

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14740%2F22%3A00127513" target="_blank" >RIV/00216224:14740/22:00127513 - isvavai.cz</a>

Result on the web

<a href="https://www.mdpi.com/1424-8247/15/3/373" target="_blank" >https://www.mdpi.com/1424-8247/15/3/373</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/ph15030373" target="_blank" >10.3390/ph15030373</a>

Result language

angličtina

Original language name

Polymorphic and Higher-Order G-Quadruplexes as Possible Transcription Regulators: Novel Perspectives for Future Anticancer Therapeutic Applications

Original language description

In the past two decades, significant efforts have been put into designing small molecules to target selected genomic sites where DNA conformational rearrangements control gene expression. G-rich sequences at oncogene promoters are considered good points of intervention since, under specific environmental conditions, they can fold into non-canonical tetrahelical structures known as G-quadruplexes. However, emerging evidence points to a frequent lack of correlation between small molecule targeting of G-quadruplexes at gene promoters and the expression of the associated protein, which hampers pharmaceutical applications. The wide genomic localization of G-quadruplexes along with their highly polymorphic behavior may account for this scenario, suggesting the need for more focused drug design strategies. Here, we will summarize the G4 structural features that can be considered to fulfill this goal. In particular, by comparing a telomeric sequence with the well-characterized G-rich domain of the KIT promoter, we will address how multiple secondary structures might cooperate to control genome architecture at a higher level. If this holds true, the link between drug–DNA complex formation and the associated cellular effects will need to be revisited.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

30104 - Pharmacology and pharmacy

Project

<a href="/en/project/EF20_079%2F0017045" target="_blank" >EF20_079/0017045: MSCAfellow4@MUNI</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2022

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

PHARMACEUTICALS

ISSN

1424-8247

e-ISSN

—

Volume of the periodical

15

Issue of the periodical within the volume

3

Country of publishing house

CH - SWITZERLAND

Number of pages

13

Pages from-to

373

UT code for WoS article

000774500300001

EID of the result in the Scopus database

2-s2.0-85127572246