High throughput screening of a new fluorescent G-quadruplex ligand having telomerase inhibitory activity in human A549 cells

Sourav Ghosh; Debapriya De; Victor Banerjee; Soumyajit Biswas; Utpal Ghosh

doi:10.1080/15257770.2023.2188220

High throughput screening of a new fluorescent G-quadruplex ligand having telomerase inhibitory activity in human A549 cells

Sourav Ghosh, Debapriya De, Victor Banerjee, Soumyajit Biswas, Utpal Ghosh

Research output: Contribution to journal › Article › peer-review

1 Scopus citations

Abstract

Identification of a new G-quadruplex ligand having anti-telomerase activity would be a promising strategy for cancer therapy. The screened compound from ZINC database using docking studies was experimentally verified for its binding with three different telomeric G-quadruplex DNA sequences and anti-telomerase activity in A549 cells. Identified compound is an intrinsic fluorescent molecule, permeable to live cells and has a higher affinity to 22AG out of three different telomeric G-quadruplex DNA. It showed cytotoxicity and a significant reduction of telomerase activity in human A549 cells at a very low dose. So, this compound has a good anti-cancer effect.

Original language	English
Pages (from-to)	696-717
Number of pages	22
Journal	Nucleosides, Nucleotides and Nucleic Acids
Volume	42
Issue number	9
DOIs	https://doi.org/10.1080/15257770.2023.2188220
State	Published - 1 Jan 2023
Externally published	Yes

Keywords

CD analysis
G-quadruplex structure
G4 FID assay
ZINC database
fluorescence
telomerase activity

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Genetics

UN SDGs

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

Access to Document

10.1080/15257770.2023.2188220

Cite this

@article{10ce2c5d069d435a9dd20d1fd371ddc1,

title = "High throughput screening of a new fluorescent G-quadruplex ligand having telomerase inhibitory activity in human A549 cells",

abstract = "Identification of a new G-quadruplex ligand having anti-telomerase activity would be a promising strategy for cancer therapy. The screened compound from ZINC database using docking studies was experimentally verified for its binding with three different telomeric G-quadruplex DNA sequences and anti-telomerase activity in A549 cells. Identified compound is an intrinsic fluorescent molecule, permeable to live cells and has a higher affinity to 22AG out of three different telomeric G-quadruplex DNA. It showed cytotoxicity and a significant reduction of telomerase activity in human A549 cells at a very low dose. So, this compound has a good anti-cancer effect.",

keywords = "CD analysis, G-quadruplex structure, G4 FID assay, ZINC database, fluorescence, telomerase activity",

author = "Sourav Ghosh and Debapriya De and Victor Banerjee and Soumyajit Biswas and Utpal Ghosh",

note = "Publisher Copyright: {\textcopyright} 2023 Taylor \& Francis Group, LLC.",

year = "2023",

month = jan,

day = "1",

doi = "10.1080/15257770.2023.2188220",

language = "English",

volume = "42",

pages = "696--717",

journal = "Nucleosides, Nucleotides and Nucleic Acids",

issn = "1525-7770",

publisher = "Taylor and Francis Ltd.",

number = "9",

}

TY - JOUR

T1 - High throughput screening of a new fluorescent G-quadruplex ligand having telomerase inhibitory activity in human A549 cells

AU - Ghosh, Sourav

AU - De, Debapriya

AU - Banerjee, Victor

AU - Biswas, Soumyajit

AU - Ghosh, Utpal

PY - 2023/1/1

Y1 - 2023/1/1

N2 - Identification of a new G-quadruplex ligand having anti-telomerase activity would be a promising strategy for cancer therapy. The screened compound from ZINC database using docking studies was experimentally verified for its binding with three different telomeric G-quadruplex DNA sequences and anti-telomerase activity in A549 cells. Identified compound is an intrinsic fluorescent molecule, permeable to live cells and has a higher affinity to 22AG out of three different telomeric G-quadruplex DNA. It showed cytotoxicity and a significant reduction of telomerase activity in human A549 cells at a very low dose. So, this compound has a good anti-cancer effect.

AB - Identification of a new G-quadruplex ligand having anti-telomerase activity would be a promising strategy for cancer therapy. The screened compound from ZINC database using docking studies was experimentally verified for its binding with three different telomeric G-quadruplex DNA sequences and anti-telomerase activity in A549 cells. Identified compound is an intrinsic fluorescent molecule, permeable to live cells and has a higher affinity to 22AG out of three different telomeric G-quadruplex DNA. It showed cytotoxicity and a significant reduction of telomerase activity in human A549 cells at a very low dose. So, this compound has a good anti-cancer effect.

KW - CD analysis

KW - G-quadruplex structure

KW - G4 FID assay

KW - ZINC database

KW - fluorescence

KW - telomerase activity

UR - https://www.scopus.com/pages/publications/85150743090

U2 - 10.1080/15257770.2023.2188220

DO - 10.1080/15257770.2023.2188220

M3 - Article

C2 - 36919622

AN - SCOPUS:85150743090

SN - 1525-7770

VL - 42

SP - 696

EP - 717

JO - Nucleosides, Nucleotides and Nucleic Acids

JF - Nucleosides, Nucleotides and Nucleic Acids

IS - 9

ER -

High throughput screening of a new fluorescent G-quadruplex ligand having telomerase inhibitory activity in human A549 cells

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this