NDLI: Targeting telomerase and telomeres: a click chemistry approach towards highly selective G-quadruplex ligands

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Contents and Chemical Biology

Emerging Investigators issue

Contributors to the Emerging Investigators issue ( Molecular BioSystems Vol - 4 Issue - 6 )

Photocrosslinkers illuminate interactions in living cells

Enabling methodology for the end functionalisation of glycosaminoglycan oligosaccharides

Visualization of phosphatase activity in living cells with a FRET-based calcineurin activity sensor

Direct printing of trichlorosilanes on glass for selective protein adsorption and cell growth

2-Methoxycyclopentyl analogues of a Pseudomonas aeruginosa quorum sensing modulator

Light-activated deoxyguanosine: photochemical regulation of peroxidase activity

Toward autonomously operating molecular machines driven by transition-metal catalyst

DNA packaging via combinative self-assembly

A simple solid-phase synthesis of the ubiquitous bacterial signaling molecule, c-di-GMP and analogues

A chemical approach for detecting sulfenic acid-modified proteins in living cells

Acid cleavable PEG-lipids for applications in a ternary gene delivery vector

Design, synthesis and characterization of “clickable” 4-anilinoquinazoline kinase inhibitors

Design, synthesis, and evaluation of an isotopic labeling strategy for studying fatty acid–protein binding by NMR

Chemical site-selective prenylation of proteins

Visualizing the spatial distribution of secondary metabolites produced by marine cyanobacteria and sponges via MALDI-TOF imaging

Bifunctional molecules evade cytochrome P₄₅₀ metabolism by forming protective complexes with FK506-binding protein

Conformation and the sodium ion condensation on DNA and RNA structures in the presence of a neutral cosolute as a mimic of the intracellular media

Prediction of cardiac transcription networks based on molecular data and complex clinical phenotypes

Re-engineering a split-GFP reassembly screen to examine RING-domain interactions between BARD1 and BRCA1 mutants observed in cancer patients

Estimating P-coverage of biosynthetic pathways in DNA libraries and screening by genetic selection: biotin biosynthesis in the marine microorganism chromohalobacter

Control of bacterial biofilms with marine alkaloid derivatives

Characterization of TioF, a tryptophan 2,3-dioxygenase involved in 3-hydroxyquinaldic acid formation during thiocoraline biosynthesis

Targeting telomerase and telomeres: a click chemistry approach towards highly selective G-quadruplex ligands

A quantitative study of the recruitment potential of all intracellular tyrosine residues on EGFR, FGFR1 and IGF1R

A simple strategy for the creation of a recombinant lectin microarray

The unusual macrocycle forming thioesterase of mycolactone

Accurate measurements of protein interactions in cells via improved spatial image cross-correlation spectroscopy

Thermodynamic prediction of RNA–DNA duplex-forming regions in the human genome

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Molecular BioSystems Vol - 4 Issue - 5

Molecular BioSystems Vol - 4 Issue - 4

Molecular BioSystems Vol - 4 Issue - 3

Molecular BioSystems Vol - 4 Issue - 2

Molecular BioSystems Vol -3

Molecular BioSystems Vol -2

Targeting telomerase and telomeres: a click chemistry approach towards highly selective G-quadruplex ligands

Content Provider	Royal Society of Chemistry (RSC)
Author	Neidle, Stephen Gunaratnam, Mekala Moorhouse, Adam D. Haider, Shozeb Moses, John E. Munnur, Deeksha
Copyright Year	2008
Abstract	Maintenance of telomeres—specialized complexes that protect the ends of chromosomes, is undertaken by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but is absent in most normal cells. Targeting telomere maintenance mechanisms could potentially halt tumour growth across a broad spectrum of cancer types, with little cytotoxic effect outside cancer cells. Here, we describe in detail a new class of G-quadruplex binding ligands synthesized using a click chemistry approach. These ligands comprise a 1,3-di(1,2,3-triazol-4-yl)benzene pharmacophore, and display high levels of selectivity for interaction with G-quadruplex DNA vs. duplex DNA. The ability of these ligands to inhibit the enzymatic activity of telomerase correlates with their ability to stabilize quadruplex DNA, and with estimates of affinity calculated by molecular modeling.
Starting Page	629
Ending Page	642
Page Count	14
File Format	HTM / HTML PDF
ISSN	1742206X
Volume Number	4
Issue Number	6
Journal	Molecular BioSystems
DOI	10.1039/b801822g
Language	English
Publisher	Royal Society of Chemistry
Access Restriction	Open
Subject Keyword	Molecular modelling Enzyme Benzene DNA G-quadruplex Cytotoxicity Click chemistry Telomerase Telomere Pharmacophore Cancer Quadruplex videotape
Content Type	Text
Resource Type	Article
Subject	Molecular Biology Biotechnology

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Targeting human telomerase for cancer therapeutics.

Disubstituted 2-phenyl-benzopyranopyrimidine derivatives as a new type of highly selective ligands for telomeric G-quadruplex DNA

Stabilization of G-quadruplex DNA by highly selective ligands via click chemistry.

Treating Cancer by Targeting Telomeres and Telomerase

Targeting human telomerase for cancer therapeutics

Telomere Targeting Approaches in Cancer: Beyond Length Maintenance

Telomerase and drug resistance in cancer.

Coordinated Interactions of Multiple POT1-TPP1 Proteins with Telomere DNA

Human cathelicidin peptide LL37 binds telomeric G-quadruplex

Targeting telomerase and telomeres: a click chemistry approach towards highly selective G-quadruplex ligands

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