{"doi":"10.1021/ja204326w","title":"Contribution of Telomere G-Quadruplex Stabilization to the Inhibition of Telomerase-Mediated Telomere Extension by Chemical Ligands","abstract":null,"journal":"Journal of the American Chemical Society","year":2011,"id":630061,"datarank":0.5244761342199721,"base_score":3.4965075614664802,"endowment":3.4965075614664802,"self_citation_contribution":0.5244761342199721,"citation_network_contribution":0.0,"self_endowment_contribution":0.5244761342199721,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":32,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1400010,"name":"Quan Wang","orcid":"0000-0001-5148-5210","position":1,"is_corresponding":false},{"id":1632094,"name":"Jia-quan Liu","orcid":null,"position":2,"is_corresponding":false},{"id":1632095,"name":"Yu-hua Hao","orcid":null,"position":3,"is_corresponding":false},{"id":553076,"name":"Zheng Tan","orcid":null,"position":4,"is_corresponding":false},{"id":1632093,"name":"Chang-yue Chen","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Contribution of Telomere G-Quadruplex Stabilization to the Inhibition of Telomerase-Mediated Telomere Extension by Chemical Ligands","abstract":"Inhibition of telomerase activity through stabilizing telomere G-quadruplex with small chemical ligands is emerging as a novel strategy for cancer therapy. For the large number of ligands that have been reported to inhibit telomerase activity, it is difficult to validate the contribution of G-quadruplex stabilization to the overall inhibition. Using a modified telomere repeat amplification protocol (TRAP) method to differentiate the telomere G-quadruplex independent effect from dependent ones, we analyzed several ligands that have high affinity and/or selectivity to telomere G-quadruplex. Our results show that these ligands effectively inhibited telomerase activity in the absence of telomere G-quadruplex. The expected G-quadruplex-dependent inhibition was only obvious for the cationic ligands at low K(+) concentration, but it dramatically decreased at physiological concentration of K(+). These observations demonstrate that the ligands are much more than G-quadruplex stabilizers with a strong G-quadruplex-irrelevant off-target effect. They inhibit telomerase via multiple pathways in which stabilization of telomere G-quadruplex may only make a minor or neglectable contribution under physiologically relevant conditions depending on the stability of telomere G-quadruplex under ligand-free conditions.","is_dataset_classified":null,"base_score":3.4965075614664802,"endowment":3.4965075614664802,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"21846102","pmcid":null,"openalex_id":"https://openalex.org/W1970283190","authors":[],"funders":[],"total_grants":0,"fwci":1.2165,"citation_percentile":0.76837543,"influential_citations":0,"citation_trend":[{"year":2012,"count":3},{"year":2013,"count":2},{"year":2014,"count":5},{"year":2015,"count":4},{"year":2016,"count":1},{"year":2018,"count":1},{"year":2019,"count":2},{"year":2020,"count":3},{"year":2021,"count":1},{"year":2022,"count":4},{"year":2023,"count":2},{"year":2024,"count":2},{"year":2025,"count":1}],"oa_status":"closed","license":null,"oa_locations":[{"url":"https://pubs.acs.org/doi/pdf/10.1021/ja204326w","host_type":"publisher"},{"url":"https://doi.org/10.1021/ja204326w","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/21846102","host_type":"repository"}],"fields_of_study":["Advanced biosensing and bioanalysis techniques","DNA and Nucleic Acid Chemistry","RNA Interference and Gene Delivery"],"mesh_terms":["Carbazoles","Dose-Response Relationship, Drug","Humans","Indoles","Ligands","Organometallic Compounds","Pyridinium Compounds","Structure-Activity Relationship","Telomere","Telomerase","G-Quadruplexes"],"keywords":["Telomere","Telomerase","G-quadruplex","Chemistry","Ligand (biochemistry)","Biochemistry","Biophysics","Stereochemistry","DNA","Receptor","Gene","Biology"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-05T20:22:40.655079Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}