ArticleStructure (London, England : 1993)2015
Structural Basis of Telomerase Inhibition by the Highly Specific BIBR1532.
Article in Structure (London, England : 1993), 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 71 papers, 1 of them a synthesis that pooled it.
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Who cites it
71 citing papers in PubMed, 1 synthesis or guideline pooled it, 126 citations in OpenAlex.
- The role of telomerase reverse transcriptase (TERT) promoter mutations in prognosis in bladder cancer.Bioengineered · 2021Pooled it
- The Different Faces of the Selective Human Telomerase Inhibitor: BIBR1532 and Its Derivatives.Current issues in molecular biology · 2026Article
- Cryo-EM sheds light on the mechanism of human telomerase inhibition by BIBR1532.Nature chemical biology · 2026Article
- Structures of human telomerase with BIBR1532 reveal novel mechanism of inhibition.Nature chemical biology · 2026Article
- Targeting Telomerase in Cancer: Vaccine-Based Strategies, Clinical Evidence, and Synergy with Immunotherapy.Diseases (Basel, Switzerland) · 2026Review
- Repurposing MK0873 as a non-covalent hTERT-Targeting compound: a proof of concept study.Frontiers in aging · 2026Article
- Exploiting the Achilles' heel of cancer through a structure-based drug-repurposing approach and experimental validation of top drugs using the TRAP assay.Molecular diversity · 2025Article
- High-Throughput Screening Tool to Identify Small Molecule Inhibitors of Telomerase.ACS chemical biology · 2025Article
- Key genes altered in glioblastoma based on bioinformatics (Review).Oncology letters · 2025Review
- Beyond Telomeres: Unveiling the Extratelomeric Functions of TERT in B-Cell Malignancies.Cancers · 2025Review
- Effect of host telomerase inhibition on human cytomegalovirus.Journal of virology · 2025Article
- Essential Oil fromMolecules (Basel, Switzerland) · 2025Article
- Telomerase in cancer- ongoing quest and future discoveries.Molecular biology reports · 2025Review
- A Review of Telomere Attrition in Cancer and Aging: Current Molecular Insights and Future Therapeutic Approaches.Cancers · 2025Review
- Chitosan capped-NLCs enhanced codelivery of gefitinib and simvastatin into MDR HCC: impact of compositions on cell death, JNK3, and Telomerase.Oncology research · 2025Article
- Recent progress in human telomerase structure and its therapeutic targeting.Frontiers in molecular biosciences · 2025Review
- Design of Potent Telomerase Inhibitors using Ligand-based Approaches and Molecular Dynamics Simulations Studies.Current drug discovery technologies · 2025Article
- Complex Biophysical and Computational Analyses of G-Quadruplex Ligands: The Porphyrin Stacks Back.Chemistry (Weinheim an der Bergstrasse, Germany) · 2024Article
- Genomic landscape of malignant phyllodes tumors reveals multiple targetable opportunities.The oncologist · 2024Article
- A High-Throughput Immune-Oncology Screen Identifies Immunostimulatory Properties of Cytotoxic Chemotherapy Agents in TNBC.Cancers · 2024Article
11 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
BIBR1532 is a highly specific telomerase inhibitor, although the molecular basis for inhibition is unknown. Here we present the crystal structure of BIBR1532 bound to Tribolium castaneum catalytic subunit of telomerase (tcTERT). BIBR1532 binds to a conserved hydrophobic pocket (FVYL motif) on the outer surface of the thumb domain. The FVYL motif is near TRBD residues that bind the activation domain (CR4/5) of hTER. RNA binding assays show that the human TERT (hTERT) thumb domain binds the P6.1 stem loop of CR4/5 in vitro. hTERT mutations of the FVYL pocket alter wild-type CR4/5 binding and cause telomere attrition in cells. Furthermore, the hTERT FVYL mutations V1025F, N1028H, and V1090M are implicated in dyskeratosis congenita and aplastic anemia, further supporting the biological and clinical relevance of this novel motif. We propose that CR4/5 contacts with the telomerase thumb domain contribute to telomerase ribonucleoprotein assembly and promote enzymatic activity.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.