Contact and support
Need help, have a question, or want to contact the ResearchHub team?
© 2026 ResearchHub. Built for responsible scholarly connection.
Privacy-aware community infrastructureResearch graph
References from The Pharmacologic Profile of ART6043, a First-in-Class Clinical DNA Polymerase Theta Polymerase Domain Inhibitor Potentiating PARP Inhibitor Efficacy. Local targets link to admitted publications; unresolved targets remain external evidence.
Multifaceted nature of DNA polymerase θ
10.3390/ijms24043619 · 2023 · External reference
Genome protection by DNA polymerase θ
10.1146/annurev-genet-072920-041046 · 2022 · External reference
Mechanism, cellular functions and cancer roles of polymerase-theta-mediated DNA end joining
10.1038/s41580-021-00405-2 · 2022 · External reference
DNA polymerase theta is preferentially expressed in lymphoid tissues and upregulated in human cancers
10.1002/ijc.11666 · 2004 · External reference
Overexpression of POLQ confers a poor prognosis in early breast cancer patients
10.18632/oncotarget.124 · 2010 · External reference
DNA polymerase theta up-regulation is associated with poor survival in breast cancer, perturbs DNA replication, and promotes genetic instability
10.1073/pnas.0910759107 · 2010 · External reference
Targeting polymerase θ impairs tumorigenesis and enhances radiosensitivity in lung adenocarcinoma
10.1111/cas.15727 · 2023 · External reference
POLQ immunostaining behaves as a prognostic factor for pancreatic carcinoma
10.3389/fonc.2024.1433179 · 2024 · External reference
Overexpression of human DNA polymerase theta is a biomarker of aggressive and DNA repair-deficient papillary thyroid cancers
10.1016/j.surg.2024.05.006 · 2024 · External reference
Phenotype-based identification of mouse chromosome instability mutants
10.1093/genetics/163.3.1031 · 2003 · External reference
The mouse genomic instability mutation chaos1 is an allele of Polq that exhibits genetic interaction with Atm
10.1128/mcb.24.23.10381-10389.2004 · 2004 · External reference
Targeting polymerase theta (POLθ) for cancer therapy
10.1007/978-3-031-30065-3_15 · 2023 · External reference
Polθ: emerging synthetic lethal partner in homologous recombination-deficient tumors
10.1038/s41417-024-00815-2 · 2024 · External reference
Small molecules targeting DNA polymerase theta (POLθ) as promising synthetic lethal agents for precision cancer therapy
10.1021/acs.jmedchem.2c02101 · 2023 · External reference
Polθ inhibition: an anticancer therapy for HR-deficient tumours
10.3390/ijms24010319 · 2022 · External reference
Targeting non-homologous and alternative end joining repair to enhance cancer radiosensitivity
10.1016/j.semradonc.2021.09.007 · 2022 · External reference
Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance
10.1038/s41467-021-23463-8 · 2021 · External reference
Discovery, characterization, and structure-based optimization of small-molecule in vitro and in vivo probes for human DNA polymerase theta
10.1021/acs.jmedchem.2c01142 · 2022 · External reference
Small-molecule Polθ inhibitors provide safe and effective tumor radiosensitization in preclinical models
10.1158/1078-0432.ccr-22-2977 · 2023 · External reference
Identification of RP-6685, an orally bioavailable compound that inhibits the DNA polymerase activity of Polθ
10.1021/acs.jmedchem.2c00998 · 2022 · External reference
A first-in-class polymerase theta inhibitor selectively targets homologous-recombination-deficient tumors
10.1038/s43018-021-00203-x · 2021 · External reference
The shieldin complex mediates 53BP1-dependent DNA repair
10.1038/s41586-018-0340-7 · 2018 · External reference
DNA repair network analysis reveals shieldin as a key regulator of NHEJ and PARP inhibitor sensitivity
10.1016/j.cell.2018.03.050 · 2018 · External reference
Shieldin complex promotes DNA end-joining and counters homologous recombination in BRCA1-null cells
10.1038/s41556-018-0140-1 · 2018 · External reference
POLQ seals post-replicative ssDNA gaps to maintain genome stability in BRCA-deficient cancer cells
10.1016/j.molcel.2022.11.008 · 2022 · External reference
Mechanisms of synthetic lethality between BRCA1/2 and 53BP1 deficiencies and DNA polymerase theta targeting
10.1038/s41467-023-43677-2 · 2023 · External reference
Clinical BRCA1/2 reversion analysis identifies hotspot mutations and predicted neoantigens associated with therapy resistance
10.1158/2159-8290.cd-19-1485 · 2020 · External reference
Elucidating acquired PARP inhibitor resistance in advanced prostate cancer
10.1016/j.ccell.2024.10.015 · 2024 · External reference
A meta-analysis of reversion mutations in BRCA genes identifies signatures of DNA end-joining repair mechanisms driving therapy resistance
10.1016/j.annonc.2020.10.470 · 2021 · External reference
POLQ (Pol theta), a DNA polymerase and DNA-dependent ATPase in human cells
10.1093/nar/gkg814 · 2003 · External reference
Probing the structure and function of polymerase θ helicase-like domain
10.1016/j.dnarep.2022.103358 · 2022 · External reference
Essential roles for polymerase θ-mediated end joining in the repair of chromosome breaks
10.1016/j.molcel.2016.06.020 · 2016 · External reference
Discovery of a small-molecule inhibitor that traps Polθ on DNA and synergizes with PARP inhibitors
10.1038/s41467-024-46593-1 · 2024 · External reference
The discovery of RP-2119: a potent, selective, and orally bioavailable Polθ ATPase inhibitor
10.1021/acs.jmedchem.5c02103 · 2025 · External reference
Novobiocin blocks nucleic acid binding to Polθ and inhibits stimulation of its ATPase activity
10.1093/nar/gkad727 · 2023 · External reference
Combenefit: an interactive platform for the analysis and visualization of drug combinations
10.1093/bioinformatics/btw230 · 2016 · External reference
Modelling of compound combination effects and applications to efficacy and toxicity: state-of-the-art, challenges and perspectives
10.1016/j.drudis.2015.09.003 · 2016 · External reference
BRCA-deficient mouse mammary tumor organoids to study cancer-drug resistance
10.1038/nmeth.4535 · 2018 · External reference
Quantitative, titratable and high-throughput reporter assays to measure DNA double strand break repair activity in cells
10.1093/nar/gkad1196 · 2024 · External reference
CellTool: an open-source software combining bio-image analysis and mathematical modeling for the study of DNA repair dynamics
10.3390/ijms242316784 · 2023 · External reference
NanoBRETTM live-cell kinase selectivity profiling adapted for high-throughput screening
10.1007/978-1-0716-3397-7_8 · 2023 · External reference
Mammalian polymerase θ promotes alternative NHEJ and suppresses recombination
10.1038/nature14157 · 2015 · External reference
Homologous-recombination-deficient tumours are dependent on Polθ-mediated repair
10.1038/nature14184 · 2015 · External reference
RHINO directs MMEJ to repair DNA breaks in mitosis
10.1126/science.adh3694 · 2023 · External reference
A comparative pharmacokinetic study of PARP inhibitors demonstrates favorable properties for niraparib efficacy in preclinical tumor models
10.18632/oncotarget.26354 · 2018 · External reference
RTx-303, an orally bioavailable Polθ polymerase inhibitor that potentiates PARP inhibitors in BRCA mutant tumors
10.1021/acs.jmedchem.5c00551 · 2025 · External reference
Discovery of SY-589, a highly potent and orally bioavailable Polθ helicase inhibitor for the treatment of HR-deficient tumors
10.1021/acs.jmedchem.5c02689 · 2026 · External reference
A small interfering RNA screen of genes involved in DNA repair identifies tumor-specific radiosensitization by POLQ knockdown
10.1158/0008-5472.can-09-4040 · 2010 · External reference
Lack of DNA polymerase theta (POLQ) radiosensitizes bone marrow stromal cells in vitro and increases reticulocyte micronuclei after total-body irradiation
10.1667/rr1598.1 · 2009 · External reference
924MO First data disclosure of the first-in-class DNA polymerase theta inhibitor, ART6043, as monotherapy and in combination with olaparib, in patients with molecularly-selected advanced solid tumors
10.1016/j.annonc.2025.08.1493 · 2025 · External reference
