PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 25981734-8 2015 Of the four tested PARP-1 inhibitors only AZD2461 strongly affected cell cycle progression. AZD2461 42-49 poly(ADP-ribose) polymerase 1 Homo sapiens 19-25 27550455-0 2016 The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models. AZD2461 19-26 poly (ADP-ribose) polymerase family, member 1 Mus musculus 4-8 27550455-0 2016 The PARP Inhibitor AZD2461 Provides Insights into the Role of PARP3 Inhibition for Both Synthetic Lethality and Tolerability with Chemotherapy in Preclinical Models. AZD2461 19-26 poly (ADP-ribose) polymerase family, member 3 Mus musculus 62-67 27550455-1 2016 The PARP inhibitor AZD2461 was developed as a next-generation agent following olaparib, the first PARP inhibitor approved for cancer therapy. AZD2461 19-26 poly (ADP-ribose) polymerase family, member 1 Mus musculus 4-8 27550455-1 2016 The PARP inhibitor AZD2461 was developed as a next-generation agent following olaparib, the first PARP inhibitor approved for cancer therapy. AZD2461 19-26 poly (ADP-ribose) polymerase family, member 1 Mus musculus 98-102 26100884-6 2015 Indeed, resistance could be circumvented by using another PARP inhibitor, AZD2461, which is a poor Pgp substrate. AZD2461 74-81 poly (ADP-ribose) polymerase family, member 1 Mus musculus 58-62 26100884-6 2015 Indeed, resistance could be circumvented by using another PARP inhibitor, AZD2461, which is a poor Pgp substrate. AZD2461 74-81 phosphoglycolate phosphatase Mus musculus 99-102 23103855-5 2013 Importantly, PARPi resistance was minimized by long-term treatment with the novel PARP inhibitor AZD2461, which is a poor P-glycoprotein substrate. AZD2461 97-104 poly (ADP-ribose) polymerase family, member 1 Mus musculus 13-17 25337581-7 2014 RESULTS: Unlike NU1025, AZD2461, a new PARP-1 inhibitor, markedly reduced the numbers of living MCF-7 and SKBr-3 cells. AZD2461 24-31 poly(ADP-ribose) polymerase 1 Homo sapiens 39-45 25337581-10 2014 CONCLUSIONS: Our data show that inhibition of PARP-1 by AZD2461 is synthetically lethal for NU1025-resistant MCF-7 and SKBr-3 breast cancer cells. AZD2461 56-63 poly(ADP-ribose) polymerase 1 Homo sapiens 46-52 34653407-0 2021 Anticancer effect of AZD2461 PARP inhibitor against colon cancer cells carrying wt or dysfunctional p53. AZD2461 21-28 poly(ADP-ribose) polymerase 1 Homo sapiens 29-33 34728235-2 2022 Here we show that the PARP-1/2/3 inhibitor AZD2461 in combination with the CHK1 inhibitor UCN-01 altered the DNA damage response and reduced cell proliferation in PEL cells, an aggressive B cell lymphoma highly resistant to chemotherapies. AZD2461 43-50 poly(ADP-ribose) polymerase 1 Homo sapiens 22-32 34728235-3 2022 AZD2461/UCN-01 combination activated p53/p21 and downregulated c-Myc in these cells, leading to a reduced expression level of RAD51, molecule involved in DNA repair. AZD2461 0-7 tumor protein p53 Homo sapiens 37-40 34728235-3 2022 AZD2461/UCN-01 combination activated p53/p21 and downregulated c-Myc in these cells, leading to a reduced expression level of RAD51, molecule involved in DNA repair. AZD2461 0-7 H3 histone pseudogene 16 Homo sapiens 41-44 34728235-3 2022 AZD2461/UCN-01 combination activated p53/p21 and downregulated c-Myc in these cells, leading to a reduced expression level of RAD51, molecule involved in DNA repair. AZD2461 0-7 MYC proto-oncogene, bHLH transcription factor Homo sapiens 63-68 34728235-3 2022 AZD2461/UCN-01 combination activated p53/p21 and downregulated c-Myc in these cells, leading to a reduced expression level of RAD51, molecule involved in DNA repair. AZD2461 0-7 RAD51 recombinase Homo sapiens 126-131 34728235-4 2022 The effect of AZD2461/UCN-01 on c-Myc and p53/p21 was inter-dependent and, besides impairing cell proliferation, contributed to the activation of the replicative cycle of KSHV, carried in a latent state in PEL cells. AZD2461 14-21 MYC proto-oncogene, bHLH transcription factor Homo sapiens 32-37 34728235-4 2022 The effect of AZD2461/UCN-01 on c-Myc and p53/p21 was inter-dependent and, besides impairing cell proliferation, contributed to the activation of the replicative cycle of KSHV, carried in a latent state in PEL cells. AZD2461 14-21 tumor protein p53 Homo sapiens 42-45 34728235-4 2022 The effect of AZD2461/UCN-01 on c-Myc and p53/p21 was inter-dependent and, besides impairing cell proliferation, contributed to the activation of the replicative cycle of KSHV, carried in a latent state in PEL cells. AZD2461 14-21 H3 histone pseudogene 16 Homo sapiens 46-49 34653407-0 2021 Anticancer effect of AZD2461 PARP inhibitor against colon cancer cells carrying wt or dysfunctional p53. AZD2461 21-28 tumor protein p53 Homo sapiens 100-103 34653407-5 2021 In this study, we addressed this topic by using a well-tolerated PARP 1/2/3 inhibitor, namely AZD2461, against colon cancer cell lines with different p53 status. AZD2461 94-101 poly(ADP-ribose) polymerase 1 Homo sapiens 65-75 34653407-6 2021 We found that AZD2461 reduced cell proliferation in wtp53 and p53-/- cancer cells by increasing ROS and DNA damage, while R273H mutant (mut) p53 counteracted these effects. AZD2461 14-21 tumor protein p53 Homo sapiens 62-65 34653407-7 2021 Moreover, AZD2461 improved the reduction of cell proliferation by low dose radiation (IR) in wtp53 cancer cells, in which a down-regulation of BRCA-1 occurred. AZD2461 10-17 BRCA1 DNA repair associated Homo sapiens 143-149 34653407-8 2021 AZD2461 did not affect cell proliferation of mutp53 colon cancer cells also in combination with low dose radiation, suggesting that only wt p53 or p53 null colon cancer cells could benefit AZD2461 treatment. AZD2461 189-196 tumor protein p53 Homo sapiens 140-143 34653407-8 2021 AZD2461 did not affect cell proliferation of mutp53 colon cancer cells also in combination with low dose radiation, suggesting that only wt p53 or p53 null colon cancer cells could benefit AZD2461 treatment. AZD2461 189-196 tumor protein p53 Homo sapiens 147-150 32342268-0 2020 [18F]AZD2461, an Insight on Difference in PARP Binding Profiles for DNA Damage Response PET Imaging. AZD2461 5-12 poly (ADP-ribose) polymerase family, member 1 Mus musculus 42-46 35526484-4 2022 Indeed, PARP and CHK1 inhibition by AZD2461 and UCN-01, by downregulating c-Myc, reduced the expression of XBP1s, constitutively expressed in these cells, and upregulated CHOP. AZD2461 36-43 collagen type XI alpha 2 chain Homo sapiens 8-12 35526484-4 2022 Indeed, PARP and CHK1 inhibition by AZD2461 and UCN-01, by downregulating c-Myc, reduced the expression of XBP1s, constitutively expressed in these cells, and upregulated CHOP. AZD2461 36-43 checkpoint kinase 1 Homo sapiens 17-21 35526484-4 2022 Indeed, PARP and CHK1 inhibition by AZD2461 and UCN-01, by downregulating c-Myc, reduced the expression of XBP1s, constitutively expressed in these cells, and upregulated CHOP. AZD2461 36-43 MYC proto-oncogene, bHLH transcription factor Homo sapiens 74-79 35526484-4 2022 Indeed, PARP and CHK1 inhibition by AZD2461 and UCN-01, by downregulating c-Myc, reduced the expression of XBP1s, constitutively expressed in these cells, and upregulated CHOP. AZD2461 36-43 DNA damage inducible transcript 3 Homo sapiens 171-175 35216385-3 2022 In this study, we found that TSA and, even more effectively, VPA synergized with AZD2461, PARP1, 2 and 3 inhibitor (PARPi) to induce DNA damage and reduce pancreatic cancer cell survival. AZD2461 81-88 poly(ADP-ribose) polymerase 1 Homo sapiens 90-104 32342268-3 2020 Herein, we propose to study AZD2461, a PARP inhibitor with lower affinity towards PARP3, and to investigate its potential for PARP targeting in vivo. AZD2461 28-35 poly (ADP-ribose) polymerase family, member 1 Mus musculus 39-43 32342268-3 2020 Herein, we propose to study AZD2461, a PARP inhibitor with lower affinity towards PARP3, and to investigate its potential for PARP targeting in vivo. AZD2461 28-35 poly (ADP-ribose) polymerase family, member 3 Mus musculus 82-87 32342268-3 2020 Herein, we propose to study AZD2461, a PARP inhibitor with lower affinity towards PARP3, and to investigate its potential for PARP targeting in vivo. AZD2461 28-35 poly (ADP-ribose) polymerase family, member 1 Mus musculus 82-86 32342268-4 2020 METHODS: Using the Cu-mediated 18F-fluorodeboronation of a carefully designed radiolabelling precursor, we accessed the 18F-labelled isotopologue of the PARP inhibitor AZD2461. AZD2461 168-175 poly (ADP-ribose) polymerase family, member 1 Mus musculus 153-157 32342268-8 2020 [18F]AZD2461 was taken up in vivo in PARP1-expressing tumours, and the highest uptake was observed for PSN-1 cells (7.34 +- 1.16 %ID/g). AZD2461 5-12 poly (ADP-ribose) polymerase family, member 1 Mus musculus 37-42 32342268-8 2020 [18F]AZD2461 was taken up in vivo in PARP1-expressing tumours, and the highest uptake was observed for PSN-1 cells (7.34 +- 1.16 %ID/g). AZD2461 5-12 5'-nucleotidase, cytosolic III Mus musculus 103-108 31102368-0 2019 Novel Poly(Adenosine Diphosphate-Ribose) Polymerase (PARP) Inhibitor, AZD2461, Down-Regulates VEGF and Induces Apoptosis in Prostate Cancer Cells Background: Prostate cancer (Pca) is a heterogeneous disease, and current treatments are not based on molecular stratification. AZD2461 70-77 poly(ADP-ribose) polymerase 1 Homo sapiens 53-57 31102368-0 2019 Novel Poly(Adenosine Diphosphate-Ribose) Polymerase (PARP) Inhibitor, AZD2461, Down-Regulates VEGF and Induces Apoptosis in Prostate Cancer Cells Background: Prostate cancer (Pca) is a heterogeneous disease, and current treatments are not based on molecular stratification. AZD2461 70-77 vascular endothelial growth factor A Homo sapiens 94-98 31102368-2 2019 Therefore, this preliminary study was designed to evaluate whether PTEN expression status could have an impact on the sensitivity of invasive Pca cells to the PARP inhibitor, AZD2461. AZD2461 175-182 phosphatase and tensin homolog Homo sapiens 67-71 31102368-2 2019 Therefore, this preliminary study was designed to evaluate whether PTEN expression status could have an impact on the sensitivity of invasive Pca cells to the PARP inhibitor, AZD2461. AZD2461 175-182 poly(ADP-ribose) polymerase 1 Homo sapiens 159-163 31102368-7 2019 Treatment of cells by AZD2461 also caused a significant increase in apoptosis through caspase3 activation in both cell lines. AZD2461 22-29 caspase 3 Homo sapiens 86-94 31102368-9 2019 Conclusion: AZD2461 suppresses the growth of prostate tumor cells since AZD2461 monotherapy could prove to be efficacious, especially against cells not expressing PTEN besides activating the possible apoptosis-independent cell death pathways. AZD2461 12-19 phosphatase and tensin homolog Homo sapiens 163-167 30390553-0 2019 Synthesis and evaluation of an AZD2461 [18F]PET probe in non-human primates reveals the PARP-1 inhibitor to be non-blood-brain barrier penetrant. AZD2461 31-38 poly(ADP-ribose) polymerase 1 Homo sapiens 88-94 31423128-2 2019 This study was designed to determine the efficacy of combination therapy of a histone deacetylase inhibitor, valproic acid (VPA) and a novel PARP inhibitor AZD2461 in both PC-3 (PTEN-mutated) and DU145 (PTEN-unmutated) prostate cancer cell lines. AZD2461 156-163 collagen type XI alpha 2 chain Homo sapiens 141-145 31423128-2 2019 This study was designed to determine the efficacy of combination therapy of a histone deacetylase inhibitor, valproic acid (VPA) and a novel PARP inhibitor AZD2461 in both PC-3 (PTEN-mutated) and DU145 (PTEN-unmutated) prostate cancer cell lines. AZD2461 156-163 proprotein convertase subtilisin/kexin type 1 Homo sapiens 172-176 31423128-2 2019 This study was designed to determine the efficacy of combination therapy of a histone deacetylase inhibitor, valproic acid (VPA) and a novel PARP inhibitor AZD2461 in both PC-3 (PTEN-mutated) and DU145 (PTEN-unmutated) prostate cancer cell lines. AZD2461 156-163 phosphatase and tensin homolog Homo sapiens 178-182 31423128-7 2019 We observed a synergistic relationship between VPA and AZD2461 in all affected fractions of PC-3 cells (CI<0.9), but not in DU145 cells (CI>1.1). AZD2461 55-62 proprotein convertase subtilisin/kexin type 1 Homo sapiens 92-96 31423128-8 2019 Annexin-V staining analysis revealed a significant induction of apoptosis when PC-3 cells were treated with VPA+AZD2461 (p<0.05). AZD2461 112-119 annexin A5 Homo sapiens 0-9 31423128-8 2019 Annexin-V staining analysis revealed a significant induction of apoptosis when PC-3 cells were treated with VPA+AZD2461 (p<0.05). AZD2461 112-119 proprotein convertase subtilisin/kexin type 1 Homo sapiens 79-83 31423128-9 2019 Both mRNA and protein levels of Rad51 and Mre11 were significantly decreased in PC-3 cells co-treated with VPA+AZD2461 while enhanced H2AX phosphorylation was found in PC-3 cells after 12 and 24 hours of co-treatment (p<0.05). AZD2461 111-118 RAD51 recombinase Homo sapiens 32-37 31423128-9 2019 Both mRNA and protein levels of Rad51 and Mre11 were significantly decreased in PC-3 cells co-treated with VPA+AZD2461 while enhanced H2AX phosphorylation was found in PC-3 cells after 12 and 24 hours of co-treatment (p<0.05). AZD2461 111-118 MRE11 homolog, double strand break repair nuclease Homo sapiens 42-47 31423128-9 2019 Both mRNA and protein levels of Rad51 and Mre11 were significantly decreased in PC-3 cells co-treated with VPA+AZD2461 while enhanced H2AX phosphorylation was found in PC-3 cells after 12 and 24 hours of co-treatment (p<0.05). AZD2461 111-118 proprotein convertase subtilisin/kexin type 1 Homo sapiens 80-84 31423128-10 2019 Our findings established a preclinical rationale for selective targeting of HR repair pathways by a combination of VPA and AZD2461 as a mechanism for reducing the HR pathway sufficiency in PTEN-mutated prostate cancer cells. AZD2461 123-130 phosphatase and tensin homolog Homo sapiens 189-193 31380319-3 2019 This study wishes to assess whether the combination of AZD2461 as a newly developed PARP1 inhibitor and valproic acid (VPA), a histone deacetylase inhibitor could effectively reduce the growth of MCF-7 cells with no fundamental DNA repair defect. AZD2461 55-62 poly(ADP-ribose) polymerase 1 Homo sapiens 84-89 30390553-1 2019 Poly(ADP-ribose)polymerase-1 inhibitor (PARPi) AZD2461 was designed to be a weak P-glycoprotein (P-gp) analogue of FDA approved olaparib. AZD2461 47-54 poly(ADP-ribose) polymerase 1 Homo sapiens 0-28 30390553-1 2019 Poly(ADP-ribose)polymerase-1 inhibitor (PARPi) AZD2461 was designed to be a weak P-glycoprotein (P-gp) analogue of FDA approved olaparib. AZD2461 47-54 ATP binding cassette subfamily B member 1 Homo sapiens 81-95 30390553-1 2019 Poly(ADP-ribose)polymerase-1 inhibitor (PARPi) AZD2461 was designed to be a weak P-glycoprotein (P-gp) analogue of FDA approved olaparib. AZD2461 47-54 ATP binding cassette subfamily B member 1 Homo sapiens 97-101 30390553-2 2019 With this chemical property in mind, we utilized the AZD2461 ligand architecture to develop a CNS penetrant and PARP-1 selective imaging probe, in order to investigate PARP-1 mediated neuroinflammation and neurodegenerative diseases, such as Alzheimer"s and Parkinson"s. AZD2461 53-60 poly(ADP-ribose) polymerase 1 Homo sapiens 112-118 30390553-2 2019 With this chemical property in mind, we utilized the AZD2461 ligand architecture to develop a CNS penetrant and PARP-1 selective imaging probe, in order to investigate PARP-1 mediated neuroinflammation and neurodegenerative diseases, such as Alzheimer"s and Parkinson"s. AZD2461 53-60 poly(ADP-ribose) polymerase 1 Homo sapiens 168-174 30390553-3 2019 Our work led to the identification of several high-affinity PARPi, including AZD2461 congener 9e (PARP-1 IC50 = 3.9 +- 1.2 nM), which was further evaluated as a potential 18F-PET brain imaging probe. AZD2461 77-84 poly(ADP-ribose) polymerase 1 Homo sapiens 98-104 30357520-7 2019 RESULTS: Olaparib and AZD2461 dose-dependently reduced growth of both RH30 and RD cells by arresting growth at G2/M phase and by modulating the expression, activation and subcellular localization of specific cell cycle regulators. AZD2461 22-29 Rh blood group D antigen Homo sapiens 70-74 30357520-8 2019 Downregulation of phospho-AKT levels and accumulation of gammaH2AX, a specific marker of DNA damage, were significantly and persistently induced by Olaparib and AZD2461 exposure, this leading to apoptosis-related cell death. AZD2461 161-168 AKT serine/threonine kinase 1 Homo sapiens 26-29 30252484-0 2018 ABCB1 Attenuates the Brain Penetration of the PARP Inhibitor AZD2461. AZD2461 61-68 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 0-5 30252484-0 2018 ABCB1 Attenuates the Brain Penetration of the PARP Inhibitor AZD2461. AZD2461 61-68 poly (ADP-ribose) polymerase family, member 1 Mus musculus 46-50 30252484-4 2018 AZD2461 is a novel PARP inhibitor that is unaffected by P-gp mediated resistance in breast cancer models and thus appears to have promising characteristics for brain penetration. AZD2461 0-7 poly (ADP-ribose) polymerase family, member 1 Mus musculus 19-23 30198004-0 2018 Altering Nitrogen Heterocycles of AZD2461 Affords High Affinity Poly(ADP-ribose) Polymerase-1 Inhibitors with Decreased P-Glycoprotein Interactions. AZD2461 34-41 ATP binding cassette subfamily B member 1 Homo sapiens 120-134 30198004-2 2018 AZD2461, a congener of FDA approved olaparib, is a potent PARPi with high affinity for PARP-1 and nonsubstrate for P-glycoprotein (P-gp), an attractive characteristic for cancer therapeutics. AZD2461 0-7 poly(ADP-ribose) polymerase 1 Homo sapiens 87-93 30198004-2 2018 AZD2461, a congener of FDA approved olaparib, is a potent PARPi with high affinity for PARP-1 and nonsubstrate for P-glycoprotein (P-gp), an attractive characteristic for cancer therapeutics. AZD2461 0-7 ATP binding cassette subfamily B member 1 Homo sapiens 115-129 30198004-2 2018 AZD2461, a congener of FDA approved olaparib, is a potent PARPi with high affinity for PARP-1 and nonsubstrate for P-glycoprotein (P-gp), an attractive characteristic for cancer therapeutics. AZD2461 0-7 ATP binding cassette subfamily B member 1 Homo sapiens 131-135 30198004-3 2018 Analogues of AZD2461 were synthesized and profiled in BRCA1 functional and nonfunctional cell lines, revealing compounds (2, 3, and 5) of low cytotoxicity and excellent PARP-1 affinities (~4-8 nM). AZD2461 13-20 BRCA1 DNA repair associated Homo sapiens 54-59 30198004-3 2018 Analogues of AZD2461 were synthesized and profiled in BRCA1 functional and nonfunctional cell lines, revealing compounds (2, 3, and 5) of low cytotoxicity and excellent PARP-1 affinities (~4-8 nM). AZD2461 13-20 poly(ADP-ribose) polymerase 1 Homo sapiens 169-175