Search Results - "Gill, Sonja J"
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Combinations of PARP Inhibitors with Temozolomide Drive PARP1 Trapping and Apoptosis in Ewing's Sarcoma
Published in PloS one (27-10-2015)“…Ewing's sarcoma is a malignant pediatric bone tumor with a poor prognosis for patients with metastatic or recurrent disease. Ewing's sarcoma cells are acutely…”
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Preclinical Characterization of AZD5305, A Next-Generation, Highly Selective PARP1 Inhibitor and Trapper
Published in Clinical cancer research (01-11-2022)“…We hypothesized that inhibition and trapping of PARP1 alone would be sufficient to achieve antitumor activity. In particular, we aimed to achieve selectivity…”
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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}- N -methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs
Published in Journal of medicinal chemistry (14-10-2021)“…Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA…”
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Radiopotentiation Profiling of Multiple Inhibitors of the DNA Damage Response for Early Clinical Development
Published in Molecular cancer therapeutics (01-09-2021)“…Radiotherapy is an effective anticancer treatment, but combinations with targeted agents that maximize efficacy while sparing normal tissue are needed. Here,…”
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Preclinical Characterization of AZD9574, a Blood-Brain Barrier Penetrant Inhibitor of PARP1
Published in Clinical cancer research (01-04-2024)“…We evaluated the properties and activity of AZD9574, a blood-brain barrier (BBB) penetrant selective inhibitor of PARP1, and assessed its efficacy and safety…”
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Abstract 1374: The novel PARP1-selective inhibitor AZD5305 has reduced hematological toxicity when compared to PARP1/2 inhibitors in pre-clinical models
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Current clinical poly (ADP-ribose) polymerase (PARP) inhibitors target both PARP1 and PARP2 and they all cause clinical cytopenias with varying severity…”
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Abstract 296: Structure-based and property-based drug design of AZD5305, a highly selective PARP1 inhibitor and trapper
Published in Cancer research (Chicago, Ill.) (01-07-2021)“…Since the approval of olaparib in 2014 for BRCA mutated (BRCAm) ovarian cancer, many PARP inhibitors have been developed and have seen widespread success…”
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Discovery of 5‑{4-[(7-Ethyl-6-oxo‑5,6-dihydro‑1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}‑N‑methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs
Published in Journal of medicinal chemistry (14-10-2021)“…Poly-ADP-ribose-polymerase (PARP) inhibitors have achieved regulatory approval in oncology for homologous recombination repair deficient tumors including BRCA…”
Get full text
Journal Article