[PDF] Top 20 A decade of clinical development of PARP inhibitors in perspective.
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A decade of clinical development of PARP inhibitors in perspective.
... with PARP inhibitors are summarized; (A) combinations of PARPi with other compounds targeting alternatives DDR nodes aim to maximize accumulation DNA damage during G1 and S phases of the cell cycle, ... See full document
11
Novel treatment strategies in triple-negative breast cancer: specific role of poly(adenosine diphosphate-ribose) polymerase inhibition
... Abstract: Inhibitors of the poly(adenosine triphosphate-ribose) polymerase (PARP)-1 enzyme induce synthetic lethality in cancers with ineffective DNA (DNA) repair or homologous repair deficiency, and have ... See full document
10
NF- B signaling mediates acquired resistance after PARP inhibition
... BRCA1. PARP inhibitor-resistant clones (R10 and R100 in ...of PARP inhibitor (Olaparib AZD2281, KU-0059436) (10nM, 100nM and 500nM, ...generate PARP inhibitor- resistant lines, we have used olaparib ... See full document
15
PARP inhibitors: Synthetic lethality in the clinic.
... and development of the PARPi/BRCA SL ...the development of biomarkers and an understanding of drug resistance ...pre- clinical approaches to identify mechanisms of drug resistance alongside early ... See full document
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Advances in using PARP inhibitors to treat cancer
... a PARP inhibitor to a topoisomerase I poison has been demonstrated in tumor biopsies and circulating tumor cells by measurement of gH2AX foci, a marker of DNA double strand breaks, in patients trea- ted with ... See full document
5
<div>Emerging treatment options for ovarian cancer: focus on rucaparib</div>
... (PARP) inhibitors (PARPi) are an exciting class of anticancer drugs, which have revolutionized the management of BRCA mutant/homologous recombination-deficient recurrent high-grade serous ovarian cancer ... See full document
12
Update on Poly ADP ribose polymerase inhibition for ovarian cancer treatment
... catalytic inhibitors blocking repair of DNA SSBs by the BER/ SSBR pathway ...initial clinical development of PARPi focused on their role as chemo-sensitizers, and their single-agent activity was ... See full document
18
Advances and perspectives of PARP inhibitors
... the clinical trial NCT02000622, Olaparib tablet was approved by FDA for the treatment of human epidermal growth factor receptor-2 (Her-2) negative, metastatic breast cancer patients who had been treated with ... See full document
12
An update on PARP inhibitors for the treatment of cancer
... The development of poly (adenosine diphosphate [ADP]) ribose polymerase (PARP) inhibitors (PARPi) has progressed greatly over the last few years and has shown encouraging results in the BRCA1/2 ... See full document
10
Beyond DNA repair: the novel immunological potential of PARP inhibitors.
... Drug Development Department (DITEP), SPV is principal investigator or sub-investigator of clinical trials from Abbvie, Agios Pharmaceuticals, Amgen, Argen-X Bvba, Arno Therapeutics, Astex Pharmaceuticals, ... See full document
5
Targeting DNA Repair in Cancer: Beyond PARP Inhibitors.
... ADP-ribosylation inhibitors are already in clinical development/use, given the essential role of ubiquitylation and de- ubiquitylation in the DDR, modulating DNA repair through the use of specific ... See full document
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The evolving landscape of predictive biomarkers of response to PARP inhibitors
... polymerase inhibitors (PARPis) are DNA-damaging agents that trap PARP-DNA complexes and interfere with DNA ...of PARP-1 confers high resistance to PARPis, it has not been established whether or not ... See full document
5
A clinical perspective on the role of chronic inflammation in gastrointestinal cancer
... There is accumulating evidence for the involvement of chronic inflammation in the carcinogenesis of most GI malignancies, and the underlying cellular and molecular processes are increasingly understood. Chronic inflamma- ... See full document
12
Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP
... JNJ-26854165, a novel tryptamine derivative, is an oral MDM2 inhibitor. Pre-clinical studies have shown bind- ing of JNJ-26854165 to RING domain of MDM2 inhibits the interaction of MDM2-p53 complex to the protea- ... See full document
14
Clinical development of 1% azithromycin in DuraSite<sup>®</sup>, a topical azalide anti-infective for ocular surface therapy
... 3 clinical trial for bacterial ...trial. Clinical and bacteriologic con- fi rmation of infection was obtained for the worst affected eye at study entry and ... See full document
8
<p>Cardiac toxicity of immune-checkpoint inhibitors: a clinical case of nivolumab-induced myocarditis and review of the evidence and new challenges</p>
... Nivolumab, a fully human immunoglobulin (Ig) G4 monoclonal antibody direc- ted against cell surface receptor PD1, has been approved for the treatment of patients with advanced renal cell carcinoma previously treated with ... See full document
8
Cumulative clinical experience from over a decade of use of levofloxacin in community-acquired pneumonia: critical appraisal and role in therapy
... results demonstrated that fAUC:MIC ratios of #82 and #86 for levofloxacin were associated with a first-step parC muta- tion and second-step gyrA mutation in S. pneumoniae. These resistance breakpoints for levofloxacin ... See full document
10
Resistance relationships between platinum and parp inhibitors in ovarian cancer
... Gene expression was compared between:• Relatively Olaparib Sensitive A2780, CAOV3, ES-2, HOC-1 • Relatively Olaparib Resistant HEY, IGROV-1, OVCAR420 OVCAR432 • When comparing the relati[r] ... See full document
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A perspective on the development of Genetics in Spain during the XX Century
... Madrid soon became a small Mecca for anybody with an interest in developmental genetics and García-Bellido began to exert a global influence by creating a framework which later was going to become central to the ... See full document
14
A Decade of Development of Ethylidenethiosemicarbazides as Building Blocks for Synthesis of Azoles and Azines (A Review)
... survey, we represent three approaches about ethylidenethiosemicarbazides, with different aryl or heterocyclic moieties, including synthesis, reactivity, and their biological activities..[r] ... See full document
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