Results 151 to 160 of about 6,510 (175)

Abstract 5515: In vivo efficacy of the PARG inhibitor Gallotannin against triple negative breast cancer.

Cancer Research, 2013
Abstract Breast cancer patients whose tumors fall into the triple negative category have the poorest clinical outcomes. These patients are at high risk for metastatic recurrence and have poor overall survival. Clearly, new therapeutic strategies are needed to combat triple negative tumors both at the time of onset and if necessary, at ...
Tiejun Zhao, Qiang Sun, Amanda Lovato, Sonia del Rincon, Michael Witcher   +4 more
openaire   +1 more source

2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG

2016
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions ...
Mcgonagle, Alison, Jordan,, Allan, Waszkowycz,, Bohdan, Hutton,, Colin, Waddell,, Ian, Hitchin, James, Smith, Kate, Hamilton, Niall   +7 more
openaire   +1 more source

Abstract NT-117: INHIBITION OF PARG, SENSITIZES OVARIAN CANCER CELLS TO PARP INHIBITORS AND DNA DAMAGING AGENTS

Clinical Cancer Research, 2019
Abstract BACKGROUND: Poly(ADP-ribose) glycohydrolase (PARG) is responsible poly(ADP-ribose) (PAR) catabolism, which is synthesized by poly(ADP-ribose) polymerases (PARPs) at the site of DNA single-strand breaks (SSB). Faulty PAR formation or disintegration inhibits SSB repair.
Emad Matanes, Tahira Baloch, David Octeau, Roy Kessous, Liron Kogan, Ido Laskov, Walter Gotlieb, Amber Yasmeen   +7 more
openaire   +1 more source

Abstract C39: First-in-class inhibitors of the putatively undruggable DNA repair target Poly(ADP-ribose) glycohydrolase (PARG)

Molecular Cancer Therapeutics, 2015
Abstract Poly(ADP-ribose) glycohydrolase (PARG) is the only enzyme known to catalyse hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, thereby reversing the effects of poly(ADP-ribose) polymerases (PARPs). PARG depletion, using RNAi, results in several effects such as PAR chain persistence, progression of single- to double ...
Bohdan Waszkowycz, Dominic James, Ben Acton, Emma Fairweather, Sam Fritzl, Niall Hamilton, Nicola Hamilton, Sarah Holt, James Hitchen, Colin Hutton, Stuart Jones, Allan Jordan, Alison McGonagle, Daniel Mould, Helen Small, Kate Smith, Alexandra Stowell, Ian D. Waddell, Donald Ogilvie   +18 more
openaire   +1 more source

Pharmacological characterisation of novel, cell active, inhibitors of Poly(ADP-ribose glycohydrolase (PARG)

2014
Poly(ADP-ribose) glycohydrolase (PARG) is the only enzyme known to catalyse hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, thereby reversing the effects of poly(ADP-ribose) polymerases. Total PARG deficiency leads to cell death whilst PARG depletion, using RNAi, leads to pleiotropic effects such as PAR chain persistence, progression of
Waddell, Ian, James, Dominic, Jordan, Allan, Hamilton, Nicola, McGonagle, Alison, Smith, Kate, Stowell, Alexandra, Waszkowycz, Bohdan, Ogilvie, Donald   +8 more
openaire   +1 more source

“PARG Inhibitors’ Success: A Long Way to Go!”

Current Enzyme Inhibition, 2015
Anuradha Pandey, Pooja Makhija, Prakash G.Chandak, Anil Bhanudas Gaikwad   +3 more
openaire   +1 more source

Abstract 7148: Small molecule inhibitor of FEN1 nuclease utilizing a novel metal-binding pharmacophore synergizes with inhibitors of USP1, PARP, PARG and ATR

Cancer Research
Abstract Flap endonuclease 1 (FEN1) is a structure-specific metallonuclease that cleaves 5’ DNA flaps during replication and repair. FEN1 is an attractive target for development of anticancer therapeutics because it is overexpressed in many tumor types and has a large number of synthetic lethality partners including genes in Homologous ...
Jason Munguia, Sanjay Agarwalla, Elaine Guo, Dave Martin, Junhua Fan, Dave Lonergan, David Puerta, Zachary Zimmerman, Konstantin Taganov   +8 more
openaire   +1 more source

Inhibition of PARG sensitizes ovarian cancer cells to PARP inhibitors and DNA damaging agents

Gynecologic Oncology, 2020
E. Matanes, L. Kogan, V. López-Ozuna, C. Mitric, O. Raban, N. Eisenberg, T. Baloch, S. Salvador, S. Lau, W.H. Gotlieb, A. Yasmeen   +10 more
openaire   +1 more source

Abstract B022: FORX-428: A best-in class PARG inhibitor with promising anti-tumor activity in preclinical cancer models

Molecular Cancer Therapeutics
Abstract The formation of poly (ADP-ribose) (PAR) chains from NAD+ catalyzed by PARP enzymes is a pivotal posttranslational modification at sites of DNA lesions or stalled replication forks and serves as a scaffold to recruit DNA repair proteins.
Frank Tadashi. Zenke, Ulrich Lücking, Olivier Querolle, Andreas Goutopoulos, Luca Iacovino, Marta Malattia, Alessandro Potenza, Nicolas Bocquet, Alena Freudenmann, Serena Bologna, Vasilis Dionellis, Giacomo Rossetti, Marina Gysin, Hanna Kok, Roxanne Lourman, Jason Clochard, Anika Kuster, Irena Konstantinova, Sotirios Sotiriou, Thanos Halazonetis, Jens Würthner, Tarig Bashir   +21 more
openaire   +1 more source

PARG inhibition limits HCC progression and potentiates the efficacy of immune checkpoint therapy

Journal of Hepatology, 2022
Zheng Chen, Qiang Zhou, Shuang Liu
exaly