Results 101 to 110 of about 3,357,233 (168)

PARG Inhibitors and Functional PARG Inhibition Models

Current Protein & Peptide Science, 2016
Poly(ADP-ribose) polymerases (PARPs) family proteins catalyze poly(ADP-ribosylation) (PARylation) by conjugating ADP-ribose residues repeatedly on amino acid residues using nicotinamide adenine dinucleotide as a substrate. The inhibitors of PARP widely block DNA repair processes and are currently examined in clinical trials of cancer therapy.
Yuka, Sasaki, Miyuki, Hozumi, Hiroaki, Fujimori, Yasufumi, Murakami, Fumiaki, Koizumi, Kengo, Inoue, Mitsuko, Masutani   +6 more
openaire   +2 more sources

Abstract 2667: PARG inhibition augments CHK1 inhibitor-induced replication stress and synergistically kills ovarian cancer cells

Cancer Research, 2023
Ovarian cancer (OC) is one of the leading causes of cancer-related deaths in women in the United States. PARP inhibitors showed promising clinical responses; however, most of the patients eventually relapse and succumb to the resistant disease ...
Ganesh Acharya, Chinnadurai Mani, Mark Reedy, Komaraiah Palle   +3 more
semanticscholar   +1 more source

Abstract LB_A19: Genome-wide CRISPR/Cas9 screens for the identification of targeted vulnerabilties in PARP inhibitor-resistant PARG;BRCA2-deficient tumor cells: A focus on EXO1/FEN1-mediated DNA repair

Molecular Cancer Therapeutics, 2023
Targeting poly(ADP-ribose) glycohydrolase (PARG) is currently explored as a therapeutic approach to treat various cancer types, but we have a poor understanding of the specific genetic vulnerabilities that would make cancer cells susceptible to such a ...
Christina Andronikou, Kamila Burdova, Diego Dibitetto, C. Lieftink, R. Beijersbergen, Hana Hanzlikova, Jos Jonkers, S. Rottenberg   +7 more
semanticscholar   +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
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.
F. Zenke, Ulrich Lücking, Olivier Querolle, Andreas Goutopoulos, L. Iacovino, Marta Malattia, Alessandro Potenza, Nicolas Bocquet, Alena Freudenmann, Serena Bologna, V. Dionellis, Giacomo G. Rossetti, Marina Gysin, Hanna Kok, Roxanne Lourman, Jason Clochard, Anika Kuster, Irena Konstantinova, Sotirios Sotiriou, Thanos Halazonetis, J. Würthner, Tarig Bashir   +21 more
semanticscholar   +1 more source

Abstract B005: Regulation of replication-induced PARP1/PARP2 activation by base excision repair: Implications for PARP and PARG inhibitor resistance

Molecular Cancer Therapeutics
Acquired poly (ADP-ribose) polymerases (PARP)-inhibitor (PARPi) and/or poly (ADP-ribose) glycohydrolase (PARG)-inhibitor (PARGi) resistance in BRCA1/2-defective tumors is common, emphasizing the need for identifying new targets.
Md Ibrahim, Md Maruf Khan, Wynand P. Roos, Rasha Q. Al-Rahaleh, Faisal Hayat, M. Migaud, R. Sobol   +6 more
semanticscholar   +1 more source

Abstract 2083: Discovery of ETX-19477, a novel and selective PARG inhibitor with high potency against tumors with underlying replication stress

Cancer Research
DNA damage response (DDR) is an important cellular process that is regulated by poly ADP ribosylation (PARylation). PARP1 binds to DNA break sites and then catalyzes PARylation, which leads to recruitment of repair factors and initiation of base ...
J. Holleran, Tamara S. Rodems, Shweta Sharma, A. Santini, Cindy Wuerz, Juping Liu, L. Tian, Joseph Dosch, J. Nader, Richard Rivera, Shyama Herath, Joseph Marakovits, Christopher McBride, R. Stansfield, Amy Salyards, James M. Veal, Jeffrey A. Stafford, Gretchen Bain   +17 more
semanticscholar   +1 more source

Abstract 3366: FoRx-06-428 is a novel PARG inhibitor with potent anti-tumor efficacy in preclinical cancer models

Cancer Research
The formation of poly(ADP-ribose) (PAR) chains from NAD+ precursors by PARP enzymes is a characteristic posttranslational modification during DNA damage repair.
Olivier Querolle, Ulrich Lücking, L. Iacovino, Alena Freudenmann, Giacomo G. Rossetti, Marina Gysin, Serena Bologna, V. Dionellis, Marta Malattia, Alessandro Potenza, Nicolas Bocquet, Irena Konstantinova, Andreas Goutopoulos, Sotirios Sotiriou, Thanos Halazonetis, Tarig Bashir, Frank Zenke   +16 more
semanticscholar   +1 more source

Abstract 7114: Exploring the landscape of PARP and PARG inhibitor selectivity in live cells using NanoBRET™ target engagement assays

Cancer Research
The 17-member poly(ADP-ribose) polymerase (PARP) family of proteins mediate a number of cellular processes including gene transcription, cell-division and DNA-repair.
Ani Michaud, Kelly Teske, Jennifer Wilkinson, C. Zimprich, James D. Vasta, Cesear R. Corona, Min Zhou, Elizabeth R Dominguez, Kaitlin Dunn-Hoffman, M. Robers   +9 more
semanticscholar   +1 more source

Abstract 3909: PARG inhibitor sensitivity is correlated with accumulation of single strand DNA gaps in preclinical models of ovarian cancer

Cancer Research
Poly (ADP-ribose) glycohydrolase (PARG) is a dePARylating enzyme which promotes DNA repair in conjunction with PARP1 by removal of poly (ADP-ribose) (PAR).
Ramya Ravindranathan, O. Somuncu, Yuqing Jiao, A. A. D. Da Costa, Benjamin P Lamarre, David B Martignetti, G. Zambrano, S. Mukkavalli, Joyce F. Liu, B. Kochupurakkal, J. Lazaro, K. Parmar, G. Shapiro, Alan D. D'Andrea   +13 more
semanticscholar   +1 more source

Abstract 4533: Identification of DAT-2000A, a novel potent PARG inhibitor that selectively inhibits PARPi-resistant and homologous-recombination-deficient tumors

Cancer Research
A significant portion of patients with homologous recombination repair deficiencies(HRD) do not respond to PARP inhibitors, and even among those who initially respond, resistance often develops after PARP inhibitor treatment. This underscores the unmet
Dan Yan, Yan Zhang, Zhangqi Yu, Yao Zhang, Jingxi Zhang, Bin Wang, Huixian Chen, Jingxue Shi, Zhiwei Bao, Xiaoling Lin, Jincong Zhuo, Kevin Zhou   +11 more
semanticscholar   +1 more source