Results 111 to 120 of about 3,357,233 (168)

Abstract 7095: QLS1403, a novel and potent PARG inhibitor with robust anti-tumor efficacy in homologous recombination deficient cancer models

Cancer Research
Cancer cells experience high levels of endogenous replication stress due to persistent proliferative signaling. Poly (ADP-ribose) polymerase (PARP) is a first responder to DNA damage, catalyzing the synthesis of poly (ADP-ribose) (PAR) chains that ...
Tingting Xia, Wei-Zen Wei, X. Lv, Jianfei Wang, Shengnan Zhang, Jun Chen, Xianyun Huang, Guozhi Liang, Lan Zhang, Ling Li, Ping Chen, Dong Yang, Fan Chen, Guqin Shi, Jiahua Chu, Dongdong Wu, Weimei Sun, Liang Xie, W. Qian, Daqing Sun, Weikang Tao   +20 more
semanticscholar   +1 more source

Abstract CT288: First-in-human study of oral PARG inhibitor SYN608 in advanced solid tumors

Cancer Research
SYN608 is a novel, selective, orally bioavailable poly(ADP-ribose) glycohydrolase (PARG) inhibitor. PARG plays a critical role in the DNA damage response by reversing protein PARylation and maintaining dynamic balance with PARP activity. Inhibition
Jin Li, Xiaohua Wu, Qi Dang, Ke Wang, Zhengbo Song, Jun Zhou, Yuji Zhang, Jian Zhang, Jiajia Li, W. Shen, Shengjie Yang, Hongli Li, Lu Sun, Liyan Zhou, Jianan Jin, Duo Wu, Yue Xie, Xuzhen Tang, Chao Kan, Song Shi, Hu He, Song Liu, Xiaochun Yu   +22 more
semanticscholar   +1 more source

First-in-human phase 1/2 study of ETX-19477, an oral, potent, and selective PARG inhibitor, in patients with advanced solid tumors (ERADIC8).

Journal of Clinical Oncology
3109 Background: Poly(ADP-ribose) glycohydrolase (PARG) is an enzyme that catalyzes the removal of poly-ADP-ribose (PAR) chains from proteins during DNA damage repair.
Ezra Y. Rosen, P. Advani, Kalyan Banda, F. Batalini, M. Cecchini, N. Chan, W. McKean, A. Spira, S. Yadav, T.A. Yap, Kevin K. Zarrabi, Sanjay K. Trehan, Daniel McCormick, Gretchen Bain, J. Holleran, R. Stansfield, A. Santini, James M. Veal, Jeffrey A. Stafford, R. Penson   +19 more
semanticscholar   +1 more source

A nonradiometric, high-throughput assay for poly(ADP-ribose) glycohydrolase (PARG): application to inhibitor identification and evaluation

Analytical Biochemistry, 2004
The enzyme poly(ADP-ribose) glycohydrolase (PARG) catalyzes the hydrolysis of glycosidic bonds of ADP-ribose polymers, producing monomeric ADP-ribose units. Thus, in conjunction with poly(ADP-ribose) polymerase (PARP), PARG activity regulates the extent of in vivo poly(ADP-ribosyl)ation.
Paul J Hergenrother, Karson Putt
exaly   +3 more sources

Targeting PARG reduces M2 polarization critical for PARP inhibitor resistance in ovarian cancer

Gynecologic Oncology
R. M. Borrero, Antons Martincuks, Hua Yu, Lorna Rodriguez-Rodriguez   +3 more
semanticscholar   +2 more sources

Cell-Based Screening for New PARP Inhibitors Utilizing PARG-Mutated Mouse Embryonic Stem Cells

2022
According to the most recent data, cancer is among the leading cause of death in the United States and accounted for more than 600,000 deaths in 2021. Around 30% of these cancer-related deaths were caused by breast, prostate, and ovarian cancers. PARP-1 inhibitors show the most promising results in treatment of these three types of cancers and have ...
Yaroslava, Karpova, Danping, Guo, Alexei V, Tulin   +2 more
openaire   +2 more sources

Design and synthesis of phenolic hydrazide hydrazones as potent poly(ADP-ribose) glycohydrolase (PARG) inhibitors

Bioorganic & Medicinal Chemistry Letters, 2014
Poly(ADP-ribose) polymerase (PARP) and poly(ADP-ribose) glycohydrolase (PARG) are enzymes responsible for catalyzing the formation and degradation of poly(ADP-ribose) (PAR) polymers, respectively. Activation of PARP has been shown to be involved in cell death induced by genotoxic stimuli.
Rafiqul, Islam, Fumiaki, Koizumi, Yasuo, Kodera, Kengo, Inoue, Tadashi, Okawara, Mitsuko, Masutani   +5 more
openaire   +2 more sources

Abstract 245: Expanding the therapeutic window of PARP inhibitors by co-administering PARG inhibitors.

Cancer Research
Abstract Background: Homologous recombination (HR) deficiency sensitizes tumors to PARP inhibitors (PARPi), which are standard-of-care for HR-deficient cancers. Despite their efficacy, clinical use of PARPi is limited by on-target toxicity, particularly anemia, leading to dose reductions and ...
Giacomo G. Rossetti, Michalis Petropoulos, Theodoros Rampias, Thanos D. Halazonetis   +3 more
openaire   +1 more source

Abstract 4263: QX-001352 is a novel and specific inhibitor of PARG with potentially BIC in vitro and in vivo anti-tumor efficacy

Cancer Research
When DNA is damaged one of the critical steps is the addition of Poly-ADP-ribose (PAR) chains to target proteins. Poly ADP-ribose polymerase 1 (PARP1) is an enzyme that adds PAR chains to target DNA repair proteins including itself.
Dafydd H Thomas, Xianhai Huang, Vijay Reddy, Wayne Tang   +3 more
semanticscholar   +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
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 ...
Jason Munguia, Sanjay Agarwalla, E. Guo, Dave Martin, Junhua Fan, Dave Lonergan, David Puerta, Z. Zimmerman, Konstantin Taganov   +8 more
semanticscholar   +1 more source