Results 141 to 150 of about 6,510 (175)

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

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

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

Cancer Research, 2023
Abstract 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. Currently, it lacks effective therapies to prevent and treat OC, which warrants novel
Ganesh Acharya, Chinnadurai Mani, Mark B. Reedy, Komaraiah Palle   +3 more
openaire   +1 more source

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 2745: Pharmacological characterisation of cell active inhibitors of Poly(ADP-ribose) glycohydrolase (PARG)

Cancer Research, 2014
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. Total PARG deficiency leads to cell death whilst PARG depletion, using RNAi, leads to pleiotropic effects such as PAR chain ...
Dominic James, Allan Jordan, Nicola Hamilton, Alison McGonagle, Kate Smith, Alexandra Stowell, Ian Waddell, Bohdan Waszkowycz, Donald Ogilvie   +8 more
openaire   +1 more source

Abstract 7112: Preclinical profile of novel and potent small molecule inhibitors of PARG

Cancer Research
Abstract Poly(ADP-ribose) glycohydrolase (PARG) is primary enzyme involved in the dePARylation process of DNA repair, specifically in the single strand break repair (SSBRs). PARG is a macrodomain protein with exo- and endo-glycohydrolase activity that liberates free ADP-ribose and PAR chains, respectively.
Sukanya Patra, Manoj Pothuganti, Githavani Kummari, Venu Sankeshi, Jyothipriya Kapaka, Navnath Karche, Ramamohan Mekala, Srikant Viswanadha   +7 more
openaire   +1 more source

Abstract 3714: Optimisation of quinazolinedione sulphonamides as novel inhibitors of poly(ADP Ribose) glycohydrolase (PARG)

Cancer Research, 2016
Abstract The macrodomain protein poly(ADP ribose) glycohydrolase (PARG) has been shown to be a critical component in the repair of single stand DNA breaks and counteracts the function of the ARTD family of poly(ADP ribose) polymerases, commonly known as the PARPs.
Kate Smith, Ben Acton, Dominic James, Cliff Jones, Stuart Jones, Allan Jordan, Nicola Hamilton, Alison McGonagle, Daniel Mould, Helen Small, Alex Stowell, Julie Tucker, Ian Waddell, Bohdan Waszkowycz, Donald Ogilvie   +14 more
openaire   +1 more source

Abstract 6972: Discovery of XNW29016, a PARG inhibitor for HRD cancer therapy

Cancer Research
Abstract DNA damage repair enzymes are promising targets as genomic instability and DNA repair defects are important characteristics of cancer cells PARylation catalysed by PARP1/2 is a kind of reversible protein modification, which has central functions in maintaining genome stability.
Yonghan Hu, Haiyang Wei, Dawei Wan, Ben Ma, Jiajing Xu, Shihua Wang, Liang Kong, Zhe Zhang, Yuanbao Li, Zhenwei Wu, Yuzhen Hou, Wengui Wang, Xiaojun Liu, Meijie Le, Jing Qiang   +14 more
openaire   +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.
Karson S, Putt, Paul J, Hergenrother
openaire   +2 more sources

Abstract 3715: Benzimidazolone sulphonamides - potent, selective and drug-like inhibitors of poly(ADP Ribose) Glycohydrolase (PARG)

Cancer Research, 2016
Abstract In recent years, many proteins involved in DNA repair, such as ATR, ATM and PARP, have received considerable attention as potential points of therapeutic intervention in cancer. Indeed, these efforts have recently delivered several agents into clinical evaluation or FDA regulatory approval.
Allan Jordan, Ben Acton, Nicola Hamilton, James Hitchin, Colin Hutton, Dominic James, Cliff Jones, Stuart Jones, Alison McGonagle, Helen Small, Kate Smith, Alex Stowell, Julie Tucker, Ian Waddell, Bohdan Waszkowycz, Donald Ogilvie   +15 more
openaire   +1 more source