Results 1 to 10 of about 6,396 (123)

Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death [PDF]

Nature Communications, 2019
PARG catalyzes the removal of poly(ADP-ribose) (PAR) from target proteins and executes critical functions in the DNA damage response. Here the authors provide structural and biological insight with small molecule PARG inhibitors and show that PARG ...
Jerry H. Houl, Zu Ye, Chris A. Brosey, Lakshitha P. F. Balapiti-Modarage, Sarita Namjoshi, Albino Bacolla, Daniel Laverty, Brian L. Walker, Yasin Pourfarjam, Leslie S. Warden, Naga Babu Chinnam, Davide Moiani, Roderick A. Stegeman, Mei-Kuang Chen, Mien-Chie Hung, Zachary D. Nagel, Tom Ellenberger, In-Kwon Kim, Darin E. Jones, Zamal Ahmed, John A. Tainer   +20 more
doaj   +4 more sources

Loss‐of‐function genetic screen unveils synergistic efficacy of PARG inhibition with combined 5‐fluorouracil and irinotecan treatment in colorectal cancer [PDF]

Clinical and Translational Medicine
Background Colorectal cancer (CRC) remains a major global health concern, partly due to resistance to therapy and the lack of new effective treatments for advanced disease.
Cristina Queralt, Cristina Moreta‐Moraleda, Marta Costa, Ferran Grau‐Leal, Jeannine Diesch, Carla Vendrell‐Ayats, Eva Musulén, Roni H G Wright, Cristina Bugés, José Luis Manzano, Sara Cabrero‐de las Heras, Johannes Zuber, Marcus Buschbeck, Sonia‐V Forcales, Eva Martínez‐Balibrea   +14 more
doaj   +3 more sources

Synergistic Cellular Toxicity from Inhibition of Poly(ADP-ribose) Glycohydrolase (PARG) and Ubiquitin-Specific Protease 1 (USP1) [PDF]

Toxics
Ubiquitin-specific protease 1 (USP1) is an emerging target for poly(ADP-ribose) polymerase 1 (PARP1) inhibitor-resistant and BRCA1/BRCA2 mutant tumors.
Stefan M. Leonard, Charlotte R. Pearson, Wynand P. Roos, Robert W. Sobol   +3 more
doaj   +2 more sources

PARG inhibition suppresses breast cancer progression and potentiates immunoresponse through MTDH degradation mediated by E3 ligase ITCH-dependent ubiquitination [PDF]

npj Breast Cancer
PARG plays an important role in cancer progression and immunoresponse, but its role in breast cancer is not yet fully elucidated. The advanced breast cancer is still a persistent challenge in clinical oncology.
Junnai Wang, Yanhua Dong, Weiwei Lun, Manman Nai, Yajing Shi, Jianfang Geng, Wenhui Cai, Jiaxi Liu, Hongyu Li, Lei Li   +9 more
doaj   +2 more sources

Suppression of ADP-ribosylation reversal triggers cell vulnerability to alkylating agents [PDF]

Neoplasia: An International Journal for Oncology Research
The ADP-ribosyl hydrolases PARG and ARH3 counteract PARP enzymatic activity by removing ADP-ribosylation. PARG and ARH3 activities have a synthetic lethal effect; however, the specific molecular mechanisms underlying this response remain unknown.
Rocco Caggiano, Evgeniia Prokhorova, Lena Duma, Kira Schützenhofer, Raffaella Lauro, Giuliana Catara, Rosa Marina Melillo, Angela Celetti, Rebecca Smith, S John Weroha, Scott H Kaufmann, Ivan Ahel, Luca Palazzo   +12 more
doaj   +2 more sources

Genomic and biological aspects of resistance to selective poly(ADP‐ribose) glycohydrolase inhibitor PDD00017273 in human colorectal cancer cells

Cancer Reports, 2023
Background Poly(ADP‐ribose) glycohydrolase (PARG) is a key enzyme in poly(ADP‐ribose) (PAR) metabolism and a potential anticancer target. Many drug candidates have been developed to inhibit its enzymatic activity.
Kaede Tsuda, Chinatsu Kurasaka, Yoko Ogino, Akira Sato   +3 more
doaj   +1 more source

Inhibition of Poly ADP-Ribose Glycohydrolase Sensitizes Ovarian Cancer Cells to Poly ADP-Ribose Polymerase Inhibitors and Platinum Agents

Frontiers in Oncology, 2021
BackgroundPoly ADP-ribose glycohydrolase (PARG) is responsible for the catabolism of PARP-synthesized PAR to free ADP-ribose. Inhibition of PARG leads to DNA repair interruption and consequently induces cell death.
Emad Matanes, Emad Matanes, Vanessa M. López-Ozuna, David Octeau, Tahira Baloch, Florentin Racovitan, Amandeep Kaur Dhillon, Roy Kessous, Roy Kessous, Oded Raban, Oded Raban, Liron Kogan, Liron Kogan, Shannon Salvador, Shannon Salvador, Susie Lau, Susie Lau, Walter H. Gotlieb, Walter H. Gotlieb, Amber Yasmeen   +19 more
doaj   +1 more source

Crystallographic and biochemical analysis of the mouse poly(ADP-ribose) glycohydrolase. [PDF]

PLoS ONE, 2014
Protein poly(ADP-ribosyl)ation (PARylation) regulates a number of important cellular processes. Poly(ADP-ribose) glycohydrolase (PARG) is the primary enzyme responsible for hydrolyzing the poly(ADP-ribose) (PAR) polymer in vivo.
Zhizhi Wang, Jean-Philippe Gagné, Guy G Poirier, Wenqing Xu   +3 more
doaj   +1 more source

Host Cell Poly(ADP-ribose) glycohydrolase Is Crucial for Trypanosoma cruzi Infection Cycle [PDF]

, 2013
Trypanosoma cruzi, etiological agent of Chagas´ disease, has a complex life cycle which involves the invasion of mammalian host cells, differentiation and intracellular replication.
Alonso, Guillermo Daniel, Fernandez Villamil, Silvia Hebe, Flawia, Mirtha Maria, Kevorkian, María Laura, Schlesinger, Mariana, Vilchez Larrea, Salomé Catalina   +5 more
core   +14 more sources

Poly(ADP-ribosyl)ation is involved in the epigenetic control of TET1 gene transcription [PDF]

, 2014
TET enzymes are the epigenetic factors involved in the formation of the Sixth DNA base 5-hydroxymethylcytosine, whose deregulation has been associated with tumorigenesis.
Bacalini, MARIA GIULIA, Caiafa, Paola, Calabrese, Roberta, Ciccarone, Fabio, Franceschi, C, Guastafierro, Tiziana, Mariano, Germano, Reale, Anna, Valentini, Elisabetta, Zampieri, Michele   +9 more
core   +9 more sources