Results 1 to 10 of about 5,177 (98)

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

Nat Commun, 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 ...
Houl JH, Ye Z, Brosey CA, Balapiti-Modarage LPF, Namjoshi S, Bacolla A, Laverty D, Walker BL, Pourfarjam Y, Warden LS, Babu Chinnam N, Moiani D, Stegeman RA, Chen MK, Hung MC, Nagel ZD, Ellenberger T, Kim IK, Jones DE, Ahmed Z, Tainer JA.   +20 more
europepmc   +3 more sources

Anticancer sensitivities and biological characteristics of HCT116 cells resistant to the selective poly(ADP-ribose) glycohydrolase inhibitor. [PDF]

FEBS Open Bio
Poly(ADP‐ribose) glycohydrolase (PARG) is a key enzyme involved in poly(ADP‐ribose) (PAR) degradation and is considered a potential anticancer target. We previously investigated resistance mechanisms to the PARG inhibitor PDD00017273 in human colorectal ...
Tsuda K, Ogino Y, Sato A.
europepmc   +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.
Leonard SM, Pearson CR, Roos WP, Sobol RW.   +3 more
europepmc   +2 more sources

PARG inhibition reduces ssDNA levels and limits RPA loading upon replication fork collapse. [PDF]

EMBO Rep
Poly(ADP-ribosyl)ation (PARylation) is a transient post-translational modification catalyzed by PARP enzymes and reversed by PARG. PARG inhibition causes sustained PARylation and is being explored as an anticancer strategy, but its cellular consequences ...
Mihuț A, Ghosh D, Kószó A, Szüts D, Salajkova SA, Andrs M, Dobrovolna J, Fajka-Boja R, Timinszky G.   +8 more
europepmc   +2 more sources

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

Clin Transl Med
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.
Queralt C, Moreta-Moraleda C, Costa M, Grau-Leal F, Diesch J, Vendrell-Ayats C, Musulén E, Wright RHG, Bugés C, Manzano JL, Cabrero-de Las Heras S, Zuber J, Buschbeck M, Forcales SV, Martínez-Balibrea E.   +14 more
europepmc   +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.
Wang J, Dong Y, Lun W, Nai M, Shi Y, Geng J, Cai W, Liu J, Li H, Li L.   +9 more
europepmc   +2 more sources

Poly(ADP-ribose) glycohydrolase enforces p21 degradation via dePARylation to promote gastric cancer progression. [PDF]

J Clin Invest
Dysregulation of cell cycle checkpoints is a cancer hallmark, with ubiquitination-controlled protein stability playing a pivotal role. Although p21, a key cyclin-dependent kinase inhibitor, is tightly regulated by ubiquitin-mediated degradation, the key ...
Hu Y, Bao Q, Huang Y, Wang Y, Zhao X, Nan J, Meng Y, Deng M, Li Y, Zhuang Z, He H, Zu D, Zhong Y, Zhang C, Wang B, Li R, He Y, Wang Q, Liu M, Tainer JA, Shi Y, Cheng X, Jing J, Ye Z.   +23 more
europepmc   +2 more sources

PARG inhibitor sensitivity correlates with accumulation of single-stranded DNA gaps in preclinical models of ovarian cancer. [PDF]

Proc Natl Acad Sci U S A
Ravindranathan R, Somuncu O, da Costa AABA, Mukkavalli S, Lamarre BP, Nguyen H, Grochala C, Jiao Y, Liu J, Kochupurakkal B, Parmar K, Shapiro GI, D'Andrea AD.   +12 more
europepmc   +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