PARP inhibitor

Poly(ADP-ribose)polyrmerase (PARP) inhibitors, 42 (2004) 125 P2 Purinoreceptor ligands, 38 (2001) 115 p38 MAP kinase inhibitors, 38 (2001) 1 Paclitaxel, anticancer agent, 32 (1995) 289... 

PARP-1 in vitro. The insulator function of most of the same CTCF target sites was sensitive to the general PARP inhibitor 3-aminobenzamide. Collectively, these results support a role for PAR and PARP(s) in the activity of insulators, with an insulator-bound protein, possibly CTCF, as a target for PARylation. 

Curtin NJ (2006) PARP inhibitors and cancer therapy. In Biirlde A (ed) Poly(ADP-Ribosyl)ation. Landes Bioscience, Georgetown, pp218—233... 

Down-regulation of BRCA protein or interference of Rad51 foci formation has been reported for a variety of conditions including inhibition of CDKl (30), mild hyperthermia (31), hypoxia (32), loss of PTEN (33, 34), loss of PALB2 (35), or over-expression of EMSY (36). The BRCAness phenotype induced under all these conditions makes cancer cells more sensitive to PARP inhibition. The key is to develop a functional assay for BRCAness to enable stratification of cancer patients for clinical trials of PARP inhibitors. 

Liu X, Shi Y, Maag DX et al (2012) Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor. Clin Cancer Res 18 510-523... 

Schelman WR, Sandhu SK, Moreno GV et al (2011) First-in-human trial of a poly(ADP)-ribose polymerase (PARP) inhibitor MK-4827 in advanced cancer patients with antitumor activity in BRCA-deficient tumors and sporadic ovarian cancers (soc). J Clin Oncol 29 abstr 3102... 

Isakoff S, Overmoyer B, Tung N et al (2010) A phase II trial of the PARP inhibitor veliparib (ABT888) and temozolomide for metastatic breast cancer. J CKn Oncol 28 abstr 1019... 

Ibragimova I, Cairns P (2011) Assays for hyper-methylation of the BRCAI gene promoter in tumor cells to predict sensitivity to PARP-inhibitor therapy. Methods Mol Biol 780 277-291... 

Mendes P, Ana M, Martin SA et al (2009) Synthetic lethal targeting of PTEN mutant cells with PARP inhibitors. EMBO Mol Med 1 315-322... 

Since isoquinolinones are known to be very potent inhibitors of poly(ADP-ribose)polymerase (PARP), thieno[3,4-( ]pyridin-4-ones have been studied for their potential as PARP inhibitors <1999BMC297>. Early studies indicate that the sulfur analogues also act as potent PARP inhibitors. Thienopyridine diazonium salts can be converted into heterocyclic dyes that are useful as disperse dyes for polyester fabrics <2005DP(64)223, 2006DP(70)60>. 

Constantino et al. used the combination of a docking-based alignment and 3D QSAR analysis to build a predictive model for 46 poly(ADP-ribose)polymer-ase (PARP) inhibitors [67]. Representative PARP inhibitors were docked into... 

Costantino, G., Macchiarulo, A., Camaio-ni, E., Pellicciari, R. Modeling of Poly(-ADP-ribose)polymerase (PARP) Inhibitors. Docking of Ligands and Quantitative Structure-Activity Relationship Analysis. J. Med. Chem. 2001, 44, 3786-3794. 

Miller BA (2004) Inhibition of TRPM2 function by PARP inhibitors protects ceUs from oxidtidve stress-induced death. Br J Pharmacol 143 515-516... 

Human mononuclear leukocytes are a good model for studying SM-induced cytotoxicity. Niacinamide, 3-aminobenzamide, and PARP inhibitors have been shown to be... 

Inhibitors of mono(ADP-ribose) transferase, lipid peroxidation, and protein synthesis are not effective in reducing SM-induced cell death, while PARP inhibitors are found to be efifective in reducing the cytotoxic effects of SM in human lymphocytes. The compound s ability to inhibit PARP has a direct correlation to its ability to reduce SM-induced cell death. PARP plays an important role in SM-induced cell death (Clayson et al., 1993). The effectiveness of various therapeutic agents, namely niacin,... 

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