PARP
Poly (ADP-ribose) polymerase (PARP; EC 2.4.2.12) is found in the cell’s nucleus. The main role is to detect and signal single strand DNA breaks, preventing healthy cells from malfunctioning and programmed cell death. Cancer cells may also use PARP to repair DNA damage, thus extending their uncontrolled growth. Such cancers can become resistant to treatment (chemotherapy and/or radiation). PARP inhibitors may be especially helpful for the treatment of tumors due to genetic mutations of BRCA1 and BRCA2[1]. Human tankyrases, or TRF1-interacting ankyrin-related ADP-ribose polymerases, are specific PARPs that enhance telomerase access to telomeres, and post-translationally modify multiple proteins involved in processes including maintenance of telomere length, sister telomere association, and trafficking of glut4-containing vesicles[2],[3].
[1] A. Patel, S.H. Kaufmann. Development of PARP Inhibitors: An Unfinished Story. Oncology. 2010, 24, 66-68.
[2] Y.J. Chiang et al. Tankyrase 1 and Tankyrase 2 Are Essential but Redundant for Mouse Embryonic Development. PLoSONE 2008, 3, e2639.
[3] H. Seimiya. The telomeric PARP, tankyrases, as targets for cancer therapy. Br. J. Cancer. 2006, 94, 341-345.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 1593 | ABT 888 | PARP inhibitor | €55.00 | |
| 2888 | ABT 888 dihydrochloride | PARP inhibitor | Recently added | €95.00 |
| 1529 | AG 014699 | PARP1 inhibitor | €75.00 | |
| 1496 | Aminobenzamide, 3- | Competitive small molecule inhibitor of PARP | €45.00 | |
| 1464 | AZD 2281 | PARP inhibitor | €55.00 | |
| 2241 | AZD 2461 | PARP inhibitor with poor P-glycoprotein substrate qualities | €105.00 | |
| 1268 | DR 2313 | PARP inhibitor | €90.00 | |
| 1566 | Iniparib | PARP inhibitor | €65.00 | |
| 2537 | Isoquinolinediol, 1,5- | PARP1 inhibitor and neuroprotective agent | €50.00 | |
| 2001 | KU 0058948 hydrochloride | Potent and specific PARP1 inhibitor | €135.00 | |
| 2759 | ME0328 | PARP3/ARTD3 inhibitor | €95.00 | |
| 2928 | Niraparib | Potent, selective, and orally available PARP1/2 inhibitor | Recently added | €105.00 |
| 1370 | NU 1025 | PARP inhibitor | €80.00 | |
| 2502 | Talazoparib | Potent, selective, and orally available PARP1/2 inhibitor | €105.00 | |
| 2369 | UPF 1069 | PARP-2 inhibitor with >26 fold selectivity over PARP1 | €75.00 | |