Pharmacological enzyme inhibitors of poly (ADP-ribose) polymerases
Model of the inhibitor olaparib (dark gray) occupying the NAD+-binding site of PARP1. From PDB: 5DS3.
PARP inhibitors are a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase (PARP).
They are developed for multiple indications, including the treatment of heritable cancers.[1] Several forms of cancer are more dependent on PARP than regular cells, making PARP (PARP1, PARP2 etc.) an attractive target for cancer therapy.[2][3][4][5] PARP inhibitors appear to improve progression-free survival in women with recurrent platinum-sensitive ovarian cancer, as evidenced mainly by olaparib added to conventional treatment.[6]
In addition to their use in cancer therapy, PARP inhibitors are considered a potential treatment for acute life-threatening diseases, such as stroke and myocardial infarction, as well as for long-term neurodegenerative diseases.[7]
^Blankenhorn D (2009-06-25). "PARP inhibitors working against inherited cancers | ZDNet Healthcare | ZDNet.com". ZDNet Healthcare owned by CBS Interactive Inc. ZDNet. Archived from the original on 2009-06-28. Retrieved 2019-12-05.
^Pam Stephan. "PARP Inhibitor and DNA Polymerase Repair - PARP Inhibitor". About.com Health.
^"Development of PARP Inhibitors: An Unfinished Story". cancernetwork.com. ONCOLOGY Vol 24 No 1. 24 (1). 15 January 2010.
^"PARP Inhibitors – More Widely Effective than First Thought". drugdiscoveryopinion.com.
^"PARP inhibitors: Halting cancer by halting DNA repair". Cancer Research UK. 24 September 2020.
^Tattersall, Abigail; Ryan, Neil; Wiggans, Alison J.; Rogozińska, Ewelina; Morrison, Jo (2022-02-16). "Poly(ADP-ribose) polymerase (PARP) inhibitors for the treatment of ovarian cancer". The Cochrane Database of Systematic Reviews. 2022 (2): CD007929. doi:10.1002/14651858.CD007929.pub4. ISSN 1469-493X. PMC 8848772. PMID 35170751.
^Graziani G, Szabó C (July 2005). "Clinical perspectives of PARP inhibitors". Pharmacological Research. 52 (1): 109–18. doi:10.1016/j.phrs.2005.02.013. PMID 15911339.
PARPinhibitors are a group of pharmacological inhibitors of the enzyme poly ADP ribose polymerase (PARP). They are developed for multiple indications...
BRCA-mutated advanced ovarian cancer in adults. It is a PARPinhibitor, inhibiting poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair. It acts against...
prostate cancer. It is an orally available poly ADP ribose polymerase PARPinhibitor marketed by Pfizer for the treatment of advanced breast cancer with...
potential anti-cancer drug acting as a PARPinhibitor. It kills cancer cells by blocking a protein called PARP, thereby preventing the repair of DNA or...
fallopian tube, or primary peritoneal cancer. It is taken by mouth. It is a PARPinhibitor. The most common side effects include nausea (feeling sick), thrombocytopenia...
Rucaparib, sold under the brand name Rubraca, is a PARPinhibitor used as an anti-cancer agent. Rucaparib is a first-in-class pharmaceutical drug targeting...
irreversible inhibitor of PARP1 (hence, a PARPinhibitor) and possibly other enzymes through covalent modification, but its effects against PARP were later...
Poly [ADP-ribose] polymerase 1 (PARP-1) also known as NAD+ ADP-ribosyltransferase 1 or poly[ADP-ribose] synthase 1 is an enzyme that in humans is encoded...
which biomarkers are predictive of responsiveness to PARPinhibitors. Rucaparib is another PARPinhibitor being researched in BRCA-positive and BRCA-negative...
PD1 inhibitor that was approved by the FDA in 2014. Pembrolizumab is approved to treat melanoma and lung cancer. Antibody BGB-A317 is a PD-1 inhibitor (designed...
cancer. It is approved for use in China. It is an inhibitor of the poly (ADP-ribose) polymerase (PARP) enzyme. It is also being studied for its potential...
mTOR was made in 1994 while investigating the mechanism of action of its inhibitor, rapamycin. Rapamycin was first discovered in 1975 in a soil sample from...
A mitotic inhibitor, microtubule inhibitor, or tubulin inhibitor, is a drug that inhibits mitosis, or cell division, and is used in treating cancer, gout...
BRCAness. This classifier can be applied to assess the implementation of PARPinhibitors in patients with BRCA1/BRCA2 deficiency. The final output is a probability...
plant and animal PARP1 proteins. Some PARPinhibitor anti-cancer drugs (primarily aimed at PARP1) also inhibit PARP2, e.g. niraparib. PARP2 has been shown...
therapy including small-molecule drugs or monoclonal antibodies, and PARPinhibitors such as olaparib. Other therapies include hyperthermia, immunotherapy...
and if positive for the BRAF V600 mutation, a BRAF inhibitor or BRAF inhibitor with an MEK inhibitor. Effectiveness was established based on objective...
it. PARPinhibitors are used to treat endometrial cancer with PTEN mutations, specifically, mutations that lower the expression of PTEN. The PARP inhibitor...
gene (BRCA1 and 2), a treatment which received FDA approval in 2016 (PARPinhibitor). A sub-case of synthetic lethality, where vulnerabilities are exposed...
treatment of various types of cancer. Pamiparib is a member of the PARPinhibitor drug class. In China, it is approved for the treatment of germline BRCA...
the treatment of certain kinds of breast cancer. Ribociclib is a kinase inhibitor. It was developed by Novartis and Astex Pharmaceuticals. The most common...
and stops synthesis; and IRI – irinotecan (Camptosar), a topoisomerase inhibitor, which prevents DNA from uncoiling and duplicating. FOLFIRI is used for...
compound LT-673, an orally available poly (ADP-ribose) polymerase (PARP) inhibitor studied for the treatment of patients with rare, genetically defined...
non-peptidic proteasome inhibitor discovered was the natural product lactacystin. Disulfiram has been proposed as another proteasome inhibitor. Epigallocatechin-3-gallate...
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