Poly (ADP-Ribose) Polymerases (PARPs) and PARP Inhibitor-Targeted Therapeutics.
Anticancer Agents Med Chem
; 19(2): 206-212, 2019.
Article
en En
| MEDLINE
| ID: mdl-30417796
ABSTRACT
BACKGROUND:
Poly-ADP-ribosylation, that is, adding ADP-ribose moieties to a protein, is a unique type of protein post-translational modification that regulates various cellular processes such as DNA repair, mitosis, transcription, and cell growth. Small-molecule inhibitors of poly-ADP-ribose polymerase 1 (PARP1) have been developed as anticancer agents because inhibition of PARP enzymes may be a synthetic lethal strategy for cancers with or BRCA2 mutations. However, there are still questions surrounding PARP inhibitors. METHODS/RESULTS:
Data were collected from Pubmed, Medline, through searching of these keywords "PARP", "BRCA", "Synthetic lethal" and "Tankyrase inhibitors". We describe the current knowledge of PARP inhibition and its effects on DNA damage; mechanisms of resistance to PARP inhibitors; the evolution of PARP inhibitors; and the potential use of PARP5a/b (tankyrases) inhibitors in cancer treatment.CONCLUSION:
PARP inhibitors are already showing promise as therapeutic tools, especially in the management of BRCA-mutated breast and ovarian cancers but also in tumors with dysfunctional BRCA genes. Small-molecule tankyrase inhibitors are important for increasing our understanding of tankyrase biology.Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Neoplasias Ováricas
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Neoplasias de la Mama
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Poli(ADP-Ribosa) Polimerasas
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Bibliotecas de Moléculas Pequeñas
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Inhibidores de Poli(ADP-Ribosa) Polimerasas
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Antineoplásicos
Límite:
Animals
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Female
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Humans
Idioma:
En
Año:
2019
Tipo del documento:
Article