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Revealing the selective mechanisms of inhibitors to PARP-1 and PARP-2 via multiple computational methods [PDF]

open access: yesPeerJ, 2020
Background Research has shown that Poly-ADP-ribose polymerases 1 (PARP-1) is a potential therapeutic target in the clinical treatment of breast cancer.
Hongye Hu   +3 more
doaj   +3 more sources

CldU sensitizes BRCA2 reverse-mutated cells to PARP inhibitors [PDF]

open access: yesFrontiers in Oncology
PARP inhibitors are widely used class of drugs for the treatment of homologous recombination deficient cancers, including BRCA mutated ones. These drugs led to substantial improvement in survival, particularly for patients with BRCA mutated tumors ...
Nawel Zouggari   +9 more
doaj   +2 more sources

PARP inhibitors and breast cancer: from therapeutic breakthrough to resistance challenge [PDF]

open access: yesExperimental and Molecular Medicine
Breast cancer remains the leading cause of cancer-related mortality among women worldwide. Poly(ADP-ribose) polymerase (PARP) inhibitors have emerged as a critical therapeutic option, particularly for patients with triple-negative breast cancer and other
Weiyun Wang   +10 more
doaj   +2 more sources

PARP Inhibitors in Ovarian Cancer [PDF]

open access: yesRecent Patents on Anti-Cancer Drug Discovery, 2018
Treatment of Epithelial Ovarian Cancer (EOC), historically based on surgery and platinum doublet chemotherapy, is associated with high risk of relapse and poor prognosis for recurrent disease. In this landscape, the innovative treatment with PARP inhibitors (PARPis) demonstrated an outstanding activity in EOC, and is currently changing clinical ...
Giorgio Valabrega   +2 more
exaly   +3 more sources

PARP inhibitors in melanoma treatment: potential, challenges, and future directions [PDF]

open access: yesFrontiers in Oncology
Genome integrity is a critical driver of cellular stability, and defects in the processes that maintain genome health are potent sources of cancer progression.
Angela Anaeme   +4 more
doaj   +2 more sources

PARP inhibitors for prostate cancer

open access: yesSeminars in Oncology
Poly(ADP-ribose) polymerase (PARP) inhibitors have transformed the treatment landscape for patients with metastatic castration-resistant prostate cancer (mCRPC) and alterations in DNA damage response genes. This has also led to widespread use of genomic testing in all patients with mCRPC.
Nick Beije, Johann S de Bono
exaly   +3 more sources

PARP inhibitors [PDF]

open access: yesHereditary Cancer in Clinical Practice, 2015
بوليميرازات بولي (ADP - ريبوز)، التي يتم اختصارها باسم PARPs، هي مجموعة من البروتينات المألوفة التي تلعب دورًا مركزيًا في إصلاح الحمض النووي باستخدام مسار إصلاح استئصال القاعدة (BER). هناك حوالي 17 بروتينًا في هذه العائلة منها PARPs النووية الأولية هي PARP -1 و PARP -2 و PARP -3 و tankyrases 1 و 2 (PARP -5a و -5b).
Maheen Anwar   +2 more
  +8 more sources

Combined inhibition of PARP and EZH2 for cancer treatment: Current status, opportunities, and challenges

open access: yesFrontiers in Pharmacology, 2022
Tumors with BRCA1/2 mutations or homologous recombination repair defects are sensitive to PARP inhibitors through the mechanism of synthetic lethality. Several PARP inhibitors are currently approved for ovarian, breast and pancreatic cancer in clinical ...
Xi Zhang   +5 more
doaj   +1 more source

Polyadenosine diphosphate-ribose polymerase inhibitors: advances, implications, and challenges in tumor radiotherapy sensitization

open access: yesFrontiers in Oncology, 2023
Polyadenosine diphosphate-ribose polymerase (PARP) is a key modifying enzyme in cells, which participates in single-strand break repair and indirectly affects double-strand break repair.
Yi Zhang   +6 more
doaj   +1 more source

Design and synthesis of benzodiazepines as brain penetrating PARP-1 inhibitors

open access: yesJournal of Enzyme Inhibition and Medicinal Chemistry, 2022
The poly (ADP-ribose) polymerase (PARP) inhibitors play a crucial role in cancer therapy. However, most approved PARP inhibitors cannot cross the blood-brain barrier, thus limiting their application in the central nervous system. Here, 55 benzodiazepines
Jiang Yu   +8 more
doaj   +1 more source

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