Selective PARP1 inhibitors, PARP1-based dual-target inhibitors, PROTAC PARP1 degraders, and prodrugs of PARP1 inhibitors for cancer therapy

X Peng, W Pan, F Jiang, W Chen, Z Qi, W Peng… - Pharmacological …, 2022 - Elsevier
Poly ADP-ribose polymerase (PARP) plays a critical role in many cellular processes such as
DNA damage repair, gene transcription and cell apoptosis. Therefore, targeting PARP …

Therapeutic strategies of dual-target small molecules to overcome drug resistance in cancer therapy

J Ye, J Wu, B Liu - Biochimica et Biophysica Acta (BBA)-Reviews on …, 2023 - Elsevier
Despite some advances in targeted therapeutics of human cancers, curative cancer
treatment still remains a tremendous challenge due to the occurrence of drug resistance. A …

Discovery, Synthesis, and Evaluation of Novel Dual Inhibitors of a Vascular Endothelial Growth Factor Receptor and Poly (ADP-Ribose) Polymerase for BRCA Wild …

Y Li, Y Liu, D Zhang, J Chen, G Yang… - Journal of Medicinal …, 2023 - ACS Publications
Poly (ADP-ribose) polymerase (PARP) inhibitors have been approved for the treatment of
breast cancer (BC) with breast cancer susceptibility (BRCA) gene mutation. Leveraging new …

Design, synthesis, biological evaluation and molecular docking study of novel urea-based benzamide derivatives as potent poly (ADP-ribose) polymerase-1 (PARP-1) …

G Lu, W Nie, M Xin, Y Meng, J Gu, H Miao… - European Journal of …, 2022 - Elsevier
Abstract Poly (ADP-ribose) polymerase-1 (PARP-1) is one of the key members of DNA repair
enzymes that is responsible for the repair of DNA single-strand breaks. Inhibition of PARP-1 …

Discovery of Quinazoline-2,4(1H,3H)-dione Derivatives Containing a Piperizinone Moiety as Potent PARP-1/2 Inhibitors─Design, Synthesis, In Vivo Antitumor …

J Zhou, T Du, X Wang, H Yao, J Deng, Y Li… - Journal of Medicinal …, 2023 - ACS Publications
PARP-1/2 inhibitors have become an important therapeutic strategy for the treatment of HR-
deficient tumors. However, discovery of new inhibitors with an improved and distinct …

Synthesis of 3-(Pyridin-2-yl)quinazolin-2,4(1H,3H)-diones via Annulation of Anthranilic Esters with N-pyridyl Ureas

SO Baykova, KK Geyl, SV Baykov… - International Journal of …, 2023 - mdpi.com
A new route for the synthesis of quinazolin-2, 4 (1 H, 3 H)-diones and thieno [2, 3-d]
pyrimidine-2, 4 (1 H, 3 H)-diones substituted by pyridyl/quinolinyl moiety in position 3 has …

Dual target PARP1/EZH2 inhibitors inducing excessive autophagy and producing synthetic lethality for triple-negative breast cancer therapy

X Li, C Wang, S Li, F Yin, H Luo, Y Zhang, Z Luo… - European journal of …, 2023 - Elsevier
Currently available PARP inhibitors are mainly used for the treatment of BRCA-mutated
triple-negative breast cancer (TNBC), with a narrow application range of approximately 15 …

Prudent tactics to sail the boat of PARP inhibitors as therapeutics for diverse malignancies

M Rana, A Thakur, C Kaur, CH Pan… - Expert Opinion on …, 2023 - Taylor & Francis
Introduction PARP inhibitors block the DNA-repairing mechanism of PARP and represent a
promising class of anti-cancer therapy. The last decade has witnessed FDA approvals of …

Identification of [1, 2, 4] triazolo [4, 3-a] pyrazine PARP1 inhibitors with overcome acquired resistance activities

P Wang, WT Zhu, Y Wang, SS Song, Y Xi… - European Journal of …, 2023 - Elsevier
Abstract Poly (ADP-ribose) polymerase 1 (PARP1) inhibitors can selectively kill homologous
recombination (HR) deficient cancer cells and elicit anticancer effect through a mechanism …

Collagen I-induced VCAN/ERK signaling and PARP1/ZEB1-mediated metastasis facilitate OSBPL2 defect to promote colorectal cancer progression

K Lin, Y Zhao, Y Tang, Y Chen, M Lin, L He - Cell Death & Disease, 2024 - nature.com
The global burden of colorectal cancer (CRC) has rapidly increased in recent years.
Dysregulated cholesterol homeostasis facilitated by extracellular matrix (ECM) remodeling …