Design, synthesis and biological evaluation of erythrina derivatives bearing a 1,2,3-triazole moiety as PARP-1 inhibitors DOI
Shuai Li, Xinyang Li, Tingjian Zhang

и другие.

Bioorganic Chemistry, Год журнала: 2020, Номер 96, С. 103575 - 103575

Опубликована: Янв. 10, 2020

Язык: Английский

Progress of Bromophenols in Marine Algae from 2011 to 2020: Structure, Bioactivities, and Applications DOI Creative Commons

Hui Dong,

Songtao Dong,

Poul Erik Hansen

и другие.

Marine Drugs, Год журнала: 2020, Номер 18(8), С. 411 - 411

Опубликована: Авг. 4, 2020

Marine algae contain various bromophenols that have been shown to possess a variety of biological activities, including antiradical, antimicrobial, anticancer, antidiabetic, anti-inflammatory effects, and so on. Here, we briefly review the recent progress these marine biomaterials their derivatives from 2011 2020, with respect structure, bioactivities, potential application as pharmaceuticals.

Язык: Английский

Процитировано

45
Selective PARP1 inhibitors, PARP1-based dual-target inhibitors, PROTAC PARP1 degraders, and prodrugs of PARP1 inhibitors for cancer therapy DOI
Xiaopeng Peng,

Wanyi Pan,

Feng Jiang

и другие.

Pharmacological Research, Год журнала: 2022, Номер 186, С. 106529 - 106529

Опубликована: Окт. 31, 2022

Язык: Английский

Процитировано

24
Design of Selective PARP-1 Inhibitors and Antitumor Studies DOI
Yiting Zhang, Xiangqian Li, Fang Liu

и другие.

Journal of Medicinal Chemistry, Год журнала: 2024, Номер 67(11), С. 8877 - 8901

Опубликована: Май 22, 2024

Designing selective PARP-1 inhibitors has become a new strategy for anticancer drug development. By sequence comparison of and PARP-2, we identified possible site (S site) consisting several different amino acid residues α-5 helix D-loop. Targeting this S site, 140 compounds were designed, synthesized, characterized their activities mechanisms. Compound

Язык: Английский

Процитировано

5
Recent Progress in Poly(ADP–Ribose) Polymerase‐1 Inhibitors for Application in Cancer DOI Open Access

Anuradha Mehra,

Sayemul Islam, Rekha Sangwan

и другие.

ChemistrySelect, Год журнала: 2025, Номер 10(1)

Опубликована: Янв. 1, 2025

Abstract An ADP‐ribosylating enzyme called poly (ADP–ribose) polymerase 1 (PARP1) is necessary to start several types of DNA repair. PARP1 also contributes significantly the regulation gene expression through enzyme‐independent motif recognition and enzyme‐dependent chromatin remodeling. Thus, synthetic lethality achieved in therapy tumors cancers by blocking undesired repair inhibition its activity with small molecules. In addition outlining most recent research from 2019 2024 on precise ways which regulates each process independently, we discussed how transcription are interdependent enough that perturbations caused enzymatic inhibition, disease‐related hyperactivation. Herein, this concept review systematically summarizes different approach for designing selective inhibitor i) PARP1–DNA trapping approach, ii) hybrid iii) PROTAC iv) dual target updates clinical trials.

Язык: Английский

Процитировано

0
Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1) DOI Creative Commons
Zhimin Zhang, Xinyue Chang,

Chixiao Zhang

и другие.

Journal of Enzyme Inhibition and Medicinal Chemistry, Год журнала: 2020, Номер 35(1), С. 1606 - 1615

Опубликована: Янв. 1, 2020

Poly(ADP-ribose) polymerase-1 (PARP-1), a critical DNA repair enzyme in the base excision pathway, has been pursued as an attractive cancer therapeutic target. Intervention with PARP-1 proved to be more sensitive cells carrying BRCA1/2 mutations. Several inhibitors have available on market for treatment of breast, ovarian and prostatic cancer. Promisingly, newly developed proteolysis targeting chimaeras (PROTACs) may provide potential strategy based degradation PARP-1. Here we report design, synthesis, evaluation chimaera (PROTAC) combination inhibitor olaparib CRBN (cereblon) ligand lenalidomide. In SW620 cells, our probe-quality degrader compound 2 effectively induced which results anti-proliferation, apoptosis, cell cycle arresting, migratory inhibition. Thus, findings qualify new chemical probe knockdown.

Язык: Английский

Процитировано

35
Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2 DOI
Yu Jiang, Lingling Luo,

Tong Hu

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2021, Номер 227, С. 113898 - 113898

Опубликована: Окт. 11, 2021

Язык: Английский

Процитировано

29
Multi-therapies Based on PARP Inhibition: Potential Therapeutic Approaches for Cancer Treatment DOI
Jie Zhang, Yuqi Gao, Zipeng Zhang

и другие.

Journal of Medicinal Chemistry, Год журнала: 2022, Номер 65(24), С. 16099 - 16127

Опубликована: Дек. 13, 2022

The nuclear enzymes called poly(ADP-ribose)polymerases (PARPs) are known to catalyze the process of PARylation, which plays a vital role in various cellular functions. They have become important targets for discovery novel antitumor drugs since their inhibition can induce significant lethality tumor cells. Therefore, researchers all over world been focusing on developing and potent PARP inhibitors cancer therapy. Studies shown that other agents, such as EZH2 EGFR inhibitors, play synergistic combined with effects may provide rational strategy improve effectiveness current anticancer regimens. In this Perspective, we sum up recent advance PARP-targeted including single-target inhibitors/degraders dual-target inhibitors/degraders, discuss fundamental theory these give insight into corresponding structure–activity relationships agents.

Язык: Английский

Процитировано

20
Design, synthesis, biological evaluation and molecular docking study of novel urea-based benzamide derivatives as potent poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors DOI

Guoqing Lu,

Wenxing Nie,

Meixiu Xin

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2022, Номер 243, С. 114790 - 114790

Опубликована: Сен. 23, 2022

Язык: Английский

Процитировано

19
An overview of compound properties, multiparameter optimization, and computational drug design methods for PARP-1 inhibitor drugs DOI
Bhakti Umesh Hirlekar,

Anila Nuthi,

Krishan Dev Singh

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2023, Номер 252, С. 115300 - 115300

Опубликована: Март 22, 2023

Язык: Английский

Процитировано

11
Advances in Development of Selective Antitumor Inhibitors That Target PARP-1 DOI
Fang Liu, Jia‐Shu Chen, Xiangqian Li

и другие.

Journal of Medicinal Chemistry, Год журнала: 2023, Номер 66(24), С. 16464 - 16483

Опубликована: Дек. 13, 2023

Cancer is a major threat to the lives and health of people around world, development effective antitumor drugs that exhibit fewer toxic effects an important aspect cancer treatment. PARP inhibitors are target pathways involved in DNA-damage repair. The currently approved include olaparib, niraparib, rucaparib, talazoparib, fuzuloparib, pamiparib. Hematological toxicities associated with simultaneous inhibition PARP-1 PARP-2 have limited clinical applications these drugs. present review introduces necessity for research on selective from perspective structural functional mechanisms inhibition. A recently reported provides foundation exploring novel strategies designing structure–activity relationships combined computer simulations.

Язык: Английский

Процитировано

11