1.Xiaopeng Peng, Wanyi Pan, Feng Jiang, Weiming Chen, Zetao Qi, Weijie Peng, Jianjun Chen, Selective PARP1 inhibitors, PARP1-based dual-target inhibitors, PROTAC PARP1 degraders, and prodrugs of PARP1 inhibitors for cancer therapy, Pharmacological Research 186 (2022)...
2024年5月22日,山东大学史大永教授团队合作在JMC上发表了题为“Design of Selective PARP‑1 Inhibitors and Antitumor Studies”的文章,通过对PARP-1和PARP-2的序列比较,确定了一个可能的选择位点(S位点)。针对这个S位点,作者研究发现了化合物I16,其...
1.PARP-1: Structural insights and pharmacological targets for inhibition. DNA Repair 103 （2021） 103125.2.A therapeutic update on PARP inhibitors: implications in the treatment of glioma. Drug Discovery Today. 2020 3.《合成致死：PARP抑制剂市场攀升，未来谁来分羹？》-新浪医药 4.选择性PARP-1抑制...
N at position 3 may be C, A or T, preferably A or T, more preferably T; N at position 2 may be C; W at position 4 may be T; and R at position 1 may be A. The nucleic acid may have the sequence ACATCAAA or ACTTCAAA.REN, EE CHEEKO, HUI LING...
PARP1 inhibitors (PARPi) are known to kill tumor cells via two mechanisms (PARP1 catalytic inhibition and PARP1 trapping). The relative contribution of these two pathways in mediating the cytotoxicity of PARPi, however, is not well understood. Here we designed a series of small molecule PARP...
3#Development of KSQ-4279 as a first-in-class USP1 inhibitor for the treatment of BRCA-deficient cancers(来源:ENA 2020) 4#USP1 inhibitors show robust combination activity and a distinct resistance profile from PARP inhibitors(来源:ENA 2020)...
Results of tamoxifen and aromatase inhibitors about the risk of serious coronary malady throughout aging adults breast cancers individuals: A great examination involving country wide info. Posted on February 14, 2025 To summarize, an isocaloric diet of 2800 kcal ME/kg containing 21% CP in Aseel...
The therapeutic potential of poly(ADP-ribose) polymerase inhibitors. Pharmacol Rev 54, 375–429 (2002). 17. Kim, M. Y., Zhang, T. & Kraus, W. L. Poly(ADP-ribosyl)ation by PARP-1: 'PAR-laying' NAD+ into a nuclear signal. Genes Dev 19, 1951–1967 (2005). 18. Orsucci, D....
and non-toxic PARP-1 inhibitors using an integrated approach that combines machine learning-based screening, molecular docking simulations, and quantum mechanical calculations. We trained a widely used machine learning models, Random Forest, using bioactivity data from known PARP-1 inhibitors. After eval...
cliffs, which possibly negatively impacts the model’s predictive performance. Finally, a set of chemical transformation rules were extracted using the matched molecular pair analysis (MMPA) which provided mechanistic insights and can guide medicinal chemists in the design of novel PARP-1 inhibitors. ...