Efforts are underway to identify a broader group of patients with genomic susceptibility that may benefit from these agents. In an endeavour to enhance anti-tumour effects, PARP inhibitors have been combined with traditional cytotoxic therapy and radiotherapy; however, optimization of dosing schedules ...
Defining the cellular response to pharmacological agents is critical for understanding the mechanism of action of small molecule perturbagens. Here, we developed a 96-well-plate-based high-throughput screening infrastructure for quantitative proteomics and profiled 875 compounds in a human cancer cell ...
Through its targeted inhibition of PARP, ABT-888 demonstrates potential in the treatment of cancers with defective DNA repair mechanisms, offering a novel approach to cancer therapy. Further research and clinical trials continue to explore the full scope of ABT-888's mechanism of action and its ...
20 The resultant ER stress, causing protein misfolding, was proposed as the preferred “mechanism of action” for agents of motif type B (Figure 1).5., 20. The induced misfolded protein was suggested as the trigger for observed MCF-7 apoptosis brought about by such agents. As we recently...
Mechanism of Action Programmed cell death 1 ligand 1 Inhibitor Antibody Programmed cell death protein 1 Inhibitor Identification Summary Atezolizumab is a monoclonal antibody used to treat advanced or metastatic urothelial carcinoma with disease progression during or up to 12 months after platinum-containing...
Querying drug-induced gene expression profiles with machine learning method is an effective way for revealing drug mechanism of actions (MOAs), which is strongly supported by the growth of large scale and high-throughput gene expression databases. However, due to the lack of code-free and user ...
2. PARP-1 is not a base excision repair protein 3. SSBs do not accumulate as a primary lesion after PARP inhibition 4. Interaction between PARP-1 and HR, a story of PARP inhibitors 5. PARP is hyperactivated in HR defective cells and has a role in reactivating stalled replication forks ...
[12].Several studies have found that treatment of breast cancer cells Bcap-37 (ER+) and ZR-75-30 (ER(+); PR(−); HER2(+)) with emodin greatly reduced levels of Bcl-2 and increased the levels of c-casp3, PARP, p53, and Bax, and that its inhibitory growth and apoptosis-inducing...
KEGG enrichment analysis can also suggest the biological mechanisms of action of drugs in the human body and the pathways involved in their regulation. 2.5. Network Construction (1) Cytoscape 3.8.2 was implemented to draw the disease-herb-component-target (D-H-C-T) network to visualize the ...
In their initial studies, Pommier and his colleagues found that the PARP inhibitor olaparib was more toxic tocultured cellsthan genetic elimination of PARP1. According to Pommier, these results indicated that olaparib must have additional modes of action, and their detailed cellular analyses identified...