Plk1 inhibition
Webb29 nov. 2024 · Assessment of PLK1 inhibition is determined by changes in phosphorylation status of pTCTP, a PLK1 substrate. Genomic analysis (detection of … Webb10 rader · Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to …
Plk1 inhibition
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Webb19 aug. 2024 · PLK1 inhibitors were shown, in vitro and in vivo, to possess inhibitory activities against non-small cell lung cancer (NSCLC), and such inhibition has been … WebbPLK1 inhibition enhanced MYC degradation in osteosarcoma cells. PLK1 inhibition led to a marked decline in MYC protein abundance. The representative MYC target genes were deregulated by PLK1 inhibitors. BI2536 treatment caused a significant delay in xenograft tumor growth in mice injected with U-2 OS cells subcutaneously, ...
Webb18 feb. 2016 · For example, we recently showed that Plk1 phosphorylates Axin2, a negative regulator of the WNT/β-catenin pathway, whose expression is significantly elevated in … WebbPLK1 Inhibition Radiosensitizes Breast Cancer Cells, but Shows Low Efficacy as Monotherapy or in Combination with other Cytotoxic Drugs Author (s): María Sol Brassesco*, Julia Alejandra Pezuk, Karina Bezerra Salomão, Gabriela Molinari Roberto, Carlos Alberto Scrideli and Luiz Gonzaga Tone Volume 18, Issue 9, 2024 Page: [1252 - …
Webb1 aug. 2024 · In fact, Plk1 inhibition may be particularly effective in Ras-induced 55,65 or Her2-induced 66 tumors indicating that, independently of a possible tumor suppressor … WebbBackground and Purpose: Over the last decade, the inhibition of PLK1 has proven potent antiproliferative activity in vitro. However, the effectiveness of most synthetic targeted …
Webb17 apr. 2007 · Polo-like kinase 1 (Plk1) regulates mitotic progression in all eukaryotes and has been implicated in the transformation of human cells. Analysis of the cytological …
Webb1 mars 2016 · PLK1 depletion leading to G2/M arrest, inhibition of cell proliferation and promotion of apoptosis via downregulation of Survivin expression has also been reported . RB activity is responsible for repression of the PLK1 promoter, which in turn depends on the activity of SWI/SNF chromatin remodeling complex [ 17 ]. drought in the sahel regionWebb5 nov. 2024 · PLK1 inhibition with volasertib, alone and in combination with the BCL-2 inhibitor venetoclax, was efficacious in multiple DHL models, including mice harboring … drought in the uk case studyWebb12 juli 2024 · The first-generation PLK1 inhibitors were designed to target the catalytic N-terminal kinase domain (KD). Despite their ability to inhibit the viability and progression … drought issueWebb21 nov. 2024 · We examined the effect of PLK1 inhibition via treatment with onvansertib, an oral available PLK1 inhibitor, alone or in combination with paclitaxel on mouse … drought in west bengal coastal areaWebbWhile studies have indicated that the use of PLK1 inhibition may overcome drug resistance in chemotherapy [31,32,33], other research has aimed to enhance the efficacy of standard therapy through PLK1i-based combinations, such as in ovarian cancer with CCNE1 amplification, where the PLK1 inhibitor BI6727 in combination can potentiate the effect … drought in western united statesWebbthat PLK1 inhibition may not be propitious to all cancers. In line with this, several studies have claimed the TP53 mutation is a biomarker for cancer sensitivity to PLK1 inhibition, … drought in western usWebbPLK1 inhibition enhanced MYC degradation in osteosarcoma cells. PLK1 inhibition led to a marked decline in MYC protein abundance. The representative MYC target genes were … drought in the us west