Targeting wee1 kinase in cancer

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WebDec 7, 2024 · Selinexor for use in children with cancer is also being explored with other novel therapies, including small molecules targeting CDK 4/6 (palbociclib) and Wee1 … WebReena Beggs, Eddy S. Yang, in Advances in Protein Chemistry and Structural Biology, 2024. 4.2 Wee1. Wee1 is a tyrosine kinase that is known to be overexpressed in many cancer types such as luminal and HER2-positive breast cancer subtypes, hepatocellular carcinomas, and glioblastomas (Iorns et al., 2009).Wee1 directly interacts with histone H2B to halt …

Fighting resistance: post-PARP inhibitor treatment strategies in ...

WebFeb 3, 2024 · Cotreatment of PARGi and Wee1i shows synergistic cancer cell killing in vitro To assess possible synergies between targeting PARG and DDR candidates (ATR, CHK1, and Wee1), we performed a focused drug screen in the established PDAC cell line, PANC1. ATRi and CHK1i were not synergistic with PARGi (Supplementary Fig. S1A). WebJul 1, 2016 · WEE1 kinase plays a crucial role in the G2-M cell-cycle checkpoint arrest for DNA repair before mitotic entry. Normal cells repair damaged DNA during G1 arrest; … banjir pasir mas

Wee1 - an overview ScienceDirect Topics

WebOct 26, 2024 · Li and colleagues demonstrate that the cell-cycle checkpoint kinase CHK1 phosphorylates and inactivates FAM122A, an inhibitor of the phosphatase PP2A. Activated PP2A in turn dephosphorylates WEE1, prevents its ubiquitin-mediated proteolysis, increases WEE1 protein levels, and promotes the G2/M checkpoint. Loss of FAM122A expression is … WebNov 1, 2024 · Abstract. In the past decade, Wee1 inhibition has received widespread attention as a cancer therapy. Our research aims to discover effective, selective and drug-like Wee1 inhibitors. Herein, a series of compounds with pyrrolo [2,3-d]pyrimidine-based heterocycles were designed, synthesized and confirmed to inhibit Wee1 kinase. WebJul 9, 2024 · WEE1 is a protein kinase involved in many cellular processes, one of which is its role as a regulator of the S-phase and G2-M cell-cycle checkpoint, which respond to DNA damage or replication stress. The majority of human cancer cells have a deficient G1-S checkpoint, often via mutation of p53, and are particularly reliant on a functional G2-M ... banjir pati 2023

Therapeutic Targeting of Exportin-1 in Childhood Cancer

Synthetic lethal interaction between WEE1 and PKMYT1 is a target …

WebJan 12, 2024 · The cell-cycle checkpoint kinase WEE1 is emerging as a therapeutic target for cancer treatment. However, how its catalytic activity is regulated remains poorly understood, and reliable biomarkers ... WebSep 21, 2024 · Among them, the most promising ones target the WEE1 kinase family, which has a crucial role in cell cycle regulation and DNA damage identification and repair in both … banjir pasteurWebTargeting the checkpoint kinase WEE1. Selective sensitization of cancer cells to DNA-damaging drugs. Paola Indovina. 1,2. ... Tse AN, Carvajal R, Schwartz GK. Targeting check-point kinase 1 in cancer therapeutics. Clin Cancer Res 2007; 13:1955-60. 11. Kawabe T. G. 2. checkpoint abrogators as anticancer drugs. Mol Cancer Ther 2004; 3:513-9. pixelmon minimap 1.16.5

"WebDec 7, 2024 · Selinexor for use in children with cancer is also being explored with other novel therapies, including small molecules targeting CDK 4/6 (palbociclib) and Wee1 (AZD1775). In a study focusing on a single pediatric patient-derived cell line from a rare undifferentiated sarcoma, selinexor was effective alone, but combination with palbociclib ... " - Targeting wee1 kinase in cancer

Targeting wee1 kinase in cancer

Combined Targeting of PARG and Wee1 Causes Decreased Cell …

WebApr 3, 2014 · Abstract. Wee1 is a major regulator of mitotic entry. It phosphorylates and inactivates CDC2/ CDK1, and its functional role is considered to be in G2 checkpoint signaling. MK-1775, a potent and selective small molecular inhibitor of Wee1 kinase, has been recently shown to have activity sensitizing to DNA-damaging agents and … WebJun 8, 2024 · Loss of G1 checkpoint control is common in cancer through TP53, ATM mutations, Rb loss or cyclin E overexpression, providing a stronger rationale for targeting the S/G2 checkpoints. This review will focus on the ATM-CHK2-p53-p21 pathway and the ATR-CHK1-WEE1 pathway and ongoing efforts to target these pathways for patient benefit.

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WebFeb 17, 2024 · Frontiers Targeting the DNA Damage Response for Cancer Therapy by Inhibiting the Kinase Wee1 Cancer cells typically heavily rely on the G2/M checkpoint to survive endogenous and exogenous DNA damage, such as genotoxic stress due to genome instability or radiation and chemotherapy. WebAug 14, 2024 · Wee1 is a protein kinase that regulates the G 2 checkpoint and prevents entry into mitosis in response to DNA damage. Cyclin-dependent kinases (CDK) are a family of …

WebJul 5, 2011 · WEE1 kinase, as gatekeeper of the G 2-checkpoint arrest, holds potential as a therapeutic target to manipulate entry into mitosis of cancer cells. Compelling preclinical … WebApr 4, 2024 · Results: Through the large-scale unbiased combination screening of -1,400 kinase inhibitors, we identified a WEE1 inhibitor (AZD1775), a G2/M checkpoint abrogator in clinical-stage development, as ...

WebOct 1, 2016 · There are few WEE1 inhibitors and there is scope to improve WEE1 inhibitor selectivity and the properties of the inhibitors to permit targeting of specific cancer types. … WebFeb 19, 2024 · The human genome encodes 538 protein kinases that transfer a γ-phosphate group from ATP to serine, threonine, or tyrosine residues. Many of these kinases are …

WebFeb 17, 2024 · As most cancer therapies aim to induce lethal amounts of DNA damage in cancer cells, Wee1 overexpression promotes cancer cell survival (and resistance) by …

WebSep 1, 2010 · Wee1 is a cell cycle kinase, which has recently emerged as a cancer target. [1][2] [3] Wee1 controls cell cycle transitions by inactivating the mitosis-specific … banjir pantai timur 2022WebJan 1, 2024 · Targeting WEE1 as a cancer therapy. Recent studies have shown that WEE1 inhibition can overcome chemotherapy resistance in the treatment of cancer cells [130], … pixelmon mcpeWebJul 1, 2011 · WEE1 kinase is a key molecule in maintaining G₂-cell-cycle checkpoint arrest for premitotic DNA repair. Whereas normal cells repair damaged DNA during G₁-arrest, cancer cells often have a deficient G₁-arrest and largely depend on G₂-arrest. The molecular switch for the G₂-M transition is held by WEE1 and is pushed forward by CDC25. banjir pati hari iniWebNov 15, 2024 · WEE1 has emerged as an attractive target in epithelial ovarian cancer (EOC), but how EOC cells may alter their sensitivity to WEE1 inhibition remains unclear. banjir pasuruanWebMar 1, 2024 · (b) Reactivation of the HR pathway in tumors with acquired resistance to PARP inhibitors might be counteracted by various tyrosine kinase inhibitors (such as VEGF-targeted therapies) or agents targeting epigenetic regulators of HR-related genes (such as BET domain inhibitors). (c) Cancer cells depend on replication stress response for survival. pixelmon minimap modWebJun 25, 2024 · In our research, we found that WEE1 inhibitor (AZD1775) as single agent showed anti-tumor effects in PC cells, however, targeting WEE1 upregulated p-ATM level. Here, we observed that co-targeting of WEE1 and ATM acted synergistically to reduce cell proliferation and migration, and to induce DNA damage in vitro. pixelmon miloticWebSep 21, 2024 · The WEE1 kinase family consists of three serine/threonine kinases sharing conserved molecular structures and encoded by the following genes: WEE1 (WEE1 G2 … pixelmon mew