Results 11 to 20 of about 1,652 (181)

Preclinical evaluation of the antitumoral efficacy of Wee1 inhibitor AZD1775 in adrenocortical carcinoma

Pharmacological Research
Current therapy for advanced adrenocortical carcinoma (ACC) is represented by EDP-M (etoposide, doxorubicin, cisplatin + mitotane), but its efficacy is limited and new approaches are needed.
Emma Nozza, Emanuela Esposito, Genesio Di Muro, Sonia Di Bari, Rosa Catalano, Gianluca Lopez, Valentina Vaira, Anna Maria Barbieri, Giusy Marra, Federica Mangili, Donatella Treppiedi, Michele Battistin, Guido Di Dalmazi, Serena Palmieri, Emanuele Ferrante, Giovanna Mantovani, Erika Peverelli   +16 more
doaj   +6 more sources

Wee1 Rather Than Plk1 Is Inhibited by AZD1775 at Therapeutically Relevant Concentrations [PDF]

Cancers, 2019
Wee1 kinase is an inhibitor of cyclin-dependent kinase (cdk)s, crucial cell cycle progression drivers. By phosphorylating cdk1 at tyrosine 15, Wee1 inhibits activation of cyclin B-cdk1 (Cdk1), preventing cells from entering mitosis with incompletely replicated or damaged DNA.
Serpico A. F., D'alterio G., Vetrei C., Monica R. D., Nardella L., Visconti R., Grieco D.   +6 more
core   +6 more sources

AZD1775 MS Supplementary Materials from Quantitative and Mechanistic Understanding of AZD1775 Penetration across Human Blood–Brain Barrier in Glioblastoma Patients Using an IVIVE–PBPK Modeling Approach

, 2023
<p>SUPPLEMENTARY METHODS Supplementary Figure 1 Overall metabolic kinetics of AZD1775 in human liver and intestinal microsomes (HLM and HIM). Supplementary Figure 2 PBPK model simulations showing the impact of BBB integrity (i.e., PSB), transporter activity (i.e., CLefflux,vivo and CLuptake,vivo), and drug binding to brain tissues (i.e., fu,br ...
Nader Sanai, Alex Sparreboom, Seongho Kim, Youming Xie, Norissa Honea, Xun Bao, Jianmei Wu, Jing Li   +7 more
openaire   +2 more sources

Genetic determinants of response to the WEE1 inhibitor AZD1775 in ovarian cancer [PDF]

High-grade serous ovarian carcinoma (HGSOC) is an aggressive cancer with a poor prognosis. Clinical studies on the combination of the WEE1-kinase inhibitor AZD1775 and carboplatin have yielded promising results in some HGSOC patients, but not in others.
Roorda, Maurits
openaire   +3 more sources

Figure S2 from Wee1 Kinase Inhibitor AZD1775 Effectively Sensitizes Esophageal Cancer to Radiotherapy

, 2023
<p>Comparable colony numbers between cells with or without AZD1775 treatment suggests 100 nM AZD1775 has minimal cell cytotoxicity on cells. OE33, SK4, FLO1 and KYSE cells were cultured in media containing 100 nM AZD1775 and subjected to clonogenic survival assay. Each dose was prepared in triplicate per experiment, and no less than 2 experiments
Terence M. Williams, Steven H. Lin, Junran Zhang, Eric D. Miller, Andrew J. Hu, Tianyun Li, Cory J. Pettit, Changxian Shen, Linlin Yang   +8 more
openaire   +2 more sources

Figure S5 from Wee1 Kinase Inhibitor AZD1775 Effectively Sensitizes Esophageal Cancer to Radiotherapy

, 2023
<p>AGS TP53 wildtype adenocarcinoma cells were not effectively radiosensitized by the combination of AZD1775 and radiation. DER= dose enhancement ratio.</p>
Terence M. Williams, Steven H. Lin, Junran Zhang, Eric D. Miller, Andrew J. Hu, Tianyun Li, Cory J. Pettit, Changxian Shen, Linlin Yang   +8 more
openaire   +2 more sources

Figure S1 from Wee1 Kinase Inhibitor AZD1775 Effectively Sensitizes Esophageal Cancer to Radiotherapy

, 2023
<p>CDK1 and genes from an AZD1775 responsiveness gene signature are up-regulated in ESCA, particularly squamous cell carcinoma. (A) Analysis of multiple esophageal cancer mRNA expression datasets (Su Esophagus 2 and Hu Esophagus) in Oncomine (http://oncomine.org/) confirms up-regulation of CDK1 in ESCA tumor versus normal tissues.
Terence M. Williams, Steven H. Lin, Junran Zhang, Eric D. Miller, Andrew J. Hu, Tianyun Li, Cory J. Pettit, Changxian Shen, Linlin Yang   +8 more
openaire   +2 more sources

Sequential drug treatment targeting cell cycle and cell fate regulatory programs blocks non-genetic cancer evolution in acute lymphoblastic leukemia [PDF]

Genome Biology
Background Targeted therapies exploiting vulnerabilities of cancer cells hold promise for improving patient outcome and reducing side-effects of chemotherapy. However, efficacy of precision therapies is limited in part because of tumor cell heterogeneity.
Alena Malyukova, Mari Lahnalampi, Ton Falqués-Costa, Petri Pölönen, Mikko Sipola, Juha Mehtonen, Susanna Teppo, Karen Akopyan, Johanna Viiliainen, Olli Lohi, Anna K. Hagström-Andersson, Merja Heinäniemi, Olle Sangfelt   +12 more
doaj   +2 more sources

The Combination of the PARP Inhibitor Olaparib and the WEE1 Inhibitor AZD1775 as a New Therapeutic Option for Small Cell Lung Cancer [PDF]

Clinical Cancer Research, 2018
Abstract Purpose: Introduced in 1987, platinum-based chemotherapy remains standard of care for small cell lung cancer (SCLC), a most aggressive, recalcitrant tumor. Prominent barriers to progress are paucity of tumor tissue to identify drug targets and patient-relevant models to interrogate novel therapies.
Lallo, Alice, Frese, Kristopher K., Morrow, Christopher J., Sloane, Robert, Gulati, Sakshi, Schenk, Maximillian W., Trapani, Francesca, Simms, Nicole, Galvin, Melanie, Brown, Stewart, Hodgkinson, Cassandra L., Priest, Lynsey, Hughes, Adina, Lai, Zhongwu, Cadogan, Elaine, Khandelwal, Garima, Simpson, Kathryn L., Miller, Crispin, Blackhall, Fiona, O'Connor, Mark J., Dive, Caroline   +20 more
openaire   +7 more sources

Abstract 291: Sequential treatment with the Wee1 inhibitor, AZD1775, enhances the effect of trabectedin in the L-sarcomas

Cancer Research, 2017
Abstract Soft tissue sarcomas are heterogeneous mesenchymal neoplasms and account for 1% of all cancers in adults. Over 50 sarcomas subtypes have been classified and many have very limited treatment options. Chemotherapies such as doxorubicin, dacarbazine and gemcitabine have had very low response rates.
Elgilda Musi, Grazia Ambrosini, Gary K. Schwartz   +2 more
openaire   +2 more sources