Results 41 to 50 of about 677,925 (163)

Overcoming PARP Inhibitor and Platinum Resistance with WEE1 Inhibitors in Ovarian Cancer [PDF]

healthbook TIMES Oncology Hematology, 2021
Poly (ADP-ribose) polymerase inhibitors (PARPi) have transformed the treatment of high-grade epithelial ovarian cancer (EOC), with demonstrated efficacy in the recurrent as well as newly diagnosed disease. However, women with EOC inevitably acquire resistance to both platinum chemotherapy and PARPi.
openaire   +2 more sources

Combined Inhibition of ATR and WEE1 as a Novel Therapeutic Strategy in Triple-Negative Breast Cancer

Neoplasia: An International Journal for Oncology Research, 2018
Triple negative breast cancer (TNBC) is a highly aggressive subtype of breast cancer that poses a clinical challenge. Thus, new therapy strategies are urgently needed.
Juan Jin, Hehui Fang, Fang Yang, Wenfei Ji, Nan Guan, Zijia Sun, Yaqin Shi, Guohua Zhou, Xiaoxiang Guan   +8 more
doaj   +1 more source

Targeting WEE1 kinase as a p53-independent therapeutic strategy in high-risk and relapsed acute lymphoblastic leukemia

Cancer Cell International, 2023
Background Outcomes for patients with relapsed acute lymphoblastic leukemia (ALL) are poor and there is a need for novel therapies to improve outcomes.
Hayden L. Bell, Helen J. Blair, Mankaran Singh, Anthony V. Moorman, Olaf Heidenreich, Frederik W. van Delft, John Lunec, Julie A. E. Irving   +7 more
doaj   +1 more source

Cell cycle regulation by the Wee1 Inhibitor PD0166285, Pyrido [2,3-d] pyimidine, in the B16 mouse melanoma cell line

BMC Cancer, 2006
Background Wee1 kinase plays a critical role in maintaining G2 arrest through its inhibitory phosphorylation of cdc2. In previous reports, a pyridopyrimidine molecule PD0166285 was identified to inhibit Wee1 activity at nanomolar concentrations.
Sakamoto Masaharu, Selvendiran Karuppaiyah, Nakamura Toru, Torimura Takuji, Shinkawa Masako, Hashimoto Osamu, Koga Hironori, Ueno Takato, Sata Michio   +8 more
doaj   +1 more source

Discovery of potential WEE1 inhibitors via hybrid virtual screening

Frontiers in Pharmacology, 2023
G2/M cell cycle checkpoint protein WEE1 kinase is a promising target for inhibiting tumor growth. Although various WEE1 inhibitors have entered clinical investigations, their therapeutic efficacy and safety profile remain unsatisfactory. In this study, we employed a comprehensive virtual screening workflow, which included Schrödinger-Glide molecular ...
Tingting Jin, Wei Xu, Roufen Chen, Liteng Shen, Jian Gao, Lei Xu, Xinglong Chi, Nengming Lin, Lixin Zhou, Zheyuan Shen, Bo Zhang   +10 more
openaire   +3 more sources

Tracking CDK1 Dynamics With a Novel Biosensor Mouse and Clinical Cohorts to Predict CDK4/6 Inhibitor Sensitivity in ER+ Breast Cancer

Advanced Science, EarlyView.
Cyclin‐dependent kinase (CDK) 1 activity is a dynamic marker of treatment response in estrogen receptor positive breast cancer. Patient cohorts reveal CDK1 activity increases during progression to invasive disease, where high expression correlates with poor survival. Using a novel Cdk1 biosensor mouse alongside in vitro models, we demonstrate that CDK1
Sarah Alexandrou, Kristine J. Fernandez, Min Li Huang, Ewan K. A. Millar, Claire Vennin, Leila Eshraghi, Tan Dat Timothy Lam, Victoria Lee, Nyah C. Brooks, Janett Stoehr, Cristian Guaman Mendez, Douglas Strathdee, David Stevenson, David Herrmann, Sandra O'Toole, Paul Timpson, Max Nobis, C. Elizabeth Caldon   +17 more
wiley   +1 more source

Gauchos and ochos: a Wee1-Cdk tango regulating mitotic entry

Cell Division, 2010
The kinase Wee1 has been recognized for a quarter century as a key inhibitor of Cyclin dependent kinase 1 (Cdk1) and mitotic entry in eukaryotes. Nonetheless, Wee1 regulation is not well understood and its large amino-terminal regulatory domain (NRD) has
Enders Greg H
doaj   +1 more source

BRCA1 Mutation‐Recognizing Tetrahedral Framework Nucleic Acid Nanoplatform Enables Coordinated PARP/WEE1 Inhibition and STING‐Associated Antitumor Immunity in Ovarian Cancer

Advanced Science, EarlyView.
BRCA1 mutation‐responsive FBOA‐tFNA selectively recognizes mutant transcripts and coordinates reduction‐responsive intracellular delivery of olaparib and adavosertib, amplifying DNA damage and weakening G2/M checkpoint protection. These effects are accompanied by STING‐associated immune activation and stronger antitumor immunity, while sequential anti ...
Chenyi Wang, Mengying Yao, Jinhui Xie, Dingjie Wang, Yashi Shi, Xiaodan Mao, Chunhua Lu, Pengming Sun   +7 more
wiley   +1 more source

Targeting WEE1 in ARID1A/TP53 Concurrent Mutant Colorectal Cancer by Exploiting R‐Loop Accumulation and DNA Repair Deficiencies

Advanced Science
ARID1A, a component of the SWI/SNF tumor suppressor complex, is frequently mutated in colorectal cancers (CRC). Here, it is found that CRC with ARID1A/TP53 concurrent mutations is highly sensitive to WEE1 inhibitors.
Chi Zhang, Yanjing Zhu, Luoyan Ai, Jingyuan Wang, Shan Yu, Yichen Wang, Xiaojing Xu, Mengling Liu, Yiyi Yu, Mengxuan Zhu, Yutong Liu, Zhenghang Xu, Haojie Zhou, Huishan Li, Qihong Huang, Qing Liu, Ke Peng, Tianshu Liu   +17 more
doaj   +1 more source

Myt1 overexpression mediates resistance to cell cycle and DNA damage checkpoint kinase inhibitors

Frontiers in Cell and Developmental Biology, 2023
Cell cycle checkpoint kinases serve as important therapeutic targets for various cancers. When they are inhibited by small molecules, checkpoint abrogation can induce cell death or further sensitize cancer cells to other genotoxic therapies. Particularly
Sargun Sokhi, Sargun Sokhi, Sargun Sokhi, Cody W. Lewis, Cody W. Lewis, Cody W. Lewis, Amirali B. Bukhari, Amirali B. Bukhari, Amirali B. Bukhari, Joanne Hadfield, Joanne Hadfield, Joanne Hadfield, Edric J. Xiao, Edric J. Xiao, Edric J. Xiao, Jeremy Fung, Jeremy Fung, Yea Jin Yoon, Yea Jin Yoon, Wen-Hsin Hsu, Wen-Hsin Hsu, Wen-Hsin Hsu, Armin M. Gamper, Armin M. Gamper, Armin M. Gamper, Gordon K. Chan, Gordon K. Chan, Gordon K. Chan   +27 more
doaj   +1 more source