[HTML][HTML] Inhibiting WEE1 selectively kills histone H3K36me3-deficient cancers by dNTP starvation

SX Pfister, E Markkanen, Y Jiang, S Sarkar… - Cancer cell, 2015 - cell.com
Summary Histone H3K36 trimethylation (H3K36me3) is frequently lost in multiple cancer
types, identifying it as an important therapeutic target. Here we identify a synthetic lethal …

WEE1 kinase limits CDK activities to safeguard DNA replication and mitotic entry

CR Elbæk, V Petrosius, CS Sørensen - Mutation Research/Fundamental …, 2020 - Elsevier
Precise execution of the cell division cycle is vital for all organisms. The Cyclin dependent
kinases (CDKs) are the main cell cycle drivers, however, their activities must be precisely …

MK1775, a selective Wee1 inhibitor, shows single-agent antitumor activity against sarcoma cells

JM Kreahling, JY Gemmer, D Reed, D Letson… - Molecular cancer …, 2012 - AACR
Wee1 is a critical component of the G2–M cell-cycle checkpoint control and mediates cell-
cycle arrest by regulating the phosphorylation of CDC2. Inhibition of Wee1 by a selective …

Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents

H Hirai, Y Iwasawa, M Okada, T Arai, T Nishibata… - Molecular cancer …, 2009 - AACR
Wee1 is a tyrosine kinase that phosphorylates and inactivates CDC2 and is involved in G2
checkpoint signaling. Because p53 is a key regulator in the G1 checkpoint, p53-deficient …

Preclinical evaluation of the WEE1 inhibitor MK-1775 as single-agent anticancer therapy

AD Guertin, J Li, Y Liu, MS Hurd, AG Schuller… - Molecular cancer …, 2013 - AACR
Inhibition of the DNA damage checkpoint kinase WEE1 potentiates genotoxic
chemotherapies by abrogating cell-cycle arrest and proper DNA repair. However, WEE1 is …

Inhibition of Wee1 Sensitizes Cancer Cells to Antimetabolite Chemotherapeutics In Vitro and In Vivo, Independent of p53 Functionality

AA Van Linden, D Baturin, JB Ford, SP Fosmire… - Molecular cancer …, 2013 - AACR
Inhibition of Wee1 is emerging as a novel therapeutic strategy for cancer, and some data
suggest that cells with dysfunctional p53 are more sensitive to Wee1 inhibition combined …

WEE1 kinase targeting combined with DNA-damaging cancer therapy catalyzes mitotic catastrophe

PC De Witt Hamer, SE Mir, D Noske… - Clinical cancer …, 2011 - AACR
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 …

Forced mitotic entry of S-phase cells as a therapeutic strategy induced by inhibition of WEE1

M Aarts, R Sharpe, I Garcia-Murillas, H Gevensleben… - Cancer discovery, 2012 - AACR
Inhibition of the protein kinase WEE1 synergizes with chemotherapy in preclinical models
and WEE1 inhibitors are being explored as potential cancer therapies. Here, we investigate …

Targeting WEE1 kinase in cancer

CJ Matheson, DS Backos, P Reigan - Trends in pharmacological sciences, 2016 - cell.com
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; however, cancer …

Unique functions of CHK1 and WEE1 underlie synergistic anti-tumor activity upon pharmacologic inhibition

AD Guertin, MM Martin, B Roberts, M Hurd, X Qu… - Cancer cell …, 2012 - Springer
Background Inhibition of kinases involved in the DNA damage response sensitizes cells to
genotoxic agents by abrogating checkpoint-induced cell cycle arrest. CHK1 and WEE1 act in …