[HTML][HTML] Development and characterization of a Wee1 kinase degrader

Z Li, BJ Pinch, CM Olson, KA Donovan, RP Nowak… - Cell chemical …, 2020 - cell.com
The G1/S cell cycle checkpoint is frequently dysregulated in cancer, leaving cancer cells
reliant on a functional G2/M checkpoint to prevent excessive DNA damage. Wee1 regulates …

[HTML][HTML] Selective Wee1 degradation by PROTAC degraders recruiting VHL and CRBN E3 ubiquitin ligases

MC Aublette, TA Harrison, EJ Thorpe… - Bioorganic & Medicinal …, 2022 - Elsevier
Abstract The Ser/Thr protein kinase Wee1 plays a regulatory role at the G 2/M checkpoint by
phosphorylating CDK1 when DNA is damaged to allow time for DNA to repair, disruption of …

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 …

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 …

Wee1 kinase as a target for cancer therapy

K Do, JH Doroshow, S Kummar - Cell cycle, 2013 - Taylor & Francis
Wee1, a protein kinase, regulates the G2 checkpoint in response to DNA damage.
Preclinical studies have elucidated the role of wee1 in DNA damage repair and the …

Molecular pathways: targeting the protein kinase Wee1 in cancer

JJJ Geenen, JHM Schellens - Clinical Cancer Research, 2017 - AACR
Wee1 is a protein kinase that regulates the G2 checkpoint and prevents entry into mitosis in
response to DNA damage. Cyclin-dependent kinases (CDK) are a family of 14 …

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 …

Synthetic and medicinal chemistry approaches toward WEE1 kinase inhibitors and its degraders

VJ Alli, P Yadav, V Suresh, SS Jadav - ACS omega, 2023 - ACS Publications
WEE1 is a checkpoint kinase critical for mitotic events, especially in cell maturation and DNA
repair. Most cancer cells' progression and survival are linked with elevated levels of WEE1 …

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 …