CEP131 Abrogates CHK1 Inhibitor-Induced Replication Defects and Is Associated with Unfavorable Outcome in Neuroblastoma

18 views | Mar 25 2021

Kiyohiro Ando et al. revealed that MDM2 was associated with CEP131 protein degradation, whereas overexpression of CEP131 accelerated neuroblastoma cell growth and exhibited resistance to CHK1i-induced replication defects. [Read the Full Post]

The phosphorylation of CHK1 at Ser345 regulates the phenotypic switching of vascular smooth muscle cells both in vitro and in vivo

28 views | Dec 25 2020

Chen Xin et al. demonstrated that phosphorylation of CHK1 under DNA damage stress modulated VSMCs phenotypic switching. [Read the Full Post]

Crystal Structure of the Kinase Domain of MerTK in Complex with AZD7762 Provides Clues for Structure-Based Drug Development

31 views | Dec 23 2020

Tae Hyun Park et al. determined the crystal structure of the MerTK:AZD7762 complex and revealed the binding mode of AZD7762 to MerTK. [Read the Full Post]

Resistance to the CHK1 inhibitor prexasertib involves functionally distinct CHK1 activities in BRCA wild-type ovarian cancer

40 views | Nov 29 2020

Jayakumar Nair et al. demonstrated new mechanistic insights of functionally distinct CHK1 activities and highlighted a potential combination treatment approach to overcome CHK1i resistance in BRCAwt HGSOC. [Read the Full Post]

Phosphoproteomics Analysis Reveals a Potential Role of CHK1 in Regulation of Innate Immunity through IRF3

42 views | Nov 09 2020

Zhen Chen et al. indicated that the CHK1-dependent regulation of IRF3 phosphorylation at S173 and S175 might play a role in the induction of innate immune response after replication stress or DNA damage, which suggested a potential function of CHK1 in the innate immune response. [Read the Full Post]

The CHK1 inhibitor MU380 significantly increases the sensitivity of human docetaxel-resistant prostate cancer cells to gemcitabine through the induction of mitotic catastrophe

37 views | Nov 09 2020

Stanislav Drápela et al. suggested that metabolically robust and selective CHK1 inhibitor MU380 could bypass docetaxel resistance and improve the effectiveness of GEM in DR mCRPC models. [Read the Full Post]

Radiosensitization by Kinase Inhibition Revealed by Phosphoproteomic Analysis of Pancreatic Cancer Cells

43 views | Oct 16 2020

Svenja Wiechmann et al.improved the understanding of radioresistance and provided avenues for developing radiotherapeutic strategies. [Read the Full Post]

A phase II study to evaluate LY2603618 in combination with gemcitabine in pancreatic cancer patients

130 views | Apr 13 2020

Laquente B et al. showed that LY2603618/gemcitabine was not superior to gemcitabine for the treatment of patients with pancreatic cancer. [Read the Full Post]

Effects of a checkpoint kinase inhibitor, AZD7762, on tumor suppression and bone remodeling

131 views | Apr 12 2020

Wang L et al. indicated that in addition to acting as a tumor suppressor, AZD7762 may prevent bone loss by inhibiting osteoclastogenesis and stimulating osteoblast mineralization. [Read the Full Post]

CHK1 Inhibition in Small-Cell Lung Cancer Produces Single-Agent Activity in Biomarker-Defined Disease Subsets and Combination Activity with Cisplatin or Olaparib

132 views | Apr 07 2020

Sen T et al. provided a preclinical proof of concept supporting the initiation of a clinical efficacy trial in patients with platinum-sensitive or platinum-resistant relapsed SCLC. [Read the Full Post]