ATM/ATR

AZ32 Reverses ABCG2-Mediated Multidrug Resistance in Colorectal Cancer

43 views | Dec 22 2023

The study established that the ATM kinase inhibitor AZ32 effectively sensitizes ABCG2-overexpressing colorectal cancer cells to chemotherapeutic drugs, such as mitoxantrone and doxorubicin, by retaining them inside cells, thus demonstrating its potential to reverse ABCG2-mediated multidrug resistance. [Read the Full Post]

Synthesis, Anticancer, Antimicrobial and Antioxidant Potential of Novel 4-(Substituted phenyl-1,3,4-oxadiazol/thiadiazol-2-yl)-4-(4-substituted phenyl) Azetidin-2-One Derivatives

22 views | Oct 16 2023

The synthesized 4-substitutedphenyl-1,3,4-oxadiazol/Thiadiazol-2-yl)-4-(4-substitutedphenyl) azetidin-2-one derivatives demonstrated high efficacy against MCF-7 cancer cell lines, significant antimicrobial potential, and potent antioxidant activity, suggesting their potential for further research and development as therapeutic agents. [Read the Full Post]

Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy

100 views | Sep 17 2023

VX-970 (berzosertib or M6620) is a promising small-molecule ATR inhibitor that shows potential as an effective anticancer drug, both as monotherapy and in combination with chemotherapy or radiotherapy strategies, based on preclinical data and ongoing phase I/II clinical trials. [Read the Full Post]

Selective inhibition of ATM-dependent double-strand break repair and checkpoint control synergistically enhances the efficacy of ATR inhibitors

99 views | Sep 17 2023

Inhibition of ATR kinase and simultaneous suppression of ATM kinase synergistically enhance cancer cell death and show promise as a novel combination approach for cancer therapy. [Read the Full Post]

Nuclear pCHK1 as a potential biomarker of increased sensitivity to ATR inhibition

53 views | Aug 19 2023

The study suggests that the nuclear-specific enrichment of checkpoint kinase 1 (CHK1) and higher levels of nuclear phosphorylated CHK1 (pCHK1) staining may serve as potential predictive biomarkers for sensitivity to the ATR inhibitor elimusertib in cancer cells. [Read the Full Post]

Preclinical validation of a novel therapeutic strategy for choroid plexus carcinoma

104 views | Aug 19 2023

This study represents a pioneering effort in identifying promising combinatorial therapeutics and highlighting the potential of intra-arterial delivery for the treatment of choroid plexus carcinoma, a rare and aggressive brain tumor in children. [Read the Full Post]

The effect of the ATM inhibitor AZD0156 on the radiosensitivity of human breast cancer and lung fibroblast cells

57 views | Jul 31 2023

The combination of irradiation and AZD0156 showed enhanced efficacy in inducing cell cycle arrest and reducing clonogenic survival in breast cancer cells, while having minimal effect on fibroblast cells. [Read the Full Post]

Dynamic of centromere associated RNAs and the centromere loading of DNA repair proteins in growing oocytes

50 views | Jul 17 2023

This study demonstrates that centromere transcription in growing oocytes, associated with DNA repair proteins, plays a role in maintaining centromere stability and kinetochore assembly, providing insights into the accurate segregation of chromosomes during oocyte maturation. [Read the Full Post]

Combination ATR (ceralasertib) and PARP (olaparib) Inhibitor (CAPRI) trial in acquired PARP-inhibitor-resistant homologous recombination deficient ovarian cancer

93 views | Jun 23 2023

The combination of olaparib and ceralasertib shows promising activity and tolerability in patients with acquired PARPi-resistant high-grade serous ovarian cancer, suggesting the potential of ATRi to overcome PARPi resistance in this population. [Read the Full Post]

Combining radiation and the ATR inhibitor berzosertib activates STING signaling and enhances immunotherapy via inhibiting SHP1 function in colorectal cancer

24 views | May 22 2023

This study found that combining ATR inhibitors, irradiation, and anti-PD-L1 therapy improved the efficacy of immunotherapy in colorectal cancer mouse models by promoting STING signaling and reinvigorating the tumor microenvironment. [Read the Full Post]