Inhibition of DNA-PK with AZD7648 Sensitizes Tumor Cells to Radiotherapy and Induces Type I IFN-Dependent Durable Tumor Control

7 views | Jun 22 2021

Kyoko Nakamura et al. found that blocking the NHEJ DNA repair pathway with AZD7648 in combination with RT leaded to durable immune-mediated tumor control. [Read the Full Post]

Partial Rescue of F508del-CFTR Stability and Trafficking Defects by Double Corrector Treatment

7 views | Jun 21 2021

Valeria Capurro et al. thought that it was still possible to further improve mutant CFTR rescue with the development of corrector combinations having maximal effects on mutant CFTR structural and functional properties. [Read the Full Post]

GDI2 is a target of paclitaxel that affects tumorigenesis of prostate cancer via the p75NTR signaling pathway

10 views | May 31 2021

Chi Liu et al. found that knocking down of GDI2 inhibited cell proliferation and promoted cell apoptosis via the p75NTR signaling pathway in prostate cancer. [Read the Full Post]

Transcriptomic analysis of CFTR-impaired endothelial cells reveals a pro-inflammatory phenotype

28 views | Feb 01 2021

Mathias Declercq et al. thought that normalisation of vascular inflammation might be a novel therapeutic strategy to ameliorate the disease severity of CF. [Read the Full Post]

Real-World Safety of CFTR Modulators in the Treatment of Cystic Fibrosis: A Systematic Review

31 views | Jan 05 2021

Renée V E Dagenais et al. thought that pharmacists played a key role in the safe initiation and monitoring of people with CF on CFTR modulator therapies. [Read the Full Post]

An integrated drug repurposing strategy for the rapid identification of potential SARS-CoV-2 viral inhibitors

54 views | Sep 01 2020

Alfonso Trezza et al. showed that Simeprevir and Lumacaftor bound the receptor-binding domain of the Spike protein with high affinity and prevented ACE2 interaction. [Read the Full Post]

The impact of ivacaftor on sinonasal pathology in S1251N-mediated cystic fibrosis patients

107 views | Jul 21 2020

Romee Gostelie et al. found that Ivacaftor appeared to improve sinonasal outcome parameters and thereby sinonasal health in patients with cystic fibrosis with an S1251N mutation. [Read the Full Post]

Corrector VX-809 promotes interactions between cytoplasmic loop one and the first nucleotide-binding domain of CFTR

179 views | Nov 12 2019

Loo TW et al. suggested that the mechanism by which VX-809 promotes maturation and stability of CFTR is by promoting CL1/NBD1 interactions. [Read the Full Post]

Some gating potentiators, including VX-770, diminish ΔF508-CFTR functional expression

355 views | Sep 29 2019

Veit G et al. indicated that VX-770 diminished the folding efficiency and the metabolic stability of ΔF508-CFTR at the endoplasmic reticulum (ER) and post-ER compartments, respectively, causing reduced cell surface ΔF508-CFTR density and function. VX-770-induced destabilization of ΔF508-CFTR was influenced by second-site suppressor mutations of the folding defect and was prevented by stabilization of the nucleotide-binding domain 1 (NBD1)-NBD2 interface. The reduced correction efficiency of ΔF508-CFTR, as well as of two other processing mutations in the presence of VX-770, suggests the need for further optimization of potentiators to maximize the clinical benefit of corrector-potentiator combination therapy in CF. [Read the Full Post]

Effect of VX-770 in persons with cystic fibrosis and the G551D-CFTR mutation

339 views | Jan 18 2019

Accurso FJ et al. evaluated the safety and adverse-event profile of VX-770 showed that VX-770 was associated with within-subject improvements in CFTR and lung function. These findings provide support for further studies of pharmacologic potentiation of CFTR as a means to treat cystic fibrosis. [Read the Full Post]