Thermodynamic Dissection of Potency and Selectivity of Cytosolic Hsp90 Inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01715
Abstract: The cytosolic Hsp90-selective inhibitor TAS-116 has an acceptable safety profile and promising antitumor activity in clinical trials. We examined the binding characteristics of TAS-116 and its analogs to determine the impact of the ligand binding… read more here.
Keywords: potency selectivity; hsp90; cytosolic hsp90; selectivity cytosolic ... See more keywords
First-in-human phase I study of an oral HSP90 inhibitor, TAS-116, in advanced solid tumors.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2017.35.15_suppl.2546
Abstract: 2546Background: TAS-116 is an oral non-ansamycin, non-purine, and non-resorcinol highly selective inhibitor of HSP90α/β. The objective of this FIH study was to determine the MTD and investigate the safety, tolerability, PK, PD (HSP70 protein levels… read more here.
Keywords: advanced solid; solid tumors; study; mtd ... See more keywords
Optimizing antidotal treatment with the oral HSP90 inhibitor TAS-116 against hydrochloric acid-induced pulmonary fibrosis in mice
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Pharmacology"
DOI: 10.3389/fphar.2022.1034464
Abstract: Exposure to high concentrations of hydrochloric acid (HCl) can lead to severe acute and chronic lung injury. In the aftermath of accidental spills, victims may be treated for the acute symptoms, but the chronic injury… read more here.
Keywords: hcl; lung injury; hydrochloric acid; tas 116 ... See more keywords