3). The nitrile moiety has been used in approved drugs such as nirmatrelvir where it was designed to form a reversible covalent bond with Cys145 of SARS-CoV-2 Metalloprotease [54]. Cyano-acrylamides were first popularised by the Taunton group in their work targeting protein kinases [55],...
Where Does the Cytoplasmic Homodimeric DNA-binding Competent STAT3 Complex (“SIF-A”) Elute Off Superose-6 FPLC? In order to detect DNA-binding competent STAT3 in the cytosolic compartment, we carried out electrophoretic mobility shift assays (EMSA) using the mutant serum-inducible element (SIE)...
ATP-binding cassette G1 Apo: Apolipoprotein ARF-1: ADP ribosylation factor 1 CETP: Cholesteryl ester transfer protein ChREBP: Carbohydrate responsive element-binding protein ER: Endoplasmic reticulum FOXO1: Forkhead box protein O1 HMG-CoA: 3-Hydroxy-3-methylglutaryl coenzyme A LCAT: Leci...
This article is based on previously conducted studies and does not contain any studies with human participants or animals performed by any of the authors. The IL-1 Family Understanding the role of IL-1 in the pathogenesis of disease has improved greatly since the publication of “Biologic Basis...
However, due to the off-target activity of these compounds (likely associated with binding to other kinases), toxicity, and/or poor bioavailability, these compounds have proven less useful for determining the functional implications of IRE1 signaling in the context of complex cellular and in vivo ...
ATP/Hyals dually responsive core-shell hyaluronan/chitosan-based drug nanocarrier for potential application in breast cancer therapy. Int. J. Biol. Macromol. 2021, 183, 839–851. [Google Scholar] [CrossRef] Yang, J.; Zhao, R.; Feng, Q.; Zhuo, X.; Wang, R. Development of a carrier ...
The compound binds the ATP pocket of MET kinase in a DFG-in conformation, forming classical hydrogen bonds (Hb) with hinge region residues [99]; in addition, its phenyl ring forms a π-π interaction with the activation loop (A-loop). Ironically, the drug was found to have off-target ...