Brousseau, Margaret E. published the artcileIdentification of a PCSK9-LDLR disruptor peptide with in vivo function, COA of Formula: C25H23NO4, the publication is Cell Chemical Biology (2022), 29(2), 249-258.e5, database is CAplus and MEDLINE.
Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates plasma low-d. lipoprotein cholesterol (LDL-C) levels by promoting hepatic LDL receptor (LDLR) degradation Therapeutic antibodies that disrupt PCSK9-LDLR binding reduce LDL-C concentrations and cardiovascular disease risk. The epidermal growth factor precursor homol. domain A (EGF-A) of the LDLR serves as a primary contact with PCSK9 via a flat interface, presenting a challenge for identifying small mol. PCSK9-LDLR disruptors. We employ an affinity-based screen of 1013in vitro-translated macrocyclic peptides to identify high-affinity PCSK9 ligands that utilize a unique, induced-fit pocket and partially disrupt the PCSK9-LDLR interaction. Structure-based design led to mols. with enhanced function and pharmacokinetic properties (e.g., 13PCSK9i). In mice, 13PCSK9i reduces plasma cholesterol levels and increases hepatic LDLR d. in a dose-dependent manner. 13PCSK9i functions by a unique, allosteric mechanism and is the smallest mol. identified to date with in vivo PCSK9-LDLR disruptor function.
Cell Chemical Biology published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C25H23NO4, COA of Formula: C25H23NO4.
Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem