Grottelli, Silvia; Annunziato, Giannamaria; Pampalone, Gioena; Pieroni, Marco; Dindo, Mirco; Ferlenghi, Francesca; Costantino, Gabriele; Cellini, Barbara published an article in Journal of Medicinal Chemistry. The title of the article was 《Identification of Human Alanine-Glyoxylate Aminotransferase Ligands as Pharmacological Chaperones for Variants Associated with Primary Hyperoxaluria Type 1》.COA of Formula: C12H18N2O The author mentioned the following in the article:
Primary hyperoxaluria type I (PH1) is a rare kidney disease due to the deficit of alanine:glyoxylate aminotransferase (AGT), a pyridoxal-5′-phosphate-dependent enzyme responsible for liver glyoxylate detoxification, which in turn prevents oxalate formation and precipitation as kidney stones. Many PH1-associated missense mutations cause AGT misfolding. Therefore, the use of pharmacol. chaperones (PCs), small mols. that promote correct folding, represents a useful therapeutic option. To identify ligands acting as PCs for AGT, we first performed a small screening of com. available compounds We tested each mol. by a dual approach aimed at defining the inhibition potency on purified proteins and the chaperone activity in cells expressing a misfolded variant associated with PH1. We then performed a chem. optimization campaign and tested the resulting synthetic mols. using the same approach. Overall, the results allowed us to identify a promising hit compound for AGT and draw conclusions about the requirements for optimal PC activity. In the experimental materials used by the author, we found (3-(4-Methylpiperazin-1-yl)phenyl)methanol(cas: 123987-13-3COA of Formula: C12H18N2O)
(3-(4-Methylpiperazin-1-yl)phenyl)methanol(cas: 123987-13-3) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.COA of Formula: C12H18N2O
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics