Synthetic Route of 432-21-3, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 432-21-3, Name is 2-Amino-6-chlorobenzotrifluoride, SMILES is NC1=CC=CC(Cl)=C1C(F)(F)F, belongs to chlorides-buliding-blocks compound. In a article, author is Dougherty, Patrick G., introduce new discover of the category.
Cyclic Peptidyl Inhibitors against CAL/CFTR Interaction for Treatment of Cystic Fibrosis
Cystic fibrosis (CF) is caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene, encoding for a chloride ion channel. Membrane expression of CFTR is negatively regulated by CFTR-associated ligand (CAL). We previously showed that inhibition of the CFTR/CAL interaction with a cell-permeable peptide improves the function of rescued F508del-CFTR. In this study, optimization of the peptidyl inhibitor yielded PGD97, which exhibits a K-D value of 6 nM for the CAL PDZ domain, >= 130-fold selectivity over closely related PDZ domains, and a serum t(1/2) of >24 h. In patient-derived F508del homozygous cells, PGD97 (100 nM) increased short-circuit currents by similar to 3-fold and further potentiated the therapeutic effects of small-molecule correctors (e.g., VX-661) by similar to 2-fold (with an EC50 of similar to 10 nM). Our results suggest that PGD97 may be used as a novel treatment for CF, either as a single agent or in combination with small-molecule correctors/potentiators.
Synthetic Route of 432-21-3, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 432-21-3 is helpful to your research.