Bruno, Claudio published the artcileThe chemosensitizing agent lubeluzole binds calmodulin and inhibits Ca2+/calmodulin-dependent kinase II, SDS of cas: 140-28-3, the publication is European Journal of Medicinal Chemistry (2016), 36-45, database is CAplus and MEDLINE.
An affinity capillary electrophoresis (ACE) method to estimate apparent dissociation constants between bovine brain calmodulin (CaM) and nonpeptidic ligands was developed. The method was validated reproducing the dissociation constants of a number of well-known CaM ligands. In particular, the potent antagonist 125-C9 was ad hoc synthesized through an improved synthetic procedure. The ACE method was successfully applied to verify CaM affinity for lubeluzole, a well-known neuroprotective agent recently proved useful to potentiate the activity of anticancer drugs. Lubeluzole was slightly less potent than 125-C9 (Kd = 2.9¡À0.7 and 0.47¡À0.06 ¦ÌM, resp.) and displayed Ca2+/calmodulin-dependent kinase II (CaMKII) inhibition (IC50 = 40¡À1 ¦ÌM). Possible binding modes of lubeluzole to CaM were explored by docking studies based on the x-ray crystal structures of several trifluoperazine-CaM complexes. An estimated dissociation constant in good agreement with the exptl. one was found and the main aminoacidic residues and interactions contributing to complex formation were highlighted. The possibility that interference with Ca2+ pathways may contribute to the previously observed chemosensitizing effects of lubeluzole on human ovarian adenocarcinoma and lung carcinoma cells are discussed.
European Journal of Medicinal Chemistry published new progress about 140-28-3. 140-28-3 belongs to catalysis-chemistry, auxiliary class Benzenes, name is N1,N2-Dibenzylethane-1,2-diamine, and the molecular formula is C16H20N2, SDS of cas: 140-28-3.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia