Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors:
The Identification of an Inhibitor Selective for LOXL2 over LOX
John H. Hutchinson
Martin W. Rowbottom
David Lonergan
Janice Darlington
Pat Prodanovich
Christopher D. King
Jilly F. Evans
Gretchen Bain
10.1021/acsmedchemlett.7b00014.s001
https://acs.figshare.com/articles/journal_contribution/Small_Molecule_Lysyl_Oxidase-like_2_LOXL2_Inhibitors_The_Identification_of_an_Inhibitor_Selective_for_LOXL2_over_LOX/4728520
Two series of novel
LOXL2 enzyme inhibitors are described: benzylamines
substituted with electron withdrawing groups at the <i>para</i>-position and 2-substituted pyridine-4-ylmethanamines. The most potent
compound, (2-chloropyridin-4-yl)methanamine <b>20</b> (hLOXL2
IC<sub>50</sub> = 126 nM), was shown to be selective for LOXL2 over
LOX and three other amine oxidases (MAO-A, MAO-B, and SSAO). Compound <b>20</b> is the first published small molecule inhibitor selective
for LOXL2 over LOX.
2017-03-01 00:00:00
MAO-A
hLOXL 2 IC 50
novel LOXL 2 enzyme inhibitors
Small Molecule Lysyl Oxidase-like 2
Inhibitor
MAO-B
LOXL 2
SSAO