2. Academic Validation
  3. Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX

Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX

  • ACS Med Chem Lett. 2017 Mar 1;8(4):423-427. doi: 10.1021/acsmedchemlett.7b00014.
John H Hutchinson 1,  Martin W Rowbottom 1,  David Lonergan 1,  Janice Darlington 1,  Pat Prodanovich 1,  Christopher D King 1,  Jilly F Evans 1,  Gretchen Bain 1
Affiliations

Affiliation

  • 1 PharmAkea Inc., 3030 Bunker Hill Street, Suite 300, San Diego, California 92109, United States.
PMID: 28435530 DOI: 10.1021/acsmedchemlett.7b00014
Abstract

Two series of novel LOXL2 Enzyme inhibitors are described: benzylamines substituted with electron withdrawing groups at the para-position and 2-substituted pyridine-4-ylmethanamines. The most potent compound, (2-chloropyridin-4-yl)methanamine 20 (hLOXL2 IC50 = 126 nM), was shown to be selective for LOXL2 over LOX and three other amine oxidases (MAO-A, MAO-B, and SSAO). Compound 20 is the first published small molecule inhibitor selective for LOXL2 over LOX.

Keywords

(2-chloropyridin-4-yl)methanamine; LOXL2; fibrosis; inhibitor; lysyl oxidase-like 2.

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