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

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.

SUBMITTER: Hutchinson JH

PROVIDER: S-EPMC5392766 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature

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

Hutchinson John H JH Rowbottom Martin W MW Lonergan David D Darlington Janice J Prodanovich Pat P King Christopher D CD Evans Jilly F JF Bain Gretchen G

ACS medicinal chemistry letters 20170301 4

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. ...[more]

PMID: 28435530

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Targeting lysyl oxidase (LOX) overcomes chemotherapy resistance in triple negative breast cancer.

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Lysyl Oxidase (LOX) Transcriptionally Regulates SNAI2 Expression and TIMP4 Secretion in Human Cancers.

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| S-EPMC8201910 | biostudies-literature

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