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Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer.

ABSTRACT: Lysyl Oxidase-like 2 (LOXL2), a member of the lysyl oxidase family of amine oxidases is known to be important in normal tissue development and homeostasis, as well as the onset and progression of solid tumors. Here we tested the anti-tumor properties of two generations of novel small molecule LOXL2 inhibitor in the MDA-MB-231 human model of breast cancer. We confirmed a functional role for LOXL2 activity in the progression of primary breast cancer. Inhibition of LOXL2 activity inhibited the growth of primary tumors and reduced primary tumor angiogenesis. Dual inhibition of LOXL2 and LOX showed a greater effect and also led to a lower overall metastatic burden in the lung and liver. Our data provides the first evidence to support a role for LOXL2 specific small molecule inhibitors as a potential therapy in breast cancer.

SUBMITTER: Chang J

PROVIDER: S-EPMC5432238 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature

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Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer.

Chang Joan J Lucas Morghan C MC Leonte Lidia E LE Garcia-Montolio Marc M Singh Lukram Babloo LB Findlay Alison D AD Deodhar Mandar M Foot Jonathan S JS Jarolimek Wolfgang W Timpson Paul P Erler Janine T JT Cox Thomas R TR

Oncotarget 20170401 16

Lysyl Oxidase-like 2 (LOXL2), a member of the lysyl oxidase family of amine oxidases is known to be important in normal tissue development and homeostasis, as well as the onset and progression of solid tumors. Here we tested the anti-tumor properties of two generations of novel small molecule LOXL2 inhibitor in the MDA-MB-231 human model of breast cancer. We confirmed a functional role for LOXL2 activity in the progression of primary breast cancer. Inhibition of LOXL2 activity inhibited the grow ...[more]

PMID: 28199967

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Dataset Information

Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer.

Publications

Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer.

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