Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer
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Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer. / Chang, Joan; Lucas, Morghan C; Leonte, Lidia Elena; Garcia-Montolio, Marc; Singh, Lukram Babloo; Findlay, Alison D; Deodhar, Mandar; Foot, Jonathan S; Jarolimek, Wolfgang; Timpson, Paul; Erler, Janine Terra; Cox, Thomas Robert.
In: OncoTarget, Vol. 8, No. 16, 10.02.2017, p. 26066-26078.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer
AU - Chang, Joan
AU - Lucas, Morghan C
AU - Leonte, Lidia Elena
AU - Garcia-Montolio, Marc
AU - Singh, Lukram Babloo
AU - Findlay, Alison D
AU - Deodhar, Mandar
AU - Foot, Jonathan S
AU - Jarolimek, Wolfgang
AU - Timpson, Paul
AU - Erler, Janine Terra
AU - Cox, Thomas Robert
PY - 2017/2/10
Y1 - 2017/2/10
N2 - 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.
AB - 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.
U2 - 10.18632/oncotarget.15257
DO - 10.18632/oncotarget.15257
M3 - Journal article
C2 - 28199967
VL - 8
SP - 26066
EP - 26078
JO - Oncotarget
JF - Oncotarget
SN - 1949-2553
IS - 16
ER -
ID: 174632765