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MRCK as a Potential Target for Claudin-Low Subtype of Breast Cancer
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MRCK as a Potential Target for Claudin-Low Subtype of Breast Cancer
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Journal Article
MRCK as a Potential Target for Claudin-Low Subtype of Breast Cancer
2024
Overview
To find new molecular targets for triple negative breast cancer (TNBC), we analyzed a large-scale drug screening dataset based on breast cancer subtypes. We discovered that BDP-9066, a specific MRCK inhibitor (MRCKi), may be an effective drug against TNBC. After confirming the efficacy and specificity of BDP-9066 against TNBC
and
, we further analyzed the underlying mechanism of specific activity of BDP-9066 against TNBC. Comparing the transcriptome of BDP-9066-sensitive and -resistant cells, the activation of the focal adhesion and YAP/TAZ pathway were found to play an important role in the sensitive cells. Furthermore, YAP/TAZ is indeed repressed by BDP-9066 in the sensitive cells, and active form of YAP suppresses the effects of BDP-9066. YAP/TAZ expression and activity are high in TNBC, especially the Claudin-low subtype, consistent with the expression of focal adhesion-related genes. Interestingly, NF-κB functions downstream of YAP/TAZ in TNBC cells and is suppressed by BDP-9066. Furthermore, the PI3 kinase pathway adversely affected the effects of BDP-9066 and that alpelisib, a PI3 kinase inhibitor, synergistically increased the effects of BDP-9066, in
mutant TNBC cells. Taken together, we have shown for the first time that MRCKi can be new drugs against TNBC, particularly the Claudin-low subtype.
Publisher
Ivyspring International Publisher Pty Ltd,Ivyspring International Publisher
Subject
1-Phosphatidylinositol 3-kinase
/ Adaptor Proteins, Signal Transducing - metabolism
/ Adhesion
/ Drugs
/ Genomics
/ Humans
/ Kinases
/ Patients
/ Phosphatidylinositol 3-Kinases - genetics
/ Phosphatidylinositol 3-Kinases - metabolism
/ Plasmids
/ Proteins
/ Software
/ Transcription Factors - genetics
/ Transcription Factors - metabolism
/ Triple Negative Breast Neoplasms - drug therapy
/ Triple Negative Breast Neoplasms - genetics
/ Triple Negative Breast Neoplasms - metabolism
/ Tumors
