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Ref Type Journal Article
PMID (29277773)
Authors Koda Y, Itoh M, Tohda S
Title Effects of MERTK Inhibitors UNC569 and UNC1062 on the Growth of Acute Myeloid Leukaemia Cells.
Journal Vol Issue Date Pages Journal Short Title
Anticancer research 38 1 2018 01 199-204 Anticancer Res
URL
Abstract Text MER proto-oncogene tyrosine kinase (MERTK) is a receptor tyrosine kinase that affects cancer cell proliferation. This study evaluated the effects of the synthetic MERTK inhibitors UNC569 and UNC1062 on in vitro growth of acute myeloid leukaemia (AML) cells.Four AML cell lines expressing MERTK were treated with UNC569 and UNC1062 and analyzed for cell proliferation, immunoblotting, and gene expression. The effects of MERTK knockdown were also evaluated.Treatment with the inhibitors suppressed cell growth and induced apoptosis in all cell lines. OCI/AML5 and TMD7 cells, in which MERTK was constitutively phosphorylated by autocrine mechanisms, were highly susceptible to these inhibitors. The treatment reduced the phosphorylation of MERTK and its down-stream signalling molecules, v-akt murine thymoma viral oncogene homolog 1 (AKT) and extracellular signal-regulated kinase (ERK). Similar effects were observed after MERTK knockdown. The inhibitors and the knockdown caused similar changes in mRNA expression.These MERTK inhibitors are potential molecular-targeted drugs for treating AML expressing constitutively phosphorylated MERTK.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
UNC1062 UNC1062 0 0
UNC569 UNC569 0 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
UNC1062 UNC 1062|UNC-1062 MERTK Inhibitor 13 UNC1062 is a small molecule inhibitor of Mertk that may inhibits tumor cell growth (PMID: 29277773).
UNC569 UNC-569|UNC 569 MERTK Inhibitor 13 UNC569 is a small molecule inhibitor of Mertk that may inhibits tumor cell growth (PMID: 29277773).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References