|Aptose Announces Two Publications of Preclinical Data Elucidating the Anticancer Mechanism of Action of APTO-253|
Identification of APTO-253 target leading to inhibition of MYC expression in AML and hypersensitivity of cancer cells with BRCA1/2 deficiencies
The first publication, entitled “APTO-253 stabilizes G-quadruplex DNA, inhibits MYC expression and induces DNA damage in acute myeloid leukemia cells,” demonstrates that the APTO-253 small molecule anticancer agent inhibits expression of the MYC oncogene and depletes cells of the MYC protein, triggers the DNA repair and stress response pathways, and promotes programmed cell death (apoptosis) in acute myeloid leukemia (AML) cell lines and fresh bone marrow samples derived from patients with AML and other hematologic malignancies that often depend on MYC upregulation. The data demonstrate a multifaceted mechanism of action for APTO-253, primarily through engagement of select G-quadruplex DNA structures, one of which is located in the promoter of the MYC gene and is uniquely suited to targeting hematopoietic malignancies.
MYC dysregulation is a common driver in many malignancies, making it an attractive therapeutic target. Repression of MYC expression by bromodomain (
The second publication, entitled “APTO-253 is a new addition to the repertoire of drugs that can exploit DNA BRCA1/2 deficiency,” expands on data from a poster presentation at the 2018
“These data provide new insights into the mechanism of action of APTO-253 and add to our knowledge of how this novel agent inhibits expression of the MYC gene, an oncogene that promotes tumor growth and resistance to drugs in AML and other cancers,” said
APTO-253 is a clinical-stage small molecule targeted therapeutic agent that inhibits expression of the MYC oncogene, leading to cell cycle arrest and programmed cell death (apoptosis) in human-derived solid tumor and hematologic cancer cells, without causing general myelosuppression of the healthy bone marrow. The MYC oncogene is overexpressed in hematologic cancers, including acute myeloid leukemia (AML). Aptose researchers have reported the ability of APTO-253 to induce cell death, or apoptosis, in multiple blood cancer cell lines including AML, as well as in vitro synergy with various classes of conventional approved and investigational therapies for AML or myelodysplastic syndromes (MDS). New findings reveal that APTO-253 might also serve certain solid tumor patients with BRCA1/2 mutations, but without causing toxicity to the normal bone marrow functions.
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