Tag: Akt

Balixafortide is a Selective and Well-Tolerated Peptidic CXCR4 Antagonist

Despite the introduction of new targeted therapies and cytotoxic agents, chemotherapy-pretreated metastatic breast cancer (MBC) remains an essentially incurable disease with only moderate median overall survival (OS). over 20 human tumor types overexpress C-X-C chemokine receptor type 4 (CXCR4). CXCR4 levels correlate with aggressive metastatic phenotypes and negative prognosis...

JBJ-04-125-02 is a Mutant-Selective and Orally Active EGFR Inhibitor

Epidermal growth factor receptor (EGFR) is a transmembrane receptor protein in humans. The discovery of activating mutations in EGFR detected in 10% to 30% of patients with non–small cell lung cancer (NSCLC). In addition, it has revolutionized the treatment of this disease. Until recently, EGFR tyrosine kinase inhibitors (TKI), including...

COTI-2 is an Orally Available Mutant p53 Activator

TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...

CC-223 is an Orally Bioavailable mTOR Kinase Inhibitor

mTOR is a serine/threonine kinase that regulates cell growth, metabolism, proliferation, and survival. mTORC1 is a master regulator of cell growth and metabolism. mTORC1 positively regulates cell growth and proliferation. mTORC2 regulates cytoskeletal organization. CC-223 is a potent mTOR kinase inhibitor with an IC50 of 0.016 μM. CC-223 is...

FPA-124 is a Selective Akt Inhibitor and Induces Apoptosis

Copper complexes play an important role in the active sites of a large number of metalloproteins in biological systems. Copper complexes also have a potential application for numerous catalytic processes in living organisms. In addition, copper complexes involve electron transfer reactions or activation of some antitumor substances. In this...

BAY 61-3606, a Syk Inhibitor, Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer

Breast cancer cells usually develop resistance to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). TRAIL shows cancer-selective killing activity. TRAIL ligand selectively kills cancer cells by initiating apoptotic signaling through the engagement of its pro-apoptotic receptors, death receptors-4 and -5. In particular, myeloid cell leukemia sequence-1 (Mcl-1) is a member...