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Dear Colleague, Welcome to the inaugural edition of our annual Mechanism of Action Magnifier™! The Magnifier series is an exclusive supplement brought to you by the publishers of Personalized Medicine in Oncology (PMO) to delve into the biochemical interaction through [ Read More ]
The MAPK pathway is constitutively activated in the majority of melanomas as a result of molecular alterations in genes encoding key components of the pathway (eg, BRAF and NRAS mutations) or upstream cell surface receptors (eg, KIT), resulting in uncontrolled [ Read More ]
Blinatumomab (derived from “B-lineage–specific antitumor mouse monoclonal antibody”) is a bispecific CD19-directed CD3 T-cell engaging antibody that binds to1-3: CD19 (expressed on the surface of cells of B-lineage origin) CD3 (expressed on the surface of T cells). More than 90% [ Read More ]
In B-cell malignancies, such as chronic lymphocytic leukemia (CLL) and indolent non-Hodgkin lymphoma, the malignant B cells rely on a number of internal and external stimuli to survive, such as the activation of the B-cell receptor, cytokine and chemokine signaling, [ Read More ]
B cells circulate between multiple sites in the body during their normal life cycle, and these B cells rely on cues from the support of microenvironments to promote proper development, maturation, and function.1 Chemotaxis to, and adhesion within, proliferative microenvironments, [ Read More ]
There are 4 isoforms of phosphatidylinositol 3-kinase (PI3K) with distinct functions and expression patterns; among those 4 isoforms, PI3K-alpha and PI3K-beta are ubiquitously expressed and involved in a range of cellular functions.1 Both PI3K-gamma and PI3K-delta are expressed predominantly in [ Read More ]
In the cell nucleus, DNA is maintained in a tightly coiled state around proteins called histones.1 During the process of DNA replication for cell division or during the synthesis of RNA and proteins, histone acetyltransferase adds acetyl groups onto the [ Read More ]
Overactive JAK pathway signaling is a key mechanism of disease in the myeloproliferative neoplasms (MPNs) polycythemia vera and myelofibrosis.1,2 Signaling of the JAK pathway plays a key role in normal cell functioning.3-6 Well-regulated JAK signaling is essential for cell production, [ Read More ]
Proteins in the B-cell lymphoma-2 (BCL-2) family are key regulators of apoptosis, and the BCL-2 gene is frequently overexpressed in leukemias and lymphomas.1,2 The BH3-only proteins of the BCL-2 family (ie, those having only the BCL-2 homology domain BH3) can [ Read More ]
Cyclin-dependent kinases (CDKs) 4 and 6 are overactive in many human cancers, resulting in a loss of regulation of the G1 cell cycle restriction point and making malignant cells less responsive to normal growth controls.1,2 CDK4 and CDK6 CDKs are [ Read More ]
Lenvatinib (Figure) is an orally administered multiple receptor tyrosine kinase (RTK) inhibitor with a novel binding mode that selectively inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors1: VEGFR1 (FLT1) VEGFR2 (KDR) VEGFR3 (FLT4). Lenvatinib also inhibits other [ Read More ]
ALK Rearrangements in Lung Adenocarcinoma ALK has been found to fuse with other partners, leading to potent malignant transformation.1,2 The most common among ALK fusion genes in lung cancer, specifically non–small cell lung cancer (NSCLC), is the EML4 ALK translocation [ Read More ]
Bavituximab is a first-in-class phosphatidylserine (PS)-targeting monoclonal antibody that blocks PS-mediated immunosuppression by multifocal reprogramming of immune cells in the tumor microenvironment to support immune activation.1 PS is a highly immunosuppressive molecule usually located inside the membrane of healthy cells, [ Read More ]
Overexpression of the epidermal growth factor receptor (EGFR) is correlated with poor prognosis in many human cancers.1 EGFR is a member of the ErbB family of receptor tyrosine kinases (TKs). EGFR activation occurs in response to ligand stimulation and/or genetic [ Read More ]
Trabectedin (ET-743) is a marine alkaloid isolated from the Caribbean tunicate Ecteinascidia turbinata, with a chemical structure characterized by 3 fused tetrahydroisoquinoline rings.1 Trabectedin binds to the minor groove of DNA and alkylates guanine at the N2 position, bending the [ Read More ]