Category: Melanoma

Enavatuzumab (PDL192) is a Humanized IgG1 Monoclonal Antibody Targeting TWEAK

Antibody-dependent cytotoxicity (ADCC) is a cell-mediated immune defense mechanism. The effector cells of the immune system actively cleave target cells, and their membrane surface antigens are bound by specific antibodies. Besides, it is one of the mechanisms by which antibodies, as part of the humoral immune response, can limit...

ABT-510 is an Anti-Angiogenic Thrombospondin Peptide

Angiogenesis is the growth of new capillaries from existing blood vessels. Steps toward angiogenesis include protease production, endothelial cell migration, and proliferation, vascular tube formation, anastomosis of newly formed tubes, synthesis of a new basement membrane, and incorporation of pericytes and smooth muscle cells. The process of angiogenesis is...

Indoximod, An Immunometabolic Adjuvant, is an IDO Pathway Inhibitor

Indoleamine 2,3-dioxygenase (IDO) is an enzyme of interest in immuno-oncology. It has immunosuppressive effects that result from its role in tryptophan catabolism. IDO1 catalyzes the initial rate-limiting step in the degradation of the essential amino acid tryptophan along the kynurenine pathway. IDO inhibits a tryptophan sufficiency signal that stimulates...

Lomeguatrib is a O6-Methylguanine-DNA Methyltransferase (MGMT) Inhibitor

O6-alkylguanine DNA alkyltransferase (also known as AGT, MGMT or AGAT) is a protein that in humans is encoded by the O6-methylguanine DNA methyltransferase (MGMT) gene. MGMT repairs the naturally occurring mutagenic DNA lesion O6-methylguanine back to guanine and prevents mismatch and errors during DNA replication and transcription. MGMT repairs...

β-Lapachone, a Naturally Occurring O-naphthoquinone, is a Topoisomerase I Inhibitor

β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover renal oxidative status. β-Lapachone reduces cisplatin-induced nephrotoxicity. In cancer cells, cisplatin forms cross-link with  DNA, which inhibits DNA  replication,...

Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor

Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...