Category: Melanoma

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...

CBL0137 is an Histone Chaperone FACT Inhibitor

Cancer harbors several characteristics, including high heterogeneity, diverse gene mutation, or rapid progression; consequently, treating cancer is difficult, and it easily relapses. Surgery, radiotherapy, chemotherapy, immunotherapy, and targeted therapy show remarkable achievements. In particular, targeted therapies promote treatment. However, we have failed to treat cancer. Chemotherapy with or without...

CX-5461 is an Orally Active rRNA Synthesis Inhibitor

RNA polymerase is an enzyme that synthesizes RNA from a DNA template. Specifically, RNA synthesis or transcription is the process of transcribing DNA nucleotide sequence information into RNA sequence information. Besides, RNA synthesis is catalyzed by a large enzyme called RNA polymerase. The basic biochemistry of RNA synthesis is...

Elesclomol (STA-4783) is an Oxidative Stress Inducer and Induces Apoptosis

Modulating reactive oxygen species (ROS) levels has been proposed as a therapeutic strategy for cancer. In normal cells, ROS are produced at low concentrations and cancer cells produce elevated levels of ROS due to increased metabolic activity, resulting in a state of chronic oxidative stress. Recent studies showed the...