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,...
Troglitazone is an Orally Active PPARγ Agonist
Pancreatic cancer is the fourth leading cause of cancer-related deaths in Japan. Gemcitabine has been the standard therapy for advanced pancreatic cancer for over a decade. Additional novel combination therapies have been developed. It includes gemcitabine plus erlotinib; a combination of leucovorin, 5-fluorouracil, irinotecan, and oxaliplatin; and gemcitabine plus...
Cyclopamine is a Hedgehog (Hh) Pathway Antagonist
Hedgehog (Hh) signal pathway is a signal pathway that transmits information to embryonic cells for appropriate cell differentiation. Specifically, Hedgehog signaling pathway is one of the key regulators of animal development. There are three mammalian Hh proteins, Shh, Indian hedgehog (IHH), and desert hedgehog (DHH). Besides, Shh and IHH...
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...
Ganetespib (STA-9090) is a HSP90 Inhibitor
Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...
Ruxolitinib (INCB018424) is an Orally Active JAK1 and JAK2 Inhibitor
The myeloproliferative neoplasms (MPNs) are a group of related clonal diseases probably arising from hematopoietic progenitor or stem cells. Patients with MPNs have an increased risk of thrombotic and bleeding complications and disease progression to acute myeloid leukemia. JAK2 is a member of the JAK family of cytoplasmic tyrosine...
MRTX9768 is an Orally Active PRMT5 Inhibitor
PRMT5 is the main type II enzyme. It catalyzes symmetric dimethylarginine of histone proteins to induce gene silencing by generating repressive histone marks. PRMT5 can also methylate nonhistone proteins such as the transcription factors p53 and p65. Modifications of these proteins by PRMT5 have relations with diverse cellular processes....