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...

Fadrozole is a Potent, Selective and Nonsteroidal Aromatase Inhibitor

Aromatase occurs widely in tissues such as adipose tissue, brain, testes, and ovaries. It is a membrane-bound microsomal complex containing NADPH-cytochrome c reductase and cytochrome P-450 units. In this article, we will introduce a potent, selective, and nonsteroidal inhibitor of aromatase, Fadrozole. It inhibits aromatase activity with an IC50...

Axitinib is a Multi-Targeted Tyrosine Kinase Inhibitor

Vascular endothelial growth factor (VEGF) is an important signal protein. Importantly, it is involved in angiogenesis and angiogenesis (blood vessels grow from a pre-existing vascular system). All members of VEGF family stimulate cell response by binding to tyrosine kinase receptors (VEGFRs) on the cell surface. Thus they dimerize and...

A 83-01 is a Potent Inhibitor of TGF-β Type I Receptor ALK5 Kinase

TGF-β, activin, nodal, and bone morphogenetic proteins (BMPs) belong to the TGF-β superfamily. It regulates a wide range of cellular responses, including cell proliferation, differentiation, adhesion, migration, and apoptosis. TGF-β and related proteins transduce signals through two distinct serine/threonine kinase receptors, including type I and type II. The function...

PR-104A is a Hypoxia-Selective DNA Cross-Linking Agent and Cytotoxin

PR-104, like TH-302, is a prodrug of nitrogen mustard that has shown some degree of efficacy in adult patients with relapsed/refractory acute myeloid leukemia (AML). PR-104A (SN 27858) is the alcohol metabolite of phosphate prodrug PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Therefore, this compound...

Oltipraz is a Nrf2 Inhibitor

Multidrug resistance-associated proteins (Mrps) are ATP-dependent transporters involved in the efflux of a vast number of endogenous and exogenous chemicals. GSH is one of the liver’s main defenses against oxidative stress because of the conjugating, scavenging, and reducing capabilities of this molecule. GSH is essential to cellular defense against...

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...