NAMPT Inhibitors Exhibit Excellent Potency and ADME Properties
Nicotinamide phosphoribosyltransferase (NAmPRTase or Nampt), also known as pre-B-cell colony-enhancing factor 1 (PBEF1) or visfatin, is highly overexpressed in many types of tumors, which makes it a great target for chemotherapy. Recent studies also suggest that Nampt plays a role in improving immune functions. University of Pittsburgh researchers have synthesized and tested a novel class of Nampt inhibitors in a current study, which shows that they have exhibited excellent potency and ADME properties.
Description
Nampt is a rate-limiting enzyme in the Nicotinamide adenine dinucleotide (NAD+) salvage pathway that converts nicotinamide to nicotinamide mononucleotide in mammals. This in turn enables NAD+ biosynthesis. Pitt researcher’s novel discovery showed the secreted form of the Nampt acts as a cytokine that stimulates NF-kb pathway and inflammation through activation of Toll-like Receptor 4 (TLR4).Applications
· Cancer patients undergoing chemotherapy· Patients with compromised immune function
Advantages
· Nampt inhibitors show excellent ADME properties· Exhibit strong potency in current testing
· Ideal target for chemotherapy and other immune treatments