Development of neutral ceramidase inhibitor tool compounds

NIH RePORTER · NIH · R01 · $390,301 · view on reporter.nih.gov ↗

Abstract

Colorectal cancer is the third most common cancer in the United States and the second leading cause of all cancer-related deaths. Despite advances in our understanding into the mechanisms that induce colon cancer formation, treatment outcomes are still not very successful. Recently, neutral ceramidases (nCDase) was identified as a therapeutic target for the treatment of colon cancer; with nCDase KO mice displaying marked decreases in adenoma and adenocarcinoma formation in an AOM-induced mouse model of colon cancer. Current substrate mimetics for nCDase exhibit undesirable pharmaceutic properties for systemic delivery; consequently, there is a lack of specific inhibitors with pharmaceutical properties suitable for in vivo studies; impeding their study as a viable cancer target. The specific objective of this proposal is to utilize high- throughput screening (HTS) to identify chemical compounds that modulate nCDase activity and can be used to advance future in vivo studies as a potential therapeutic target.

Key facts

NIH application ID
9931170
Project number
5R01CA221948-03
Recipient
STATE UNIVERSITY NEW YORK STONY BROOK
Principal Investigator
JOHN DOUGLAS HALEY
Activity code
R01
Funding institute
NIH
Fiscal year
2020
Award amount
$390,301
Award type
5
Project period
2018-07-18 → 2022-06-30