Naphthamides as anticancer agents inhibiting CREB-mediated gene transcription
OHSU # 1295
Researchers at Oregon Health & Science University discovered a novel compound that regulates transcription activity of CREB via a novel mechanism of action. Lead optimization resulted in a first in class chemical series that is potent and highly selective. The efficacy of these compounds has been validated in vitro (e.g., breast and lung cancer cell lines) and in vivo, thus, demonstrating proof-of-concept. Regulation of CREB expression with this novel class of compounds acting in under a novel mechanism of action, address an unmet medical need for treatment of cancer.
Cyclic-AMP response element binding protein (CREB) is a transcription factor that regulates gene expression. CREB-dependent gene transcription is activated when CREB interacts with the CREB-binding protein (CBP). Over expression of CREB results in a poor prognosis for the patient, therefore regulation of CREB activity can be used to treat prostate cancer, breast cancer, lung cancer, and acute myeloid leukemia.
Hydroxynapthamide lead prior to optimization
· The “targeted cancer drug” market will reach $51B by 2015 (Decision Resources, 2010)
· 33.6% of the breast cancer therapeutic market revenue in 2006 were generated from targeted drugs (Frost & Sullivan, 2008)
Dr. Xiangshu Xiao is an Assistant Professor and Scientist in the Department of Physiology and Pharmacology, and is a member of the Knight Cancer Institute at OHSU. His lab is focusing on the development of novel drugs targeting biomolecular targets.
Technology 1295 - Patent Published, PCT WO/2010/048302
Technology 1699 - Patent Filed
OHSU Technology 1295 and 1699 are available for exclusive licensing.
Xiao X, Li B, Mitton B, Ikeda A, Sakamoto KM. Targeting CREB for Cancer Therapy: Friend or Foe. Current Cancer Drug Targets.2010;10(4):384-91.
Li B, Xiao X. Discovery of a Small-molecule Inhibitor of the KIX-KID Interaction. ChemBioChem. 2009;10(17):2721-24.
- OHSU # 1699 — Pharmaceutical compositions comprising napthamides
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