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Invention E-326-2008/0

Small Molecule Activators of Human Pyruvate Kinase

Lead Inventor: Craig Thomas (NCATS)
Inventors: Douglas Auld (NCATS), Matthew Boxer (NCATS), James Inglese (NCATS), Jian-kang Jiang (NCATS), Amanda Skoumbourdis (NCATS)
Ref. No.: E-326-2008/0

Abstract: NIH investigators have discovered a series of small compounds with the potential to treat a variety of cancers as well as hemolytic anemia. Contrary to most cancer medications, these molecules can be non-toxic to normal cells because they target a protein specific to the metabolic pathways in tumors, thus representing a significant clinical advantage over less-specific chemotherapeutics.

Publications:

Pyruvate Kinase M2 Activators Promote Tetramer Formation and Suppress Tumorigenesis • Nature Chemical Biology • October 2012 • NCATS Chemical Genomics Center

Evaluation of Thieno[3,2-b]pyrrole[3,2-d]pyridazinones as Activators of the Tumor Cell Specific M2 Isoform of Pyruvate Kinase • Bioorganic & Medicinal Chemistry Letters • June 2010 • NCATS Chemical Genomics Center

Evaluation of Substituted N,N'-diarylsulfonamides as Activators of the Tumor Cell Specific M2 Isoform of Pyruvate Kinase
• Journal of Medicinal Chemistry • Feb. 11, 2010 • NCATS Chemical Genomics Center

Last updated: 07-21-2016
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