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Review

Identification of activators for the M2 isoform of human pyruvate kinase Version 3

Matthew B Boxer  1 , Jian-kang Jiang  1 , Matthew G Vander Heiden  2   3 , Min Shen  1 , Henrike Veith  1 , Lewis C Cantley  4   5 , Craig J Thomas  1
In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010.
[updated ].
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Review

Identification of activators for the M2 isoform of human pyruvate kinase Version 3

Matthew B Boxer et al.
Free Books & Documents

Excerpt

The expression of human pyruvate kinase M2 (hPK-M2) in cancer cells appears to be critical for tumor cell growth and proliferation in vivo. Because the PK-M2 isoform is expressed in all cancer cells studied, it represents a target for drug development that could potentially enable tumor cells to return to a normal state of metabolism. If this novel strategy for targeting malignancy were successful, it would be applicable to diverse types of cancer. The probes ML203 (CID-44543605), ML202 (CID-44246498), and ML170 (CID-4547230) are members of a series of highly specific allosteric activators for the tumor-specific isoform of human pyruvate kinase (M2 isoform). All three probes affect the cooperativity of phosphoenolpyruvate (PEP) binding, with little affect on adenosine diphosphate (ADP) binding, in a manner similar to Fructose-1,6-bisphosphate (FBP).

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