Kinase Domain of Pyruvate Kinase, porcine liver

TECHNICAL SPECIFICATIONS

1.MECHANISM OF ACTION

This protein domain functions as a phosphotransferase enzyme, specifically catalyzing the final ATP-generating step of glycolysis. Its catalytic mechanism involves a concerted, bi-bi ordered reaction. The enzyme binds phosphoenolpyruvate (PEP) and adenosine diphosphate (ADP) in its active site, facilitating the direct transfer of the high-energy phosphoryl group from PEP to ADP. This reaction produces one molecule of pyruvate and one molecule of ATP. 

2.PRODUCT INDICATIONS

• Enzyme Kinetics & Allosteric Regulation Studies: Characterizing substrate affinity (Km for PEP/ADP), catalytic rate (kcat), and the effects of allosteric activators (e.g., FBP) or inhibitors (e.g., ATP, phenylalanine) on the isolated catalytic domain.

• Cancer Metabolism Research: Investigating the role of PKM2 regulation in the Warburg effect, using the porcine domain as a model due to its high homology and similar regulatory properties to human PKM2.

• Drug Discovery & Screening: Serving as the direct target in high-throughput screening (HTS) campaigns to identify novel small-molecule activators or inhibitors of PKM2 for potential applications in cancer or metabolic diseases.

• Structural Biology: Providing a simplified, stable protein construct for X-ray crystallography or cryo-electron microscopy studies to determine atomic-level structures in complex with substrates, allosteric effectors, or drug candidates.

• Comparative Biochemistry: Studying evolutionary conservation of pyruvate kinase structure-function relationships across species.

3.CLINICAL EFFICACY OF PRODUCT

• Research Tool Efficacy: Its efficacy is defined by its ability to provide consistent, high-quality enzymatic activity for mechanistic studies and compound screening, generating reliable data that informs downstream development.

• Therapeutic Target Validation: PKM2, and specifically its dysregulated activity, is a well-validated target in oncology. Tumor cells often express the PKM2 isoform, which can be manipulated to favor a glycolytic phenotype that supports rapid growth.

• Drug Development Context: Research using this and similar purified PKM2 constructs has fueled the discovery of PKM2 modulators. Small-molecule activators (e.g., TEPP-46, DASA-58) that promote the active tetrameric form have shown promise in preclinical models by reversing the Warburg effect and inhibiting tumor growth. These compounds were identified and characterized using isolated PKM2 protein.

• Clinical Status: While no PKM2-targeted drug has yet received FDA approval, several candidates have progressed to early-phase clinical trials. This purified domain plays a foundational role in the preclinical research pipeline that validates the target and identifies lead compounds.




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