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http://purl.uniprot.org/citations/1854723http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/1854723http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/1854723http://www.w3.org/2000/01/rdf-schema#comment"We have recently shown that the cytosolic thyroid hormone binding protein (p58-M2) in human epidermoid carcinoma A431 cells is a monomer of pyruvate kinase, subtype M2 (PKM2). To characterize further the molecular properties of p58-M2, we overexpressed p58-M2 in Escherichia coli and purified it to homogeneity. At 22 degrees C, the monomeric p58-M2, exhibited kinase activity with an apparent Vmax of 22 +/-9 units/mg. The Km for adenosine diphosphate (ADP) and phosphoenolpyruvate (PEP) are 3.85 +/- 2.4 and 1.55 +/-0.73 mM, respectively. Upon activation by fructose 1,6-bisphosphate (Fru-1,6-P2), Vmax and Km for ADP and PEP were changed to 490 +/-27 units/mg and 0.63 +/- 0.09 and 0.13 +/-0.01 mM, respectively. These results indicated that p58-M2 has intrinsic kinase activity. Analysis of the molecular size indicated that the activation of p58-M2, by Fru-1,6-P2 resulted in the association of the monomeric p58-M2 to the tetrameric PKM2. p58-M2 bound to 3,3',5-triiodo-L-thyronine (T3) (Ka = 1.7 x 10(7) M-1) and exhibited analogue specificity, whereas PKM2 did not bind thyroid hormone. The order of binding affinity was L-T3 greater than L-thyroxine greater than 3,3',5-triiodothyropropionic acid greater than 3'-isopropyl-3,5-triiodo-L-thyronine greater than 3'5',3-triiodo-L-thyronine. Binding of T3 and its analogues resulted in the inhibition of the kinase activity of p58-M2. The order of kinase inhibitory activity and preventing its association to tetrameric PKM2 was parallel to that of binding activity.(ABSTRACT TRUNCATED AT 250 WORDS)"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.org/dc/terms/identifier"doi:10.1021/bi00243a010"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.org/dc/terms/identifier"doi:10.1021/bi00243a010"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"McPhie P."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"McPhie P."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"Lin K.-H."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"Lin K.-H."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"Cheng S.-Y."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"Cheng S.-Y."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"Ashizawa K."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/author"Ashizawa K."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/date"1991"xsd:gYear
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/date"1991"xsd:gYear
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/name"Biochemistry"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/name"Biochemistry"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/pages"7105-7111"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/pages"7105-7111"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/title"An in vitro novel mechanism of regulating the activity of pyruvate kinase M2 by thyroid hormone and fructose 1, 6-bisphosphate."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/title"An in vitro novel mechanism of regulating the activity of pyruvate kinase M2 by thyroid hormone and fructose 1, 6-bisphosphate."xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/volume"30"xsd:string
http://purl.uniprot.org/citations/1854723http://purl.uniprot.org/core/volume"30"xsd:string
http://purl.uniprot.org/citations/1854723http://www.w3.org/2004/02/skos/core#exactMatchhttp://purl.uniprot.org/pubmed/1854723
http://purl.uniprot.org/citations/1854723http://www.w3.org/2004/02/skos/core#exactMatchhttp://purl.uniprot.org/pubmed/1854723