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Human PDK1 Recombinant Protein (RPPB2598)

SKU:
RPPB2598
Product Type:
Recombinant Protein
Species:
Human
Uniprot:
Q15118
Research Area:
Enzymes
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Description

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Product Name:Human PDK1 Recombinant Protein
Product Code:RPPB2598
Size:50µg
Species:Human
Target:PDK1
Synonyms:Pyruvate dehydrogenase kinase isoform 1, PDK1, Pyruvate dehydrogenase (lipoamide) kinase isozyme 1 mitochondrial.
Source:Escherichia Coli
Physical Appearance:Sterile filtered colorless solution.
Formulation:PDK1 solution containing 20mM Tris pH-7, 0.5mM DTT, 0.1M NaCl, 0.1mM EDTA 0.1mM PMSF, 1mM MgCl2 and 40% glycerol.
Stability:PDK1 Human Recombinant although stable at 4°C for 1 week, should be stored below -18°C. Please prevent freeze thaw cycles.
Purity:Greater than 95.0% as determined by SDS-PAGE.
Amino Acid Sequence:MGSSHHHHHH SSGLVPRGSH MSSDSGSSPA SERGVPGQVD FYARFSPSPL SMKQFLDFGS VNACEKTSFM FLRQELPVRL ANIMKEISLLPDNLLRTPSV QLVQSWYIQS LQELLDFKDK SAEDAKAIYD FTDTVIRIRN RHNDVIPTMA QGVIEYKESF GVDPVTSQNV QYFLDRFYMS RISIRMLLNQ HSLLFGGKGK GSPSHRKHIG SINPNCNVLE VIKDGYENAR RLCDLYYINS PELELEELNA KSPGQPIQVV YVPSHLYHMVFELFKNAMRA TMEHHANRGV YPPIQVHVTL GNEDLTVKMS DRGGGVPLRK IDRLFNYMYS TAPRPRVETS RAVPLAGFGY GLPISRLYAQ YFQGDLKLYS LEGYGTDAVI YIKALSTDSI ERLPVYNKAA WKHYNTNHEA DDWCVPSREP KDMTTFRSA

PDK1 takes part in the regulation of enzymatic activity of mammalian pyruvate dehydrogenase which is part of a mitochondrial multienzyme complex to catalyze the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. PDK1 inhibits glioblastoma growth. PDK1 inhibits the mitochondrial pyruvate dehydrogenase complex by phosphorylation of the e1 alpha subunit, therefore contributing to the regulation of glucose metabolism. PDK1 kinase activity is negatively regulated by binding to 14-3-3.

PDK1 Human Recombinant produced in E.Coli is a single, non-glycosylated, polypeptide chain containing 429 amino acids (29-436) and having a molecular mass of 48.6 kDa. PDK1 is fused to 20 a.a. His-Tag at N-terminus and purified by proprietary chromatographic techniques.

UniProt Protein Function:PDHK1: an ubiquitously expressed, atypical protein kinase associated with the mitochondrial matrix. The PDHKs play crucial roles in switching metabolic flux from oxidative phosphorylation towards glycolysis. PDHK1 is detected in heart, pancreatic islets, and skeletal muscles. Contains a HATPase_c catalytic domain, found in several ATP-binding proteins including protein histidine kinases (PHKs), PHDKs, DNA gyrase B, topoisomerases, heat shock proteins, and DNA mismatch repair proteins. PDHK regulates glucose oxidation through inhibitory phosphorylation of the E1 alpha subunit of the mitochondrial pyruvate dehydrogenase complex (PDHC) at any one of 3 inhibitory serine residues. Inhibitory sites 1, 2, and 3 correspond to S293, S300, and S232 in human PDHA1, respectively. Four PDHK isoenzymes have been described, each with different site specificity: all four phosphorylate sites 1 and 2 but at different rates; for site 1 PDHK2 >PDHK4 >PDHK1 >PDHK3; for site 2, PDHK3> PDHK4 > PDHK2 > PDHK1. Only PDHK1 phosphorylates site 3. PDHKs are recruited to the PDHC by binding to a lipoyl group covalently attached to the inner lipoyl domain of the E2 component. PDHA1 deficiency is the most common enzyme defect in patients with primary lactic acidosis. PDHK1 is a direct HIF-1 target gene. Suppression of PDH by PDHK inhibits the conversion of pyruvate to acetyl-CoA, attenuates mitochondrial respiration, and may contribute to the increased lactate production observed in many tumors. The PDH pathway is repressed in a majority of non-small cell lung carcinomas. Inhibited by AZD7545, dichloroacetate (DCA) and radicicol. Radicicol inhibits kinase activity by binding directly to the ATP-binding pocket of PDHK, similar to HSP90 from the same ATPase/kinase superfamily.
UniProt Protein Details:

Protein type:Mitochondrial; EC 2.7.11.2; Kinase, protein; Protein kinase, atypical; ATYPICAL group; PDHK family

Chromosomal Location of Human Ortholog: 2q31.1

Cellular Component: mitochondrion; mitochondrial matrix; mitochondrial pyruvate dehydrogenase complex

Molecular Function:protein binding; pyruvate dehydrogenase (acetyl-transferring) kinase activity; ATP binding; protein kinase activity

Biological Process: cellular metabolic process; cell proliferation; glucose metabolic process; regulation of acetyl-CoA biosynthetic process from pyruvate; pyruvate metabolic process; protein amino acid phosphorylation; induction of apoptosis by oxidative stress

NCBI Summary:Pyruvate dehydrogenase (PDH) is a mitochondrial multienzyme complex that catalyzes the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. The enzymatic activity is regulated by a phosphorylation/dephosphorylation cycle. Phosphorylation of PDH by a specific pyruvate dehydrogenase kinase (PDK) results in inactivation. Multiple alternatively spliced transcript variants have been found for this gene. [provided by RefSeq, Jun 2013]
UniProt Code:Q15118
NCBI GenInfo Identifier:3183117
NCBI Gene ID:5163
NCBI Accession:Q15118.1
UniProt Secondary Accession:Q15118,Q308M4, B2R6T1, B7Z937, D3DPD8, E9PD65,
UniProt Related Accession:Q15118
Molecular Weight:436
NCBI Full Name:[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
NCBI Synonym Full Names:pyruvate dehydrogenase kinase, isozyme 1
NCBI Official Symbol:PDK1��
NCBI Protein Information:[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial; [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial; PDH kinase 1; pyruvate dehydrogenase kinase, isoenzyme 1; mitochondrial pyruvate dehydrogenase, lipoamide, kinase isoenzyme 1
UniProt Protein Name:[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
UniProt Synonym Protein Names:Pyruvate dehydrogenase kinase isoform 1; PDH kinase 1
Protein Family:[Pyruvate dehydrogenase
UniProt Gene Name:PDK1��
UniProt Entry Name:PDK1_HUMAN

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