Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTCZOF2)

DTT Name Pyruvate dehydrogenase kinase 1 (PDHK1)
Synonyms Pyruvate dehydrogenase kinase isoform 1; Pyruvate dehydrogenase (acetyl-transferring) kinase isozyme 1, mitochondrial; PDHK1; PDH kinase 1
Gene Name PDK1
DTT Type
Clinical trial target
 [1]
BioChemical Class
Kinase
UniProt ID
PDK1_HUMAN
TTD ID
T15776
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 2.7.11.2
Sequence
MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMK
QFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQE
LLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYF
LDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLC
DLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPP
IQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLP
ISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDW
CVPSREPKDMTTFRSA
Function
Kinase that plays a key role in regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Plays an important role in cellular responses to hypoxia and is important for cell proliferation under hypoxia. Protects cells against apoptosis in response to hypoxia and oxidative stress.
KEGG Pathway
HIF-1 signaling pathway (hsa04066 )
Axon guidance (hsa04360 )
Central carbon metabolism in cancer (hsa05230 )
Reactome Pathway
Signaling by Retinoic Acid (R-HSA-5362517 )
Regulation of pyruvate dehydrogenase (PDH) complex (R-HSA-204174 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dichloroacetate DMZ5Y1P Insulin-resistant disorder 5A44 Phase 4 [2]
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98 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
1,2-dihydroindazolo[4,3-bc][1,5]benzoxazepine derivative 1 DMRFXMB Metastatic cancer 2D50-2E2Z Patented [1]
Benzimidazole and imidazopyridine derivative 1 DMIXERP Metastatic cancer 2D50-2E2Z Patented [1]
Benzonaphthyridine derivative 1 DMM9J34 Metastatic cancer 2D50-2E2Z Patented [1]
Benzonaphthyridine derivative 2 DMB74LZ Metastatic cancer 2D50-2E2Z Patented [1]
Bis-indolylmaleimide derivative 1 DMOR9ZA Metastatic cancer 2D50-2E2Z Patented [1]
Dibenzo [c,f]-[2,7]naphthyridine derivative 1 DMRM5I1 Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 1 DMPRF1K Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 10 DMVTARK Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 2 DMGEFIW Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 3 DMBGTNM Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 4 DMHUIXR Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 5 DMMX6V4 Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 6 DM9IPDU Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 7 DMOAYEV Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 8 DMJTN91 Metastatic cancer 2D50-2E2Z Patented [1]
Heteroaryl-carboxamide derivative 9 DMI627Z Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 10 DMN580F Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 11 DMUOI92 Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 12 DMQJW9R Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 13 DMWOBHM Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 14 DMJ0WVR Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 15 DMWZNDO Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 16 DM6NJV7 Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 17 DMD1K7E Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 18 DMFUEDL Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 19 DMNG0WH Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 4 DM7VP8M Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 5 DMWJDEO Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 6 DM6HWN3 Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 7 DMU6LS4 Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 8 DMKPSIA Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic derivative 9 DMY4LB7 Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic-carboxamide derivative 1 DMA91IJ Metastatic cancer 2D50-2E2Z Patented [1]
Heterocyclic-carboxamide derivative 2 DMSQK50 Metastatic cancer 2D50-2E2Z Patented [1]
Imidazo quinoline derivative 1 DMGDMWA Metastatic cancer 2D50-2E2Z Patented [1]
Indazole derivative 1 DME8JTW Metastatic cancer 2D50-2E2Z Patented [1]
Indolinone derivative 1 DMTC129 Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-EP20041486488 DMDZT7Y Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20120277229 39(1.1) DMR4MSH Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20120277229 40(1.2) DMR3J9A Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20120277229 41(1.3) DM7V6E0 Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20120277229 44(1.4) DMUQ04C Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20120277229 45(1.5) DMEIA6Y Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20130053382 35(1-11) DMDHJMU Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20130053382 36(3-5) DM40FVN Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20130053382 37(4-6) DMY7Z85 Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-US20130053382 38(5-7) DMHLQ2T Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2004087707 DM809AX Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2006015124 DMV7PNF Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2008005457 DMDMJYL Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2008079988 DMKJ1HC Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2008107444 DM8L5JR Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2009153313 DMTP02Q Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2010127754 DM37FDV Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2011137219 35(1-11) DM3IZ0H Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2011137219 36(3-5) DMAQHI5 Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2011137219 37(4-6) DMSQ5J8 Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2011137219 38(5-7) DM4NXBK Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2012135799 42(1.4) DMSDRA4 Metastatic cancer 2D50-2E2Z Patented [1]
PMID25684022-Compound-WO2012135799 43(1.5) DMHI3O1 Metastatic cancer 2D50-2E2Z Patented [1]
Pyrazole derivative 61 DMO6M1Q Metastatic cancer 2D50-2E2Z Patented [1]
Pyrazolopyridines and imidazopyridine derivative 1 DMSR5FO Metastatic cancer 2D50-2E2Z Patented [1]
Pyridinone carboxamide derivative 1 DM3F4KS Metastatic cancer 2D50-2E2Z Patented [1]
Pyrido[4,3-d]pyrimidin-5(6H)-one derivative 1 DMOTGEK Metastatic cancer 2D50-2E2Z Patented [1]
Pyrimidine derivative 3 DMC3E8M Metastatic cancer 2D50-2E2Z Patented [1]
Pyrimidinone derivative 1 DM1I7Z6 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 1 DMW62LX Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 10 DMWKI89 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 11 DM0Q3HF Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 12 DMG0H73 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 13 DMHQCEJ Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 14 DMMKNP7 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 15 DMCH1DL Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 16 DMJQBVH Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 17 DMPMN92 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 18 DM987MK Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 19 DMW59Q4 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 2 DMLIRGM Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 20 DMORSH9 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 21 DMTJBCG Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 22 DM6WTR2 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 23 DMMO6JY Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 24 DMZ6YB0 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 25 DMLRTFX Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 26 DM8DHZ4 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 27 DMV30QO Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 28 DMGEIZV Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 29 DMCRVO5 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 3 DMLRA3C Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 30 DMEOKCB Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 4 DMI3X14 Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 5 DM2H95E Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 6 DMWHCOE Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 7 DMLBK8V Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 8 DMVOTKN Metastatic cancer 2D50-2E2Z Patented [1]
Thiazole carboxamide derivative 9 DM5P04R Metastatic cancer 2D50-2E2Z Patented [1]
Thieno[3,2-c]pyridine-7-carboxamide derivative 1 DM1C8MA Metastatic cancer 2D50-2E2Z Patented [1]
Thieno[3,2-c]pyridine-7-carboxamide derivative 2 DMOWFA5 Metastatic cancer 2D50-2E2Z Patented [1]
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⏷ Show the Full List of 98 Patented Agent(s)

References

1 PDK1 disruptors and modulators: a patent review.Expert Opin Ther Pat. 2015 May;25(5):513-37.
2 Comparison of Antitumor Effects of Combined and Separate Treatment with NO Synthase Inhibitor T1023 and PDK1 Inhibitor Dichloroacetate. Bull Exp Biol Med. 2019 Nov;168(1):92-94.