Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Renal carcinoma antigen NY-REN-56 (PFKFB3)
• Synonyms: iPFK2; Renal carcinoma antigen NYREN56; PFKFB3; Fructose2,6bisphosphatase; 6phosphofructo2kinase/fructose2,6bisphosphatase 3; 6PF2K/Fru2,6P2ase brain/placentatype isozyme; 6PF2K/Fru2,6P2ase 3
• Gene Name: PFKFB3
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Kinase
• UniProt ID: F263_HUMAN
• TTD ID: T23787
• Sequence:
  MPLELTQSRVQKIWVPVDHRPSLPRSCGPKLTNSPTVIVMVGLPARGKTYISKKLTRYLN
  WIGVPTKVFNVGEYRREAVKQYSSYNFFRPDNEEAMKVRKQCALAALRDVKSYLAKEGGQ
  IAVFDATNTTRERRHMILHFAKENDFKAFFIESVCDDPTVVASNIMEVKISSPDYKDCNS
  AEAMDDFMKRISCYEASYQPLDPDKCDRDLSLIKVIDVGRRFLVNRVQDHIQSRIVYYLM
  NIHVQPRTIYLCRHGENEHNLQGRIGGDSGLSSRGKKFASALSKFVEEQNLKDLRVWTSQ
  LKSTIQTAEALRLPYEQWKALNEIDAGVCEELTYEEIRDTYPEEYALREQDKYYYRYPTG
  ESYQDLVQRLEPVIMELERQENVLVICHQAVLRCLLAYFLDKSAEEMPYLKCPLHTVLKL
  TPVAYGCRVESIYLNVESVCTHRERSEDAKKGPNPLMRRNSVTPLASPEPTKKPRINSFE
  EHVASTSAALPSCLPPEVPTQLPGQNMKGSRSSADSSRKH
• Function: Synthesis and degradation of fructose 2,6-bisphosphate.
• KEGG Pathway:
  Fructose and mannose metabolism (hsa00051)
  HIF-1 signaling pathway (hsa04066)
  AMPK signaling pathway (hsa04152)
• Reactome Pathway: Glycolysis (R-HSA-70171)
• BioCyc Pathway: MetaCyc:HS10144-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PFK-158	DMIR21F	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
3PO	DMPF5OX	Pulmonary fibrosis	CB03.4	Investigative	[2]

The Drug-Metabolizing Enzyme (DME) Role of This DTT

• DTT DME Name: PFK/FBPase 3 (PFKFB3) DME Info
• Gene Name: PFKFB3

1 Investigative Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Beta-fructose phosphate	DM25QXM	N. A.	N. A.	Investigative	[3]

References

• [1] Discovery of a PFKFB3 inhibitor for phase I trial testing that synergizes with the B-Raf inhibitor vemurafenib. Cancer Metab. 2014; 2(Suppl 1): P14.
• [2] CPEB4 Increases Expression of PFKFB3 to Induce Glycolysis and Activate Mouse and Human Hepatic Stellate Cells, Promoting Liver Fibrosis. Gastroenterology. 2020 Jul;159(1):273-288.
• [3] The kinase activity of human brain 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase is regulated via inhibition by phosphoenolpyruvate. Arch Biochem Biophys. 2005 Jun 15;438(2):125-36.