Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTBL49X)

• DTT Name: Plasmodium Hypoxanthine-guanine phosphoribosyltransferase (Malaria LACZ)
• Synonyms: LACZ of Plasmodium falciparum (isolate FCR-3 / Gambia); Hypoxanthine phosphoribosyltransferase; HPRT; HGPRTase; HGPRT of Plasmodium falciparum (isolate FCR-3 / Gambia); Guanine phosphoribosyltransferase; GPRT
• Gene Name: Malaria LACZ
• DTT Type: Patented-recorded target; [1]
• BioChemical Class: Pentosyltransferase
• UniProt ID: HGXR_PLAFG
• TTD ID: T41666
• Sequence:
  MPIPNNPGAGENAFDPVFVNDDDGYDLDSFMIPAHYKKYLTKVLVPNGVIKNRIEKLAYD
  IKKVYNNEEFHILCLLKGSRGFFTALLKHLSRIHNYSAVETSKPLFGEHYVRVKSYCNDQ
  STGTLEIVSEDLSCLKGKHVLIVEDIIDTGKTLVKFCEYLKKFEIKTVAIACLFIKRTPL
  WNGFKADFVGFSIPDHFVVGYSLDYNEIFRDLDHCCLVNDEGKKKYKATSL
• Function: Converts guanine to guanosine monophosphate, and hypoxanthine to inosine monophosphate. Transfers the 5- phosphoribosyl group from 5-phosphoribosylpyrophosphate onto the purine. Plays a central role in the generation of purine nucleotides through the purine salvage pathway.
• KEGG Pathway:
  Purine metabolism (hsa00230)
  Drug metabolism - other enzymes (hsa00983)
  Metabolic pathways (hsa01100)
• Reactome Pathway: Purine salvage (R-HSA-74217)

Molecular Interaction Atlas (MIA) of This DTT

3 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
US9200020, Table 3 compound 8	DMCLHX5	N. A.	N. A.	Patented	[2]
US9200020, Table 3, Compound 1B	DMEARS2	N. A.	N. A.	Patented	[2]
US9200020, Table 3, Compound 2B	DMXFB5Z	N. A.	N. A.	Patented	[2]

16 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
3h-Pyrazolo[4,3-D]Pyrimidin-7-Ol	DMLB2W5	Discovery agent	N.A.	Investigative	[1]
5--Monophosphate-9-Beta-D-Ribofuranosyl Xanthine	DMX0EAK	Discovery agent	N.A.	Investigative	[1]
7-Hydroxy-Pyrazolo[4,3-D]Pyrimidine	DMV39XT	Discovery agent	N.A.	Investigative	[3]
9-Deazaguanine	DM68IPZ	Discovery agent	N.A.	Investigative	[1]
9-[2-(1-Phosphonobutan-2-yloxy)ethyl]guanine	DMOGD42	Discovery agent	N.A.	Investigative	[4]
9-[2-(1-Phosphonobutan-2-yloxy)ethyl]hypoxanthine	DMKHXT9	Discovery agent	N.A.	Investigative	[4]
9-[2-(1-Phosphonopropan-2-yloxy)ethyl]guanine	DMCXN6R	Discovery agent	N.A.	Investigative	[4]
Acetate Ion	DMD08RH	Discovery agent	N.A.	Investigative	[1]
Alpha-Phosphoribosylpyrophosphoric Acid	DMT6KI7	Discovery agent	N.A.	Investigative	[5]
Carboxylic PRPP	DMCTUR1	Discovery agent	N.A.	Investigative	[1]
Formic Acid	DMNFZC6	Discovery agent	N.A.	Investigative	[1]
Formycin B	DMHLYUM	Discovery agent	N.A.	Investigative	[1]
Guanosine-5',3'-Tetraphosphate	DMG2ZFV	Discovery agent	N.A.	Investigative	[1]
Guanosine-5'-Monophosphate	DM3SLZK	Discovery agent	N.A.	Investigative	[1]
Inosinic Acid	DMLR86H	Discovery agent	N.A.	Investigative	[1]
Pyrophosphate 2-	DMZQ75M	Discovery agent	N.A.	Investigative	[5]

References

• [1] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [2] 6-oxopurine phosphoribosyltransferase inhibitors. US9200020.
• [3] DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41.
• [4] Synthesis of branched 9-[2-(2-phosphonoethoxy)ethyl]purines as a new class of acyclic nucleoside phosphonates which inhibit Plasmodium falciparum h... Bioorg Med Chem. 2009 Sep 1;17(17):6218-32.
• [5] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.