Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTDBX7N)

• DTT Name: S-methyl-5'-thioadenosine phosphorylase (MTAP)
• Synonyms: Methylthioadenosine phosphorylase; MTAPase; MTA phosphorylase; MSAP; 5'-methylthioadenosine phosphorylase
• Gene Name: MTAP
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Glycosyltransferases
• UniProt ID: MTAP_HUMAN
• TTD ID: T40787
• EC Number: EC 2.4.2.28
• Sequence:
  MASGTTTTAVKIGIIGGTGLDDPEILEGRTEKYVDTPFGKPSDALILGKIKNVDCVLLAR
  HGRQHTIMPSKVNYQANIWALKEEGCTHVIVTTACGSLREEIQPGDIVIIDQFIDRTTMR
  PQSFYDGSHSCARGVCHIPMAEPFCPKTREVLIETAKKLGLRCHSKGTMVTIEGPRFSSR
  AESFMFRTWGADVINMTTVPEVVLAKEAGICYASIAMATDYDCWKEHEEAVSVDRVLKTL
  KENANKAKSLLLTTIPQIGSTEWSETLHNLKNMAQFSVLLPRH
• Function: Involved in the breakdown of MTA, a major by-product of polyamine biosynthesis. Responsible for the first step in the methionine salvage pathway after MTA has been generated from S-adenosylmethionine. Has broad substrate specificity with 6-aminopurine nucleosides as preferred substrates. Catalyzes the reversible phosphorylation of S-methyl-5'-thioadenosine (MTA) to adenine and 5-methylthioribose-1-phosphate.
• KEGG Pathway:
  Cysteine and methionine metabolism (hsa00270)
  Metabolic pathways (hsa01100)
• Reactome Pathway:
  Gene and protein expression by JAK-STAT signaling after Interleukin-12 stimulation (R-HSA-8950505)
  Methionine salvage pathway (R-HSA-1237112)
• BioCyc Pathway: MetaCyc:HS01913-MON

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
METHYLTHIOADENOSINE	DMC8J6F	Multiple sclerosis	8A40	Terminated	[1]

2 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
5'-Deoxy-5'-(Methylthio)-Tubercidin	DMR28HG	Discovery agent	N.A.	Investigative	[1]
Formycin	DMWG0P3	Discovery agent	N.A.	Investigative	[1]

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

• DTT DME Name: S-methyl-5'-thioadenosine phosphorylase (MTAP) DME Info
• Gene Name: MTAP

1 Discontinued Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
METHYLTHIOADENOSINE	DMC8J6F	Multiple sclerosis	8A40	Terminated	[2]

References

• [1] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [2] Picomolar transition state analogue inhibitors of human 5'-methylthioadenosine phosphorylase and X-ray structure with MT-immucillin-A. Biochemistry. 2004 Jan 13;43(1):9-18.