General Information of the Protein
Protein ID
PT02379
Protein Name
Bifunctional purine biosynthesis protein ATIC
Secondarily
Protein Name
AICAR transformylase/inosine monophosphate cyclohydrolase
5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase
AICAR transformylase
IMP synthase
Inosinicase
Gene Name
ATIC
Secondarily
Gene Name
PURH
OK/SW-cl.86
Sequence
MAPGQLALFSVSDKTGLVEFARNLTALGLNLVASGGTAKALRDAGLAVRDVSELTGFPEMLGGRVKTLHPAVHAGILARNIPEDNADMARLDFNLIRVVACNLYPFVKTVASPGVTVEEAVEQIDIGGVTLLRAAAKNHARVTVVCEPEDYVVVSTEMQSSESKDTSLETRRQLALKAFTHTAQYDEAISDYFRKQYSKGVSQMPLRYGMNPHQTPAQLYTLQPKLPITVLNGAPGFINLCDALNAWQLVKELKEALGIPAAASFKHVSPAGAAVGIPLSEDEAKVCMVYDLYKTLTPISAAYARARGADRMSSFGDFVALSDVCDVPTAKIISREVSDGIIAPGYEEEALTILSKKKNGNYCVLQMDQSYKPDENEVRTLFGLHLSQKRNNGVVDKSLFSNVVTKNKDLPESALRDLIVATIAVKYTQSNSVCYAKNGQVIGIGAGQQSRIHCTRLAGDKANYWWLRHHPQVLSMKFKTGVKRAEISNAIDQYVTGTIGEDEDLIKWKALFEEVPELLTEAEKKEWVEKLTEVSISSDAFFPFRDNVDRAKRSGVAYIAAPSGSAADKVVIEACDELGIILAHTNLRLFHH
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
Function
Bifunctional enzyme that catalyzes the last two steps of purine biosynthesis (PubMed:11948179, PubMed:14756554). Acts as a transformylase that incorporates a formyl group to the AMP analog AICAR (5-amino-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide) to produce the intermediate formyl-AICAR (FAICAR) (PubMed:9378707, PubMed:11948179, PubMed:10985775). Can use both 10-formyldihydrofolate and 10-formyltetrahydrofolate as the formyl donor in this reaction (PubMed:10985775). Also catalyzes the cyclization of FAICAR to IMP (PubMed:11948179, PubMed:14756554). Is able to convert thio-AICAR to 6-mercaptopurine ribonucleotide, an inhibitor of purine biosynthesis used in the treatment of human leukemias (PubMed:10985775). Promotes insulin receptor/INSR autophosphorylation and is involved in INSR internalization (PubMed:25687571).
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Uniprot ID
Primary ID:
P31939

Secondarily ID:
A8K202
E9PBU3
Q13856
Q53S28
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Ensembl ID
ENSG00000138363
HGNC ID
HGNC:794
Subcellular Location
Cytoplasm
Cytosol
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000330 , CHO Pro-4 MtxRII OuaR-2-4
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0036197
 Compound Info 
2-[(4-{[(2,4-diaminopteridin-6-yl)methyl](methyl)amino}phenyl)formamido]pentanedioic acid
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C20H22N8O5
  1
1
Ki = 880 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0882698
 Compound Info 
(5-(4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl)thiophene-3-carbonyl)-L-glutamic acid
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C20H22N4O6S2
  1
1
Ki = 1070 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0915862
 Compound Info 
(5-(4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl)thiophene-2-carbonyl)-L-glutamic acid
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C20H22N4O6S2
  1
1
Ki = 5150 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0915864
 Compound Info 
(4-(4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl)thiophene-2-carbonyl)-L-glutamic acid
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C20H22N4O6S2
  1
1
Ki = 8030 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0915865
 Compound Info 
(5-(3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl)thiophene-3-carbonyl)-L-glutamic acid
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C19H20N4O6S2
  1
1
Ki = 8370 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0035062
 Compound Info 
(S)-2-(4-(4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl)benzamido)pentanedioic acid
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C22H24N4O6S
  1
1
Ki = 9480 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0915863
 Compound Info 
(5-(3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl)thiophene-2-carbonyl)-L-glutamic acid
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C19H20N4O6S2
  1
1
Ki = 14460 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0958003
 Compound Info 
(4-(3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl)thiophene-2-carbonyl)-L-glutamic acid
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C19H20N4O6S2
  1
1
Ki = 19840 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0915866
 Compound Info 
(5-(4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl)furan-2-carbonyl)-L-glutamic acid
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C20H22N4O7S
  1
1
Ki = 24710 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000111 , MDA-MB-231
 Cell Line Info 
Cell Line ID: CL000116 , MOLT-4
 Cell Line Info 
Cell Line ID: CL000145 , NCI-H460
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0036197
 Compound Info 
2-[(4-{[(2,4-diaminopteridin-6-yl)methyl](methyl)amino}phenyl)formamido]pentanedioic acid
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C20H22N8O5
  1
1 IC50 > 20000 nM
Clinical Information about the Protein
Target 1 ( Phosphoribosylaminoimidazolecarboxamide formyltransferase (ATIC) )
Target Type Literature-reported Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Investigative Drug(s) 1 Investigative Drug  1
1 NSC-88915
 Drug Info 
Investigative
Solid tumour/cancer