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Literature summary for 2.1.2.2 extracted from

  • Wang, Y.; Mitchell-Ryan, S.; Raghavan, S.; George, C.; Orr, S.; Hou, Z.; Matherly, L.H.; Gangjee, A.
    Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents (2015), J. Med. Chem., 58, 1479-1493.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.1.2.2

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-(((5-(2-((6R)-2-amino-4-oxo-5,6,7,8-tetrahydro-1H-pyrido[2,3-d]-pyrimidin-6-yl)ethyl)thiophene-2-yl)carbonyl)amino)-pentanedioic acid LY309887 Homo sapiens
(2S)-2-(((5-(2-((6S)-2-amino-4-oxo-1,6,7,8-tetrahydropyrimido[5,4-b]-[1,4]thiazin-6-yl)ethyl)thiophene-2-yl)carbonyl)amino)-pentanedioic acid AG2034 Homo sapiens
(S)-2-(5-(3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)propyl)thiophene-2-carboxamido)pentanedioic acid
-
 Homo sapiens
(S)-2-(5-(4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)butyl)thiophene-2-carboxamido)pentanedioic acid
-
 Homo sapiens
(S)-2-(5-(5-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)pentyl)thiophene-2-carboxamido)pentanedioic acid
-
 Homo sapiens
(S)-2-(5-(6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)hexyl)thiophene-2-carboxamido)pentanedioic acid lometrexol, LMTX Homo sapiens
additional information design and synthesis of a series of 5-substituted thiopheneyl pyrrolo[2,3-d]pyrimidines with varying chain lengths (n = 1-6). The compounds show dual inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase, analysis of the unique structure-activity relationship for transport and dual target inhibition, molecular modeling and computational studies using crystal structure of human GARFTase at 1.60 A resolution, PDB ID 4EW2, overview Homo sapiens
N-([5-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]thiophen-2-yl]carbonyl)-L-glutamic acid
-
 Homo sapiens
N-([5-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]thiophen-2-yl]carbonyl)-L-glutamic acid
-
 Homo sapiens
N-[4-[3-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
-
 Homo sapiens
N-[4-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid
-
 Homo sapiens
N-[4-[4-(2-amino-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
 Homo sapiens
N-[4-[4-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)butyl]benzoyl]-L-glutamic acid
-
 Homo sapiens
N-[6-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)hexanoyl]-L-glutamic acid
-
 Homo sapiens
N-[7-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)heptanoyl]-L-glutamic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P22102
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-

Source Tissue

Source Tissue Comment Organism Textmining
KB cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
GARFTase
-
 Homo sapiens
glycinamide ribonucleotide formyltransferase
-
 Homo sapiens