Crystallization (Comment) | Organism |
---|---|
crystal structure analysis of human enzyme complexed with the sulfamido-bridged N-[(S)-(4-([(2-amino-4-hydroxy-quinazolin-6-yl)dihydroxy-lambda-4-sulfanyl]amino)phenyl)-hydroxymethyl]-L-glutamic acid at 2.55 A resolution, PDB ID 1P4R | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(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 | inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase | 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 | inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase | 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 AICARFTase at 2.55 A resolution, PDB ID 1P4R, overview. No inhibition by N-[4-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid, N-[4-[3-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)propyl]benzoyl]-L-glutamic acid, 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, 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, and (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 | |
N-[(S)-(4-([(2-amino-4-hydroxy-quinazolin-6-yl)dihydroxy-lambda-4-sulfanyl]amino)phenyl)-hydroxymethyl]-L-glutamic acid | binding structure, docking study and crystal structure analysis | 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 | inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase | 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 | inhibits de novo purine nucleotide rather than thymidylate biosynthesis via inhibition of both glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase | Homo sapiens | |
pemetrexed | the enzyme is a pharmacologically important target of anticancer drug pemetrexed, an antifolate inhibitor | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P31939 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
KB cell | - |
Homo sapiens | - |
Synonyms | Comment | Organism |
---|---|---|
5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase | - |
Homo sapiens |
AICA ribonucleotide formyltransferase | - |
Homo sapiens |
AICARFTase | - |
Homo sapiens |
ZMP formyltransferase | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
malfunction | inhibition of the enzyme results in depletion of purine nucleotides | Homo sapiens |
physiological function | the enzyme is involved in purine nucleotide biosynthesis | Homo sapiens |