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Lometrexol

Known as: L-Glutamic acid, N-(4-(2-((6R)-2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido(2,3-d)pyrimidin-6-yl)ethyl)benzoyl)-, LMTX, 6R-5,10-Dideazatetrahydrofolate 
A folate analog antimetabolite with antineoplastic activity. As the 6R diastereomer of 5,10-dideazatetrahydrofolate, lometrexol inhibits glycinamide… 
National Institutes of Health

Related topics

Related topics

5 relations

Broader (3)

Antimetabolites, AntineoplasticFolic Acid AntagonistsTetrahydrofolates
Dideaza-5,6,7,8-Tetrahydrofolic Acidfolic acid/lometrexol/paclitaxel

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
2004
2004
Biochemistry and pharmacology of glycinamide ribonucleotide formyltransferase inhibitors: LY309887 and lometrexol
SummaryLometrexol, a tight-binding antifolate inhibitor of the purine de novo enzyme glycinamide ribonucleotide formyltransferase… 
Highly Cited
2002
Highly Cited
2002
Multiple mechanisms of resistance to methotrexate and novel antifolates in human CCRF-CEM leukemia cells and their implications for folate homeostasis.
2002
2002
Mouse folylpoly-gamma-glutamate synthetase isoforms respond differently to feedback inhibition by folylpolyglutamate cofactors.
Folylpoly-gamma-glutamate synthetase (FPGS) is the enzyme responsible for metabolic trapping of reduced folate cofactors in cells… 
2000
2000
Sensitivity to 5,10-dideazatetrahydrofolate is fully conserved in a murine leukemia cell line highly resistant to methotrexate due to impaired transport mediated by the reduced folate carrier.
A murine leukemia cell line was identified that is highly resistant to methotrexate (MTX), due to impaired transport, but fully… 
2000
2000
Weekly lometrexol with daily oral folic acid is appropriate for phase II evaluation
Purpose: Lometrexol [(6R)-5,10-dideaza-5,6,7,8-tetrahydrofolate] is the prototype folate antimetabolite that targets the de novo… 
Review
1999
Review
1999
Preclinical and Clinical Evaluation of the Glycinamide Ribonucleotide Formyltransferase Inhibitors Lometrexol and LY309887
The importance of the purine de novo pathway in providing DNA precursors for cancer cell growth led to the hypothesis that novel… 
1997
1997
Tight binding of folate substrates and inhibitors to recombinant mouse glycinamide ribonucleotide formyltransferase.
The binding of the prototypical folate inhibitor of de novo purine synthesis, 5,10-dideazatetrahydrofolate (DDATHF), and its… 
1992
1992
Metabolic effects and kill of human T-cell leukemia by 5-deazaacyclotetrahydrofolate, a specific inhibitor of glycineamide ribonucleotide transformylase.
Metabolic effects and mode of cytotoxicity of 5-deazaacyclotetrahydrofolate (5-DACTHF, BW543U76), a glycineamide ribonucleotide… 
1992
1992
In vitro activity of novel antifolates against human squamous carcinoma cell lines of the head and neck with inherent resistance to methotrexate
A series of 7 human squamous carcinoma cell lines of the head and neck (HNSCC), grown in standard medium containing high folate… 
1989
1989
(6R,6S)-5,8,10-trideaza-5,6,7,8-tetrahydrofolate and 6(R,6S)-5,8,10-trideaza-5,6,7,8-tetrahydropteroyl-L-ornithine as potential antifolates and antitumor agents.
(6R,6S)-5,8,10-Trideaza-5,6,7,8-tetrahydropteroic acid was synthesized in several steps from 4,4-(ethylenedioxy)-cyclohexanone… 
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