» Articles » PMID: 22520983

The Antifolates

Overview
Specialties Hematology
Oncology
Date 2012 Apr 24
PMID 22520983
Citations 129
Authors
Affiliations
Soon will be listed here.
Abstract

This article focuses on the cellular, biochemical, and molecular pharmacology of antifolates and how a basic understanding of the mechanism of action of methotrexate, its cytotoxic determinants, mechanisms of resistance, and transport into and out of cells has led to the development of a new generation of antifolates, a process that continues in the laboratory and in the clinics. New approaches to folate-based cancer chemotherapy are described based on the targeted delivery of drugs to malignant cells.

Citing Articles

Folate receptor alpha for cancer therapy: an antibody and antibody-drug conjugate target coming of age.

Liu Y, Chen X, Evan T, Esapa B, Chenoweth A, Cheung A MAbs. 2025; 17(1):2470309.

PMID: 40045156 PMC: 11901361. DOI: 10.1080/19420862.2025.2470309.


DHFR2 RNA directly regulates dihydrofolate reductase and its expression level impacts folate one carbon metabolism.

Drago P, Bookey N, Leung K, Henry M, Meleady P, Greene N FASEB J. 2025; 39(4):e70391.

PMID: 39957677 PMC: 11831416. DOI: 10.1096/fj.202401039RR.


Peptide hydrogel-drug conjugates for tailored disease treatment.

Cauwenbergh T, Ballet S, Martin C Mater Today Bio. 2025; 31:101423.

PMID: 39944533 PMC: 11815290. DOI: 10.1016/j.mtbio.2024.101423.


Conditional lethality profiling reveals anticancer mechanisms of action and drug-nutrient interactions.

Flickinger K, Wilson K, Rossiter N, Hunger A, Vishwasrao P, Lee T Sci Adv. 2024; 10(40):eadq3591.

PMID: 39365851 PMC: 11451515. DOI: 10.1126/sciadv.adq3591.


Low dose methotrexate impaired T cell transmigration through down-regulating CXCR4 expression in rheumatoid arthritis (RA).

Ding L, Park D, Gao B, Wu L, Li M, Abedelhakim H Arthritis Res Ther. 2024; 26(1):173.

PMID: 39350214 PMC: 11440717. DOI: 10.1186/s13075-024-03403-9.


References
1.
Salazar M, Ratnam M . The folate receptor: what does it promise in tissue-targeted therapeutics?. Cancer Metastasis Rev. 2007; 26(1):141-52. DOI: 10.1007/s10555-007-9048-0. View

2.
Allegra C, Chabner B, Drake J, Lutz R, Rodbard D, Jolivet J . Enhanced inhibition of thymidylate synthase by methotrexate polyglutamates. J Biol Chem. 1985; 260(17):9720-6. View

3.
Reddy J, Xu L, Parker N, Vetzel M, Leamon C . Preclinical evaluation of (99m)Tc-EC20 for imaging folate receptor-positive tumors. J Nucl Med. 2004; 45(5):857-66. View

4.
Allegra C, Drake J, Jolivet J, Chabner B . Inhibition of phosphoribosylaminoimidazolecarboxamide transformylase by methotrexate and dihydrofolic acid polyglutamates. Proc Natl Acad Sci U S A. 1985; 82(15):4881-5. PMC: 390461. DOI: 10.1073/pnas.82.15.4881. View

5.
Braus N, Elliott D . Advances in the pathogenesis and treatment of IBD. Clin Immunol. 2009; 132(1):1-9. PMC: 2693446. DOI: 10.1016/j.clim.2009.02.006. View