Antifolates in cancer therapy: structure, activity and mechanisms of drug resistance
N Gonen, YG Assaraf - Drug Resistance Updates, 2012 - Elsevier
In the past 65 years, antifolates targeting folate metabolism played a pivotal role in drug
treatment of malignant, microbial, parasitic and chronic inflammatory diseases. Drug …
treatment of malignant, microbial, parasitic and chronic inflammatory diseases. Drug …
Molecular basis of antifolate resistance
YG Assaraf - Cancer and Metastasis Reviews, 2007 - Springer
Folates play a key role in one-carbon metabolism essential for the biosynthesis of purines,
thymidylate and hence DNA replication. The antifolate methotrexate has been rationally …
thymidylate and hence DNA replication. The antifolate methotrexate has been rationally …
The major facilitative folate transporters solute carrier 19A1 and solute carrier 46A1: biology and role in antifolate chemotherapy of cancer
This review summarizes the biology of the major facilitative membrane transporters, the
reduced folate carrier (RFC)(Solute Carrier 19A1) and the proton-coupled folate transporter …
reduced folate carrier (RFC)(Solute Carrier 19A1) and the proton-coupled folate transporter …
Folate and antifolate pharmacology.
B Kamen - Seminars in oncology, 1997 - europepmc.org
Folic acid is a water-soluble vitamin associated with the other B vitamins. In its fully reduced
form (tetrahydrofolate), folate serves as a 1-carbon donor for synthesis of purines and …
form (tetrahydrofolate), folate serves as a 1-carbon donor for synthesis of purines and …
Antifolates targeted specifically to the folate receptor
AL Jackman, DS Theti, DD Gibbs - Advanced drug delivery reviews, 2004 - Elsevier
Most antifolate drugs are efficiently transported by the reduced-folate carrier (RFC).
However, several also bind with high affinity to the α-isoform of the folate receptor (α-FR) …
However, several also bind with high affinity to the α-isoform of the folate receptor (α-FR) …
Resistance to antifolates
R Zhao, ID Goldman - Oncogene, 2003 - nature.com
The antifolates were the first class of antimetabolites to enter the clinics more than 50 years
ago. Over the following decades, a full understanding of their mechanisms of action and …
ago. Over the following decades, a full understanding of their mechanisms of action and …
The proton-coupled folate transporter: impact on pemetrexed transport and on antifolates activities compared with the reduced folate carrier
The reduced folate carrier (RFC) and the proton-coupled folate transporter (PCFT) are
ubiquitously expressed in normal and malignant mammalian tissues and in human solid …
ubiquitously expressed in normal and malignant mammalian tissues and in human solid …
Structures of human folate receptors reveal biological trafficking states and diversity in folate and antifolate recognition
AS Wibowo, M Singh, KM Reeder… - Proceedings of the …, 2013 - National Acad Sciences
Antifolates, folate analogs that inhibit vitamin B9 (folic acid)-using cellular enzymes, have
been used over several decades for the treatment of cancer and inflammatory diseases …
been used over several decades for the treatment of cancer and inflammatory diseases …
Biology of the major facilitative folate transporters SLC19A1 and SLC46A1
Z Hou, LH Matherly - Current topics in membranes, 2014 - Elsevier
This chapter focuses on the biology of the major facilitative membrane folate transporters,
the reduced folate carrier (RFC), and the proton-coupled folate transporter (PCFT). Folates …
the reduced folate carrier (RFC), and the proton-coupled folate transporter (PCFT). Folates …
The role of multidrug resistance efflux transporters in antifolate resistance and folate homeostasis
YG Assaraf - Drug Resistance Updates, 2006 - Elsevier
Members of the ATP-binding cassette (ABC) transporters including P-glycoprotein
(Pgp/ABCB1), multidrug resistance proteins (MRPs/ABCC) as well as breast cancer …
(Pgp/ABCB1), multidrug resistance proteins (MRPs/ABCC) as well as breast cancer …