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 …

Mechanisms of membrane transport of folates into cells and across epithelia

R Zhao, N Diop-Bove, M Visentin… - Annual review of …, 2011 - annualreviews.org
Until recently, the transport of folates into cells and across epithelia has been interpreted
primarily within the context of two transporters with high affinity and specificity for folates, the …

The human proton-coupled folate transporter: Biology and therapeutic applications to cancer

SK Desmoulin, Z Hou, A Gangjee… - Cancer biology & …, 2012 - Taylor & Francis
This review summarizes the biology of the proton-coupled folate transporter (PCFT). PCFT
was identified in 2006 as the primary transporter for intestinal absorption of dietary folates …

The intestinal absorption of folates

M Visentin, N Diop-Bove, R Zhao… - Annual review of …, 2014 - annualreviews.org
The properties of intestinal folate absorption were documented decades ago. However, it
was only recently that the proton-coupled folate transporter (PCFT) was identified and its …

Folate and thiamine transporters mediated by facilitative carriers (SLC19A1-3 and SLC46A1) and folate receptors

R Zhao, ID Goldman - Molecular aspects of medicine, 2013 - Elsevier
The reduced folate carrier (RFC, SLC19A1), thiamine transporter-1 (ThTr1, SLC19A2) and
thiamine transporter-2 (ThTr2, SLC19A3) evolved from the same family of solute carriers …

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 …

Chemotherapeutic drug-induced ABCG2 promoter demethylation as a novel mechanism of acquired multidrug resistance

EE Bram, M Stark, S Raz, YG Assaraf - Neoplasia, 2009 - Elsevier
ABCG2 is an efflux transporter conferring multidrug resistance (MDR) on cancer cells.
However, the initial molecular events leading to its up-regulation in MDR tumor cells are …

The DNA demethylase TET1 modifies the impact of maternal folic acid status on embryonic brain development

L Chen, BK van der Veer, Q Chen… - EMBO …, 2025 - embopress.org
Folic acid (FA) is well known to prevent neural tube defects (NTDs), but we do not know why
many human NTD cases still remain refractory to FA supplementation. Here, we investigate …

Folate transport and one-carbon metabolism in targeted therapies of epithelial ovarian cancer

A Wallace-Povirk, Z Hou, MJ Nayeen, A Gangjee… - Cancers, 2021 - mdpi.com
Simple Summary New therapies are urgently needed for ovarian cancer, the most lethal
malignancy in women. To identify new approaches for targeting ovarian cancer, metabolic …

Folylpoly-γ-glutamate synthetase: a key determinant of folate homeostasis and antifolate resistance in cancer

S Raz, M Stark, YG Assaraf - Drug Resistance Updates, 2016 - Elsevier
Mammalians are devoid of autonomous biosynthesis of folates and hence must obtain them
from the diet. Reduced folate cofactors are B9-vitamins which play a key role as donors of …