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 …

[HTML][HTML] The biological chemistry of folate receptors

AC Antony - Blood, 1992 - Elsevier
THE ESSENTIAL role of intracellular folates in effecting one-carbon transfers in critical
enzyme systems for DNA synthesis is well established. 1., 2., 3. This has led to extensive …

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 …

A miR-24 microRNA binding-site polymorphism in dihydrofolate reductase gene leads to methotrexate resistance

PJ Mishra, R Humeniuk, PJ Mishra… - Proceedings of the …, 2007 - National Acad Sciences
MicroRNAs are predicted to regulate≈ 30% of all human genes by targeting sequences in
their 3′ UTR. Polymorphisms in 3′ UTR of several genes have been reported to affect …

Design and Synthesis of Classical and Nonclassical 6-Arylthio-2,4-diamino-5-ethylpyrrolo[2,3-d]pyrimidines as Antifolates

A Gangjee, Y Zeng, T Talreja, JJ McGuire… - Journal of medicinal …, 2007 - ACS Publications
The classical antifolate N-{4-[(2, 4-diamino-5-ethyl-7 H-pyrrolo [2, 3-d] pyrimidin-6-yl)
sulfanyl] benzoyl}-l-glutamic acid (2) and 15 nonclassical analogues (3− 17) were …

Folate chemistry and metabolism

B Shane - Clinical Research and Regulatory Affairs, 2001 - Taylor & Francis
The vitamin folic acid was initially investigated as a dietary antianemia factor distinct from the
pernicious anemia factor [1] and a recent historical review details early studies on the …

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 …

[图书][B] Folate in health and disease

LB Bailey - 2009 - taylorfrancis.com
During the fifteen years since the bestselling first edition of Folate in Health and Disease
was published, there have been thousands of new research studies related to folate and its …

Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport

H Zeng, ZS Chen, MG Belinsky, PA Rea, GD Kruh - Cancer research, 2001 - AACR
We have recently determined that human multidrug resistance protein (MRP) 3, which
confers resistance to certain natural product agents and methotrexate (MTX), is competent in …

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 …