scholarly journals Synthesis, Biological, and Antitumor Activity of a Highly Potent 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Antifolate Inhibitor with Proton-Coupled Folate Transporter and Folate Receptor Selectivity over the Reduced Folate Carrier That Inhibits β-Glycinamide Ribonucleotide Formyltransferase

2011 ◽  
Vol 54 (20) ◽  
pp. 7150-7164 ◽  
Author(s):  
Lei Wang ◽  
Sita Kugel Desmoulin ◽  
Christina Cherian ◽  
Lisa Polin ◽  
Kathryn White ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Folate Receptor ◽  
Reduced Folate Carrier ◽  
Receptor Selectivity ◽  
Glycinamide Ribonucleotide Formyltransferase

scholarly journals Synthesis and Discovery of High Affinity Folate Receptor-Specific Glycinamide Ribonucleotide Formyltransferase Inhibitors with Antitumor Activity

2008 ◽  
Vol 51 (16) ◽  
pp. 5052-5063 ◽  
Author(s):  
Yijun Deng ◽  
Yiqiang Wang ◽  
Christina Cherian ◽  
Zhanjun Hou ◽  
Steven A. Buck ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Folate Receptor ◽  
Glycinamide Ribonucleotide Formyltransferase ◽  
High Affinity

scholarly journals Antitumor Activity of a Novel Double-Targeted System for Folate Receptor-Mediated Delivery of Mitomycin C

ACS Omega ◽  
2020 ◽  
Vol 5 (41) ◽  
pp. 26864-26870
Author(s):  
Yan Xu ◽  
Xiangmei Jin ◽  
Jun Zhang ◽  
Kun Wang ◽  
Xiaoyan Jin ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Mitomycin C ◽  
Folate Receptor

scholarly journals Folate Receptor–Specific Antitumor Activity of EC131, a Folate-Maytansinoid Conjugate

2007 ◽  
Vol 67 (13) ◽  
pp. 6376-6382 ◽  
Author(s):  
Joseph A. Reddy ◽  
Elaine Westrick ◽  
Hari K.R. Santhapuram ◽  
Stephen J. Howard ◽  
Michael L. Miller ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Folate Receptor

scholarly journals Upregulation of reduced folate carrier by vitamin D enhances brain folate uptake in mice lacking folate receptor alpha

2019 ◽  
Vol 116 (35) ◽  
pp. 17531-17540 ◽  
Author(s):  
Camille Alam ◽  
Susanne Aufreiter ◽  
Constantine J. Georgiou ◽  
Md. Tozammel Hoque ◽  
Richard H. Finnell ◽  
...  
Keyword(s):  
Vitamin D ◽  
Choroid Plexus ◽  
Folate Receptor ◽  
Functional Expression ◽  
Transport Systems ◽  
Reduced Folate Carrier ◽  
Folate Transport ◽  
Folate Receptor Alpha ◽  
Receptor Alpha ◽  
Neurometabolic Disorders

Folates are critical for central nervous system function. Folate transport is mediated by 3 major pathways, reduced folate carrier (RFC), proton-coupled folate transporter (PCFT), and folate receptor alpha (FRα/Folr1), known to be regulated by ligand-activated nuclear receptors. Cerebral folate delivery primarily occurs at the choroid plexus through FRα and PCFT; inactivation of these transport systems can result in very low folate levels in the cerebrospinal fluid causing childhood neurodegenerative disorders. These disorders have devastating effects in young children, and current therapeutic approaches are not sufficiently effective. Our group has previously reported in vitro that functional expression of RFC at the blood–brain barrier (BBB) and its upregulation by the vitamin D nuclear receptor (VDR) could provide an alternative route for brain folate uptake. In this study, we further demonstrated in vivo, using Folr1 knockout (KO) mice, that loss of FRα led to a substantial decrease of folate delivery to the brain and that pretreatment of Folr1 KO mice with the VDR activating ligand, calcitriol (1,25-dihydroxyvitamin D3), resulted in over a 6-fold increase in [13C5]-5-formyltetrahydrofolate ([13C5]-5-formylTHF) concentration in brain tissues, with levels comparable to wild-type animals. Brain-to-plasma concentration ratio of [13C5]-5-formylTHF was also significantly higher in calcitriol-treated Folr1 KO mice (15-fold), indicating a remarkable enhancement in brain folate delivery. These findings demonstrate that augmenting RFC functional expression at the BBB could effectively compensate for the loss of Folr1-mediated folate uptake at the choroid plexus, providing a therapeutic approach for neurometabolic disorders caused by defective brain folate transport.

scholarly journals Association of folate receptor (folr1, folr2, folr3) and reduced folate carrier (slc19a1) genes with meningomyelocele

2010 ◽  
Vol 88 (8) ◽  
pp. 689-694 ◽  
Author(s):  
Michelle R. O'Byrne ◽  
Kit Sing Au ◽  
Alanna C. Morrison ◽  
Jone-Ing Lin ◽  
Jack M. Fletcher ◽  
...  
Keyword(s):  
Folate Receptor ◽  
Reduced Folate Carrier
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