The folate receptor β as a macrophage-mediated imaging and therapeutic target in rheumatoid arthritis

DMSH Chandrupatla, CFM Molthoff… - Drug Delivery and …, 2019 - Springer
Macrophages play a key role in the pathophysiology of rheumatoid arthritis (RA). Notably,
positive correlations have been reported between synovial macrophage infiltration and …

Antivitamins for medicinal applications

F Zelder, M Sonnay, L Prieto - ChemBioChem, 2015 - Wiley Online Library
Antivitamins represent a broad class of compounds that counteract the essential effects of
vitamins. The symptoms triggered by such antinutritional factors resemble those of vitamin …

An insight into synthetic strategies and recent developments of dihydrofolate reductase inhibitors

P Chawla, G Teli, RK Gill, RK Narang - ChemistrySelect, 2021 - Wiley Online Library
The dihydrofolate reductase (DHFR) is a significant target in cancer, microbial infection,
fungal infection, malaria, leishmaniasis, and tuberculosis, among other diseases. The DHFR …

6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor α and the Proton-Coupled Folate Transporter in Human …

L Wang, A Wallace, S Raghavan, SM Deis… - Journal of medicinal …, 2015 - ACS Publications
2-Amino-4-oxo-6-substituted-pyrrolo [2, 3-d] pyrimidine antifolate thiophene regioisomers of
AGF94 (4) with a thienoyl side chain and three-carbon bridge lengths [AGF150 (5) and …

The promise and challenges of exploiting the proton-coupled folate transporter for selective therapeutic targeting of cancer

LH Matherly, Z Hou, A Gangjee - Cancer chemotherapy and …, 2018 - Springer
This review considers the “promise” of exploiting the proton-coupled folate transporter
(PCFT) for selective therapeutic targeting of cancer. PCFT was discovered in 2006 and was …

Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the …

LK Golani, A Wallace-Povirk, SM Deis… - Journal of medicinal …, 2016 - ACS Publications
Targeted antifolates with heteroatom replacements of the carbon vicinal to the phenyl ring in
1 by N (4), O (8), or S (9), or with N-substituted formyl (5), acetyl (6), or trifluoroacetyl (7) …

Fluorine-Substituted Pyrrolo[2,3-d]Pyrimidine Analogues with Tumor Targeting via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and …

M Ravindra, MR Wilson, N Tong… - Journal of medicinal …, 2018 - ACS Publications
Novel fluorinated 2-amino-4-oxo-6-substituted pyrrolo [2, 3-d] pyrimidine analogues 7–12
were synthesized and tested for selective cellular uptake by folate receptors (FRs) α and β or …

Unnatural Amino Acids: Strategies, Designs, and Applications in Medicinal Chemistry and Drug Discovery

KK Sharma, K Sharma, K Rao, A Sharma… - Journal of Medicinal …, 2024 - ACS Publications
Peptides can operate as therapeutic agents that sit within a privileged space between small
molecules and larger biologics. Despite examples of their potential to regulate receptors and …

Biology and therapeutic applications of the proton-coupled folate transporter

LH Matherly, M Schneider, A Gangjee… - Expert opinion on drug …, 2022 - Taylor & Francis
Introduction The proton-coupled folate transporter (PCFT; SLC46A1) was discovered in
2006 as the principal mechanism by which folates are absorbed in the intestine and the …

The influence of intramolecular sulfur–lone pair interactions on small-molecule drug design and receptor binding

BM Hudson, E Nguyen, DJ Tantillo - Organic & biomolecular chemistry, 2016 - pubs.rsc.org
Sulfur–lone pair interactions are important conformational control elements in sulfur-
containing heterocycles that abound in pharmaceuticals, natural products, agrochemicals …