Prodrugs of phosphonates and phosphates: crossing the membrane barrier

AJ Wiemer, DF Wiemer - … Chemistry I: Asymmetric Synthesis and Bioactive …, 2015 - Springer
A substantial portion of metabolism involves transformation of phosphate esters, including
pathways leading to nucleotides and oligonucleotides, carbohydrates, isoprenoids and …

Phosphonate prodrugs: an overview and recent advances

KM Heidel, CS Dowd - Future medicinal chemistry, 2019 - Taylor & Francis
Phosphonates, often used as isosteric replacements for phosphates, can provide important
interactions with an enzyme. Due to their high charge at physiological pH, however …

Synthesis of a phosphoantigen prodrug that potently activates Vγ9Vδ2 T-lymphocytes

CHC Hsiao, X Lin, RJ Barney, RR Shippy, J Li… - Chemistry & biology, 2014 - cell.com
Phosphoantigen-sensitive Vγ9Vδ2 T cells are important responders to infections and
malignancy. However, the mechanisms by which phosphoantigens stimulate Vγ9Vδ2 T cells …

Prodrugs of pyrophosphates and bisphosphonates: disguising phosphorus oxyanions

ES Rudge, AHY Chan, FJ Leeper - RSC Medicinal Chemistry, 2022 - pubs.rsc.org
Pyrophosphates have important functions in living systems and thus pyrophosphate-
containing molecules and their more stable bisphosphonate analogues have the potential to …

Anti-tumor activity and immunotherapeutic potential of a bisphosphonate prodrug

Y Tanaka, M Iwasaki, K Murata-Hirai, K Matsumoto… - Scientific reports, 2017 - nature.com
Bisphosphonates have benefits in breast cancer and multiple myeloma patients and have
been used with adoptive immunotherapy with γδ T cells expressing Vγ2 Vδ2 TCRs …

Prenyltransferase inhibitors: treating human ailments from cancer to parasitic infections

JD Ochocki, MD Distefano - Medchemcomm, 2013 - pubs.rsc.org
The posttranslational modification of protein prenylation is a covalent lipid modification on
the C-terminus of substrate proteins that serves to enhance membrane affinity. Oncogenic …

Geranylgeranyl diphosphate synthase: an emerging therapeutic target

AJ Wiemer, DF Wiemer, RJ Hohl - Clinical Pharmacology & …, 2011 - Wiley Online Library
Proteins modified post‐translationally by geranylgeranylation have been implicated in
numerous cellular processes related to human disease. In recent years, the study of protein …

Lipophilic Pyridinium Bisphosphonates: Potent γδ T Cell Stimulators

Y Zhang, R Cao, F Yin, FY Lin, H Wang… - Angewandte Chemie …, 2010 - Wiley Online Library
Bisphosphonates such as risedronate and ibandronate are widely used to treat a variety of
bone resorption diseases, preventing protein prenylation and disrupting osteoclast …

The intermediate enzymes of isoprenoid metabolism as anticancer targets

AJ Wiemer, RJ Hohl, DF Wiemer - Anti-Cancer Agents in …, 2009 - ingentaconnect.com
Inhibitors of isoprenoid biosynthesis are widely used to treat human disease including
statins and nitrogenous bisphosphonates. Due to the importance of core human isoprenoid …

Potent triazole bisphosphonate inhibitor of geranylgeranyl diphosphate synthase

VS Wills, C Allen, SA Holstein… - ACS medicinal chemistry …, 2015 - ACS Publications
Studies of triazole bisphosphonates have resulted in identification of a potent inhibitor of
geranylgeranyl diphosphate synthase (IC50= 45 nM) with very good selectivity for this …