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View article: Enolase inhibitors as therapeutic leads for Naegleria fowleri infection
Enolase inhibitors as therapeutic leads for Naegleria fowleri infection Open
Infections with the pathogenic free-living amoebae Naegleria fowleri can lead to life-threatening illnesses including catastrophic primary amoebic meningoencephalitis (PAM). Efficacious treatment options for these infections are lacking an…
View article: cGMP compliant one-step, one-pot automated [18F]FBnTP production for clinical imaging of mitochondrial activity
cGMP compliant one-step, one-pot automated [18F]FBnTP production for clinical imaging of mitochondrial activity Open
Background 4-[ 18 F]fluorobenzyl-triphenylphosphonium ([ 18 F]FBnTP) is a lipophilic cation PET tracer. The cellular uptake of [ 18 F]FBnTP is correlated with oxidative phosphorylation by mitochondria, which has been associated with multip…
View article: Correction: Cook et al. An Optimized Bioassay for Screening Combined Anticoronaviral Compounds for Efficacy against Feline Infectious Peritonitis Virus with Pharmacokinetic Analyses of GS-441524, Remdesivir, and Molnupiravir in Cats. Viruses 2022, 14, 2429
Correction: Cook et al. An Optimized Bioassay for Screening Combined Anticoronaviral Compounds for Efficacy against Feline Infectious Peritonitis Virus with Pharmacokinetic Analyses of GS-441524, Remdesivir, and Molnupiravir in Cats. Viruses 2022, 14, 2429 Open
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View article: Enolase inhibitors as therapeutic leads for<i>Naegleria fowleri</i>infection
Enolase inhibitors as therapeutic leads for<i>Naegleria fowleri</i>infection Open
Infections with the pathogenic free-living amoebae Naegleria fowleri can lead to life-threatening illnesses including catastrophic primary amebic meningoencephalitis (PAM). Efficacious treatment options for these infections are lacking and…
View article: Overexpression of ameloblastin in secretory ameloblasts results in demarcated, hypomineralized opacities in enamel
Overexpression of ameloblastin in secretory ameloblasts results in demarcated, hypomineralized opacities in enamel Open
Introduction: Developmental defects of the enamel manifest before tooth eruption and include amelogenesis imperfecta, a rare disease of underlying gene mutations, and molar–incisor hypomineralization (MIH), a prevalent disease in children …
View article: Enolase Inhibitors as Early Lead Therapeutics against Trypanosoma brucei
Enolase Inhibitors as Early Lead Therapeutics against Trypanosoma brucei Open
Glucose metabolism is critical for the African trypanosome, Trypanosoma brucei, serving as the lone source of ATP production for the bloodstream form (BSF) parasite in the glucose-rich environment of the host blood. Recently, phosphonate i…
View article: An Optimized Bioassay for Screening Combined Anticoronaviral Compounds for Efficacy against Feline Infectious Peritonitis Virus with Pharmacokinetic Analyses of GS-441524, Remdesivir, and Molnupiravir in Cats
An Optimized Bioassay for Screening Combined Anticoronaviral Compounds for Efficacy against Feline Infectious Peritonitis Virus with Pharmacokinetic Analyses of GS-441524, Remdesivir, and Molnupiravir in Cats Open
Feline infectious peritonitis (FIP) is a fatal disease of cats that currently lacks licensed and affordable vaccines or antiviral therapeutics. The disease has a spectrum of clinical presentations including an effusive (“wet”) form and non…
View article: Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of <i>ENO1</i>-Deleted Cancers
Prodrugs of a 1-Hydroxy-2-oxopiperidin-3-yl Phosphonate Enolase Inhibitor for the Treatment of <i>ENO1</i>-Deleted Cancers Open
Cancers harboring homozygous deletion of the glycolytic enzyme enolase 1 (ENO1) are selectively vulnerable to inhibition of the paralogous isoform, enolase 2 (ENO2). A previous work described the sustained tumor regression activities of a …
View article: Quantification of phosphonate drugs by <sup>1</sup>H-<sup>31</sup>P HSQC shows that rats are better models of primate drug exposure than mice
Quantification of phosphonate drugs by <sup>1</sup>H-<sup>31</sup>P HSQC shows that rats are better models of primate drug exposure than mice Open
The phosphonate group is a key pharmacophore in many anti-viral, anti-microbial, and anti-neoplastic drugs. Due to its high polarity and short retention time, detecting and quantifying such phosphonate-containing drugs with LC/MS-based met…
View article: Pharmacokinetics of Orally Administered GS-441524 in Dogs
Pharmacokinetics of Orally Administered GS-441524 in Dogs Open
Despite being FDA-approved for COVID-19, the clinical efficacy of remdesivir (Veklury ® ) remains contentious. We previously pointed out pharmacokinetic, pharmacodynamic and toxicology reasons for why its parent nucleoside GS-441524, is be…
View article: Impaired Anaplerosis Is a Major Contributor to Glycolysis Inhibitor Toxicity in Glioma
Impaired Anaplerosis Is a Major Contributor to Glycolysis Inhibitor Toxicity in Glioma Open
Reprogramming of metabolic pathways is crucial to satisfy the bioenergetic and biosynthetic demands and maintain the redox status of rapidly proliferating cancer cells. In tumors, the tricarboxylic acid (TCA) cycle generates biosynthetic i…
View article: Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study
Bioreducible Phosphonoamidate Pro-drug Inhibitor of Enolase: Proof of Concept Study Open
Glycolysis inhibition remains aspirational in cancer therapy. We recently described a promising phosphonate inhibitor of enolase for cancers harboring homozygous deletions of ENO1. Here, we describe the application of a nitroheterocycle ph…
View article: Expedient Method for Direct Mono-amidation of Phosphonic and Phosphoric Acids
Expedient Method for Direct Mono-amidation of Phosphonic and Phosphoric Acids Open
Mono-amidated P(V) pro-drugs predominately contribute to the vastly improved delivery of phosphate and phosphonate-containing anti-viral/cancer nucleotide analogues. However, synthetic approaches towards their formation are often harsh and…
View article: Aliphatic Amines are Viable Pro-drug Moieties in Phosphonoamidate Drugs
Aliphatic Amines are Viable Pro-drug Moieties in Phosphonoamidate Drugs Open
Phosphate and phosphonates containing a single P-N bond are frequently used pro-drug motifs to improve cell permeability of these otherwise anionic moieties. Upon entry into the cell, the P-N bond is cleaved by phosphoramidases to release …
View article: Expedient Method for Direct Mono-amidation of Phosphonic and Phosphoric Acids
Expedient Method for Direct Mono-amidation of Phosphonic and Phosphoric Acids Open
Mono-amidated P(V) pro-drugs predominately contribute to the vastly improved delivery of phosphate and phosphonate-containing anti-viral/cancer nucleotide analogues. However, synthetic approaches towards their formation are often harsh and…
View article: An Enolase Inhibitor for the Targeted Treatment of ENO1-Deleted Cancers
An Enolase Inhibitor for the Targeted Treatment of ENO1-Deleted Cancers Open
Metabolomic and figure source data discussed in the manuscript "An Enolase Inhibitor for the Targeted Treatment of ENO1-Deleted Cancers" are included
View article: Endocytosis and Enamel Formation
Endocytosis and Enamel Formation Open
Enamel formation requires consecutive stages of development to achieve its characteristic extreme mineral hardness. Mineralization depends on the initial presence then removal of degraded enamel proteins from the matrix via endocytosis. Th…