• Publications
  • Influence
Synthesis and biological evaluation of D-amino acid oxidase inhibitors.
D-amino acid oxidase (DAAO) catalyzes the oxidation of D-amino acids including d-serine, a full agonist at the glycine site of the NMDA receptor. A series of benzo[ d]isoxazol-3-ol derivatives wereExpand
  • 106
  • 9
Glutamate carboxypeptidase II inhibition protects motor neurons from death in familial amyotrophic lateral sclerosis models
Approximately 10% of cases of amyotrophic lateral sclerosis (ALS), a progressive and fatal degeneration that targets motor neurons (MNs), are inherited, and ≈20% of these cases of familial ALS (FALS)Expand
  • 103
  • 5
  • PDF
Still NAAG'ing After All These Years: The Continuing Pursuit of GCPII Inhibitors.
Nearly two decades ago, Joe Coyle published a single-authored review with the provocative title, The Nagging Question of the Function of N-Acetylaspartylglutamate (Coyle, 1997). In this review, CoyleExpand
  • 16
  • 3
High-affinity Near-infrared Fluorescent Small-molecule Contrast Agents for In Vivo Imaging of Prostate-specific Membrane Antigen
Surgical resection remains a definitive treatment for prostate cancer. Yet, prostate cancer surgery is performed without image guidance for tumor margin, extension beyond the capsule and lymph nodeExpand
  • 73
  • 2
Rational design of urea-based glutamate carboxypeptidase II (GCPII) inhibitors as versatile tools for specific drug targeting and delivery.
Glutamate carboxypeptidase II (GCPII), also known as prostate specific membrane antigen (PSMA), is an established prostate cancer marker and is considered a promising target for specific anticancerExpand
  • 25
  • 2
N-(Pivaloyloxy)alkoxy-carbonyl Prodrugs of the Glutamine Antagonist 6-Diazo-5-oxo-l-norleucine (DON) as a Potential Treatment for HIV Associated Neurocognitive Disorders.
Aberrant excitatory neurotransmission associated with overproduction of glutamate has been implicated in the development of HIV-associated neurocognitive disorders (HAND). The glutamine antagonistExpand
  • 22
  • 2
  • PDF
JHU-2545 Selectively Shields Salivary Glands and Kidneys during PSMA-Targeted Radiotherapy
PURPOSE Prostate-specific membrane antigen (PSMA) radiotherapy is a promising treatment for metastatic castration-resistant prostate cancer (mCRPC) with several beta or alpha particle-emittingExpand
  • 3
  • 2
Plasmodium falciparum, P. vivax, and P. malariae: a comparison of the active site properties of plasmepsins cloned and expressed from three different species of the malaria parasite.
Aspartic endopeptidases (plasmepsins) have been implicated in the degradation of hemoglobin in the erythrocytic stage of infection by Plasmodium falciparum. To develop new targets for drugExpand
  • 52
  • 1
Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.
We present here a structure-aided design of inhibitors targeting the active site as well as exosites of glutamate carboxypeptidase II (GCPII), a prostate cancer marker, preparing potent and selectiveExpand
  • 15
  • 1
Targeting glutamine metabolism enhances tumor specific immunity by modulating suppressive myeloid cells.
  • M. Oh, I. Sun, +17 authors J. Powell
  • Medicine, Chemistry
  • The Journal of clinical investigation
  • 23 April 2020
Myeloid cells comprise a major component of the tumor-microenvironment (TME) promoting tumor growth and immune evasion. By employing a novel small molecule inhibitor of glutamine metabolism, not onlyExpand
  • 19
  • 1
  • PDF