Abstract: Disclosed are azotomycin prodrugs their use in treating diseases, disorders, or conditions associated with excess and/or aberrant glutamine utilization, including cancer.

Abstract: Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

Abstract: Methods for the use of prodrugs of itaconic acid and 1- and 4-methyl itaconic acid for inducing hair growth and treating an inflammatory, or immune activation (adaptive or innate), skin condition or other condition associated with hair loss are disclosed.

Abstract: Prodrugs of testosterone and their use in alleviating, improving or reducing a risk of developing one or more conditions associated with androgen deprivation therapy (ADT), including orchiectomy or administration of a luteinizing hormone-releasing hormone agonist/antagonist, for the treatment of prostate cancer, including metastatic prostate cancer. In some aspects the prodrugs can be administered intranasally to target the central nervous system.

Abstract: The use of a class of prodrugs of 2-PMPA that alter tissue distribution of 2-PMPA to non-prostate tissues is disclosed. The presently disclosed prodrugs preferentially distribute to healthy tissues including the kidney, lacrimal glands, and salivary glands, which represent sites of off-target binding and toxicity for PSMA-targeted prostate cancer imaging agents and therapies. Accordingly, the 2-PMPA prodrugs can be used to pretreat, bind to, and shield the kidney and salivary glands from PSMA-targeted cytotoxic or radiotherapy.

Abstract: Methods for the use of prodrugs of itaconic acid and 1- and 4-methyl itaconic acid for inducing hair growth and treating an inflammatory, or immune activation (adaptive or innate), skin condition or other condition associated with hair loss are disclosed.

Abstract: Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

Abstract: A dendrimer formulation, such as a PAMAM dendrimer or a multiarm PEG polymeric formulation has been developed for systemic administration to the brain or central nervous system. In the preferred embodiment, the dendrimers are in the form of dendrimer nanoparticles comprising poly(amidoamine)(PAMAM) hydroxyl-terminated dendrimers covalently linked to at least one therapeutic, prophylactic or diagnostic agent for treatment of one or more symptoms of neurodegenerative, neurodevelopmental or neurological disorders such as Rett syndrome of autism spectrum disorders. D6 generation dendrimers provide significantly enhanced uptake into areas of brain injury, providing a means for diagnosis as well as drug delivery.

Abstract: Methods for treating age-related sarcopenia and/or enhancing longevity by administering one or more GCPII inhibitors, wherein the one or more GCPII inhibitors are selected from a phosphonate-based GCPII inhibitor, a phosphinate-based GCPII inhibitor, a phosphoramidate-based GCPII inhibitor, a thiol-based inhibitor, a hydroxamate-based inhibitor, and a urea-glutamate based GCPII inhibitor, including one or more of 2-PMPA and prodrugs thereof, L-DOPA, D-DOPA, caffeic acid, and prodrugs thereof, a hydroxamate-based prodrug, and a dendrimer 2-PMPA conjugate are disclosed.

Abstract: Small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer or HIV-1, are provided.

Abstract: Glutamine antagonists and their use for treating oncological, immunological, and neurological diseases are disclosed. Also disclosed are methods for treating an oncological, immunological, infectious or neurological disease or disorder, the method comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof. Also disclosed are methods of enhancing the effects of an immune checkpoint inhibitor, enabling a subject to respond to an immune checkpoint inhibitor, or enabling the toxicity or the dose or number of treatments with an immune checkpoint inhibitor to be reduced, comprising administering to a subject in need of treatment thereof a therapeutically effective amount of a glutamine antagonist of the disclosure or the pharmaceutical composition thereof, and an immune checkpoint inhibitor.

Abstract: Caffeic Acid, L-DOPA, and D-DOPA and prodrugs thereof for treating a disease, condition, or disorder associated with excess glutamate carboxypeptidase II (GCP-II) are disclosed.

Abstract: Provided are glutamine antagonists and prodrugs of glutamine analogs having formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, and X are as defined as set forth in the specification, for use in preventing and/or treating acute kidney injury.

Abstract: Compositions of dendrimers conjugated with one or more glutamine antagonist(s) that inhibit glutamine metabolism, preferably in activated microglia, and methods of use thereof for treating, alleviating, and/or preventing one or more neurological, oncological, and/or immune disorders associated with pathogenic or dysregulated glutamine-dependent pathways and/or glutamate transmission, have been developed. Dendrimers conjugated with one or more glutamine antagonists effectively inhibit the activity of glutaminase without any systemic toxicity. Dendrimers conjugated with one or more glutamine antagonists accumulate in activated microglia associated with the injured or diseased cells and tissues.

Abstract: Prodrugs of itaconic acid and 1- and 4-methyl itaconic acid and their use for treating a disease, disorder, or condition associated with inflammation are disclosed.

Abstract: Methods for the use of prodrugs of itaconic acid and 1- and 4-methyl itaconic acid for inducing hair growth and treating an inflammatory, or immune activation (adaptive or innate), skin condition or other condition associated with hair loss are disclosed.

Abstract: Prodrugs of small molecule inhibitors of neutral sphingomyelinase 2 (nSMase2) and their use for treating neurodegenerative diseases, such as, neurodegenerative diseases associated with high levels of ceramide, including, but not limited to Alzheimer's disease (AD), HIV-associated neurocognitive disorder (HAND), multiple sclerosis (MS), and amyotrophic lateral sclerosis (ALS), and, in other aspects, for treating cancer, are provided.

Abstract: The present disclosure provides prodrugs of 6-diazo-5-oxo-L-norleucine (DON) for use in treating or preventing a disease, disorder, or condition in which the inhibition of glutamine-utilizing enzymes provides a benefit.

Abstract: Methods for treating a Human Immunodeficiency Virus (HIV) infection comprising administering to a subject in need of treatment thereof an effective amount of a small molecule nSMase2 inhibitor.

Abstract: Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.