Clinical development of metabolic inhibitors for oncology

KM Lemberg, SS Gori, T Tsukamoto… - The Journal of …, 2022 - Am Soc Clin Investig
Metabolic inhibitors have been used in oncology for decades, dating back to antimetabolites
developed in the 1940s. In the past 25 years, there has been increased recognition of …

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead …

MAM Subbaiah, J Rautio, NA Meanwell - Chemical Society Reviews, 2024 - pubs.rsc.org
The delivery of a drug to a specific organ or tissue at an efficacious concentration is the
pharmacokinetic (PK) hallmark of promoting effective pharmacological action at a target site …

Troriluzole rescues glutamatergic deficits, amyloid and tau pathology, and synaptic and memory impairments in 3xTg‐AD mice

J Pfitzer, PD Pinky, S Perman, E Redmon… - Journal of …, 2025 - Wiley Online Library
Alzheimer's disease (AD) is a neurodegenerative condition in which clinical symptoms are
highly correlated with the loss of glutamatergic synapses. While later stages of AD are …

[HTML][HTML] Riluzole and novel naphthalenyl substituted aminothiazole derivatives prevent acute neural excitotoxic injury in a rat model of temporal lobe epilepsy

T Kyllo, V Singh, H Shim, S Latika, HM Nguyen… - …, 2023 - Elsevier
Epileptogenic seizures, or status epilepticus (SE), leads to excitotoxic injury in hippocampal
and limbic neurons in the kainic acid (KA) animal model of temporal lobe epilepsy (TLE) …

Neuroendocrine factors in melanoma pathogenesis

C Scheau, C Draghici, MA Ilie, M Lupu, I Solomon… - Cancers, 2021 - mdpi.com
Simple Summary Melanoma is a very aggressive and fatal malignant tumor. While curable if
diagnosed in its early stages, advanced melanoma, despite the complex therapeutic …

Current Therapy in Amyotrophic lateral sclerosis (ALS): a review on Past and Future Therapeutic Strategies

Y Wei, S Zhong, H Yang, X Wang, B Lv, Y Bian… - European Journal of …, 2024 - Elsevier
Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease that affects the first
and second motoneurons (MNs), associated with muscle weakness, paralysis and finally …

Design, synthesis, and pharmacokinetic evaluation of phosphate and amino acid ester prodrugs for improving the oral bioavailability of the HIV-1 protease inhibitor …

M AM Subbaiah, S Mandlekar, S Desikan… - Journal of Medicinal …, 2019 - ACS Publications
Phosphate and amino acid prodrugs of the HIV-1 protease inhibitor (PI) atazanavir (1) were
prepared and evaluated to address solubility and absorption limitations. While the …

Synthesis and biological evaluation of parthenolide derivatives with reduced toxicity as potential inhibitors of the NLRP3 inflammasome

Y Ou, P Sun, N Wu, H Chen, D Wu, W Hu… - Bioorganic & Medicinal …, 2020 - Elsevier
Parthenolide (PTL) can target NLRP3 inflammasome to treat inflammation and its related
disease, but its cytotoxicity limits further development as an anti-inflammatory drug. A series …

Troriluzole inhibits methamphetamine place preference in rats and normalizes methamphetamine-evoked glutamate carboxypeptidase II (GCPII) protein levels in the …

S Wiah, A Roper, P Zhao, A Shekarabi… - Drug and alcohol …, 2023 - Elsevier
Riluzole, approved to manage amyotrophic lateral sclerosis, is mechanistically unique
among glutamate-based therapeutics because it reduces glutamate transmission through a …

Identification of a 3-β-homoalanine conjugate of brusatol with reduced toxicity in mice

N Hwang, Y Pei, J Clement, ES Robertson… - Bioorganic & medicinal …, 2020 - Elsevier
Brusatol, a quassinoid natural product, is effective against multiple diseases including
hematologic malignancies, as we reported recently by targeting the PI3Kγ isoform, but …