The evolution of small molecule enzyme activators

LF Dow, AM Case, MP Paustian, BR Pinkerton… - RSC Medicinal …, 2023 - pubs.rsc.org
There is a myriad of enzymes within the body responsible for maintaining homeostasis by
providing the means to convert substrates to products as and when required. Physiological …

Permeability of metformin across an in vitro blood–brain barrier model during normoxia and oxygen-glucose deprivation conditions: role of organic cation transporters …

S Sharma, Y Zhang, KA Akter, S Nozohouri, SR Archie… - Pharmaceutics, 2023 - mdpi.com
Our lab previously established that metformin, a first-line type two diabetes treatment,
activates the Nrf2 pathway and improves post-stroke recovery. Metformin's brain …

Evaluation of systemic and brain pharmacokinetic parameters for repurposing metformin using intravenous bolus administration

S Sharma, Y Zhang, D Patel, KA Akter, S Bagchi… - The Journal of …, 2025 - Elsevier
Metformin's potential in treating ischemic stroke and neurodegenerative conditions is of
growing interest. Yet, the absence of established systemic and brain pharmacokinetic (PK) …

Small molecule neurolysin activators, potential multi-mechanism agents for ischemic stroke therapy

SH Esfahani, TJ Abbruscato, PC Trippier… - Expert Opinion on …, 2022 - Taylor & Francis
As we often learn from nature, elucidation and understanding of the brain's endogenous self-
protective and recovery mechanisms have been an emerging approach in the stroke …

Discovery of the Next Generation of Non-peptidomimetic Neurolysin Activators with High Blood-Brain Barrier Permeability: A Pharmacokinetics Study in Healthy and …

Y Zhang, S Sharma, S Jonnalagadda, S Kumari… - Pharmaceutical …, 2023 - Springer
Purpose There is growing interest in seeking pharmacological activation of neurolysin (Nln)
for stroke treatment. Discovery of central nervous system drugs remains challenging due to …

Mucoadhesive chitosan-poly (lactic-co-glycolic acid) nanoparticles for intranasal delivery of quetiapine–Development & characterization in physiologically relevant 3D …

DG Gadhave, M Quadros, AR Ugale, M Goyal… - International Journal of …, 2024 - Elsevier
Quetiapine hemifumarate (QF) delivery to the CNS via conventional formulations is
challenging due to poor solubility and lower oral bioavailability (9%). Similarly, many other …

Characterization of a Nonselective Opioid Receptor Functional Antagonist: Implications for Development as a Novel Opioid Dependence Medication

S Shahbazi Nia, YT Ortiz… - ACS Pharmacology & …, 2024 - ACS Publications
Opioids represent the most extensive category of abused substances in the United States,
and the number of fatalities caused by these drugs exceeds those associated with all other …

Imidazole Bioisostere Activators of Endopeptidase Neurolysin with Enhanced Potency and Metabolic Stability

MS Rahman, S Hadi Esfahani, Y Zhang… - ACS Medicinal …, 2024 - ACS Publications
The peptidase neurolysin (Nln) has been validated as a potential target for developing
therapeutics for ischemic stroke (IS). Overexpression of Nln in a mouse model of IS provides …

Systemic and Brain Pharmacokinetics of Milnacipran in Mice: Comparison of Intraperitoneal and Intravenous Administration

S Bagchi, E Nozohouri, Y Ahn, D Patel, U Bickel… - Pharmaceutics, 2023 - mdpi.com
Milnacipran is a dual serotonin and norepinephrine reuptake inhibitor, clinically used for the
treatment of major depression or fibromyalgia. Currently, there are no studies reporting the …

Loss of Nln Suppresses Lung Cancer Progression by Inducing Ferroptosis Through Downregulating M6a Methylation of Gpx4

L Liu, Y Ni, Y Yang, G Zhang, S Mao, N Chao… - Available at SSRN … - papers.ssrn.com
Current targeted therapies for non-small cell lung cancer (NSCLC) face significant
limitations, primarily due to the small proportion of patients who respond to existing targets …