sirolimus and desmethylclomipramine

sirolimus has been researched along with desmethylclomipramine* in 2 studies

Other Studies

2 other study(ies) available for sirolimus and desmethylclomipramine

Article	Year
In Vitro and In Vivo Pipeline for Validation of Disease-Modifying Effects of Systems Biology-Derived Network Treatments for Traumatic Brain Injury-Lessons Learned. International journal of molecular sciences, 2019, Oct-29, Volume: 20, Issue:21 We developed a pipeline for the discovery of transcriptomics-derived disease-modifying therapies and used it to validate treatments in vitro and in vivo that could be repurposed for TBI treatment. Desmethylclomipramine, ionomycin, sirolimus and trimipramine, identified by in silico LINCS analysis as candidate treatments modulating the TBI-induced transcriptomics networks, were tested in neuron-BV2 microglial co-cultures, using tumour necrosis factor α as a monitoring biomarker for neuroinflammation, nitrite for nitric oxide-mediated neurotoxicity and microtubule associated protein 2-based immunostaining for neuronal survival. Based on (a) therapeutic time window in silico, (b) blood-brain barrier penetration and water solubility, (c) anti-inflammatory and neuroprotective effects in vitro ( Topics: Animals; Anti-Inflammatory Agents; Biomarkers; Brain Injuries, Traumatic; Cell Line; Clomipramine; Coculture Techniques; Cytokines; Disease; Gene Expression; In Vitro Techniques; Ionomycin; Machine Learning; Male; Microglia; Neurons; Neuroprotection; Neuroprotective Agents; NF-E2-Related Factor 2; Nitrites; Rats; Sirolimus; Systems Biology; Transcriptome; Trimipramine; Tumor Necrosis Factor-alpha; Up-Regulation	2019
Modulating cellular autophagy for controlled antiretroviral drug release. Nanomedicine (London, England), 2018, Volume: 13, Issue:17 Pharmacologic agents that affect autophagy were tested for their abilities to enhance macrophage nanoformulated antiretroviral drug (ARV) depots and its slow release.. These agents included URMC-099, rapamycin, metformin, desmethylclomipramine, 2-hydroxy-β-cyclodextrin (HBC) and clonidine. Each was administered with nanoformulated atazanavir (ATV) nanoparticles to human monocyte-derived macrophages. ARV retention, antiretroviral activity and nanocrystal autophagosomal formation were evaluated.. URMC-099, HBC and clonidine retained ATV. HBC, URMC-099 and rapamycin improved intracellular ATV retention. URMC-099 proved superior among the group in affecting antiretroviral activities.. Autophagy inducing agents, notably URMC-099, facilitate nanoformulated ARV depots and lead to sustained release and improved antiretroviral responses. As such, they may be considered for development as part of long acting antiretroviral treatment regimens. Topics: Anti-HIV Agents; Atazanavir Sulfate; Autophagy; beta-Cyclodextrins; Cell Survival; Clomipramine; Clonidine; Drug Carriers; Drug Interactions; Drug Liberation; HIV-1; Humans; Macrophages; Metformin; Nanoparticles; Particle Size; Pyridines; Pyrroles; Sirolimus; Tissue Distribution	2018

Article

Year

In Vitro and In Vivo Pipeline for Validation of Disease-Modifying Effects of Systems Biology-Derived Network Treatments for Traumatic Brain Injury-Lessons Learned.

International journal of molecular sciences, 2019, Oct-29, Volume: 20, Issue:21

We developed a pipeline for the discovery of transcriptomics-derived disease-modifying therapies and used it to validate treatments in vitro and in vivo that could be repurposed for TBI treatment. Desmethylclomipramine, ionomycin, sirolimus and trimipramine, identified by in silico LINCS analysis as candidate treatments modulating the TBI-induced transcriptomics networks, were tested in neuron-BV2 microglial co-cultures, using tumour necrosis factor α as a monitoring biomarker for neuroinflammation, nitrite for nitric oxide-mediated neurotoxicity and microtubule associated protein 2-based immunostaining for neuronal survival. Based on (a) therapeutic time window in silico, (b) blood-brain barrier penetration and water solubility, (c) anti-inflammatory and neuroprotective effects in vitro (

Topics: Animals; Anti-Inflammatory Agents; Biomarkers; Brain Injuries, Traumatic; Cell Line; Clomipramine; Coculture Techniques; Cytokines; Disease; Gene Expression; In Vitro Techniques; Ionomycin; Machine Learning; Male; Microglia; Neurons; Neuroprotection; Neuroprotective Agents; NF-E2-Related Factor 2; Nitrites; Rats; Sirolimus; Systems Biology; Transcriptome; Trimipramine; Tumor Necrosis Factor-alpha; Up-Regulation

2019

Modulating cellular autophagy for controlled antiretroviral drug release.

Nanomedicine (London, England), 2018, Volume: 13, Issue:17

Pharmacologic agents that affect autophagy were tested for their abilities to enhance macrophage nanoformulated antiretroviral drug (ARV) depots and its slow release.. These agents included URMC-099, rapamycin, metformin, desmethylclomipramine, 2-hydroxy-β-cyclodextrin (HBC) and clonidine. Each was administered with nanoformulated atazanavir (ATV) nanoparticles to human monocyte-derived macrophages. ARV retention, antiretroviral activity and nanocrystal autophagosomal formation were evaluated.. URMC-099, HBC and clonidine retained ATV. HBC, URMC-099 and rapamycin improved intracellular ATV retention. URMC-099 proved superior among the group in affecting antiretroviral activities.. Autophagy inducing agents, notably URMC-099, facilitate nanoformulated ARV depots and lead to sustained release and improved antiretroviral responses. As such, they may be considered for development as part of long acting antiretroviral treatment regimens.

Topics: Anti-HIV Agents; Atazanavir Sulfate; Autophagy; beta-Cyclodextrins; Cell Survival; Clomipramine; Clonidine; Drug Carriers; Drug Interactions; Drug Liberation; HIV-1; Humans; Macrophages; Metformin; Nanoparticles; Particle Size; Pyridines; Pyrroles; Sirolimus; Tissue Distribution

2018