ApconiX Publications archives 

Toxicogenomics: A 2020 Vision

Toxicogenomics: A 2020 Vision Together with the promotion of non-animal testing, in vitro toxicogenomics (TGx) may play a vital role in the next generation risk assessment paradigm. A strategic shift in risk assessment provides an unprecedented opportunity for repositioning TGx in the regulatory setting. As the emerging technique continues [...]

By |2022-02-22T13:19:17+00:00April 17th, 2019|Publications, Toxicology|Comments Off on Toxicogenomics: A 2020 Vision

Differential expression of cyclin-dependent kinases in the adult human retina in relation to CDK inhibitor retinotoxicity

Differential expression of cyclin-dependent kinases in the adult human retina in relation to CDK inhibitor retinotoxicity Abstract Cyclin-dependent kinases (CDKs) are a family of kinases associated predominantly with cell cycle control, making CDK inhibitors interesting candidates for anti-cancer therapeutics. However, retinal toxicity (loss of photoreceptors) has been associated with [...]

By |2021-09-15T16:08:37+01:00January 24th, 2019|Publications, Toxicology|Comments Off on Differential expression of cyclin-dependent kinases in the adult human retina in relation to CDK inhibitor retinotoxicity

Highlight Article for Experimental Biology and Medicine

Highlight Article for Experimental Biology and Medicine “Drug discovery and development: Biomarkers of neurotoxicity and neurodegeneration”, co-authored by Abigail L Walker, Syed Z Imam and  Ruth A Roberts, has been selected as a highlight article for Experimental Biology and Medicine’s 243:13 issue. As a result of this designation it [...]

By |2022-12-13T18:16:22+00:00December 7th, 2018|Publications|Comments Off on Highlight Article for Experimental Biology and Medicine

Mother and Daughter on Front cover

Ruth Roberts and Emma Walker were featured on the front cover of Toxicology Research this month.  The mother and daughter’s review article, Collaboration and competition: ethics in toxicology hit the headlines in Volume 7. The front cover was painted by Emma, an accomplished artist as well as scientist.  Emma is currently studying for her Master’s [...]

By |2021-11-30T13:10:56+00:00July 22nd, 2018|Toxicology, Publications|Comments Off on Mother and Daughter on Front cover

Understanding drug targets: no such thing as bad news

Abstract: How can small-to-medium pharma and biotech companies enhance the chances of running a successful drug project and maximise the return on a limited number of assets? Having a full appreciation of the safety risks associated with proposed drug targets is a crucial element in understanding the unwanted side-effects that might stop a project in [...]

By |2018-10-01T17:36:10+01:00June 6th, 2018|Publications, Target Safety Assessments|Comments Off on Understanding drug targets: no such thing as bad news

Changes in the metabolome and microRNA levels in biological fluids might represent biomarkers of neurotoxicity: A trimethyltin study.

Changes in the metabolome and microRNA levels in biological fluids might represent biomarkers of neurotoxicity: A trimethyltin study. Abstract: Neurotoxicity has been linked with exposure to a number of common drugs and chemicals, yet efficient, accurate, and minimally invasive methods to detect it are lacking. Fluid-based biomarkers such as [...]

By |2023-05-30T15:41:18+01:00February 28th, 2018|Publications, Toxicology|Comments Off on Changes in the metabolome and microRNA levels in biological fluids might represent biomarkers of neurotoxicity: A trimethyltin study.

Collaboration and Competition: Ethics in Toxicology

Two of the biggest ethical challenges in pharmaceutical toxicology are the use of animals in testing and the high safety-related attrition rates in new drug development.  Yet very little is invested in these two fields compared with investment in new efficacy models, new disease targets and new technologies.  How can this be addressed?  In this [...]

By |2021-09-15T15:29:06+01:00February 9th, 2018|Publications, Toxicology|Comments Off on Collaboration and Competition: Ethics in Toxicology

N-Ethylmaleimide increases KCC2 cotransporter activity by modulating transporter phosphorylation.

Abstract K+/Cl- cotransporter 2 (KCC2) is selectively expressed in the adult nervous system and allows neurons to maintain low intracellular Cl- levels. Thus, KCC2 activity is an essential prerequisite for fast hyperpolarizing synaptic inhibition mediated by type A γ-aminobutyric acid (GABAA) receptors, which are Cl--permeable, ligand-gated ion channels. Consistent with this, deficits in the activity of [...]

By |2022-05-12T14:18:12+01:00December 1st, 2017|Publications, Ion Channels|Comments Off on N-Ethylmaleimide increases KCC2 cotransporter activity by modulating transporter phosphorylation.

The small molecule CLP257 does not modify activity of the K+/Cl- co-transporter KCC2 but does potentiate GABA A receptor activity.

Read more here: RA Cardarelli, K Jones, LI Pisella, HJ Wobst, LJ McWilliams, PM Sharpe, MP Burnham, DJ Baker, I Chudotvorova, J Guyot, L Silayeva, DH Morrow, N Dekker, S Zicha, PA Davies, J Holenz, ME Duggan, J Dunlop, RJ Mather, Q Wang, I Medina, NJ Brandon, TZ Deeb and SJ Moss. The small molecule CLP257 [...]

By |2018-07-11T14:46:53+01:00December 1st, 2017|Publications, Ion Channels|Comments Off on The small molecule CLP257 does not modify activity of the K+/Cl- co-transporter KCC2 but does potentiate GABA A receptor activity.

Target safety assessments and their role in de-risking drug discovery – Nav1.7 as an example

This poster, presented at the Gordon Research Conference in August 2017, concluded that: Target safety assessments: Provide expert assessment and interpretation of literature and available databases and are invaluable in identifying and avoiding target-related risks Inform target selection and/or prioritisation early in discovery Should contain the level of detail appropriate to the project stage Should [...]

By |2022-11-22T16:22:21+00:00August 20th, 2017|Target Safety Assessments, TSA Page, Publications|Comments Off on Target safety assessments and their role in de-risking drug discovery – Nav1.7 as an example
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