DisPATCHes newsletter Q2 2024

By Sue Peffer

In this Q2 update, we highlight important new scientific publications and posters and describe innovative TRPML1 modulator drug discovery assays developed by the Metrion team. Don’t miss the chance to register for our upcoming webinar or watch our recent recording. We also present a customer testimonial highlighting the value of working with Metrion.

The State of the Art in Secondary Pharmacology and its Impact on the Safety of New Medicines

A team of industry experts conducted an extensive survey to highlight similarities and differences in screening strategies and target panels across the pharmaceutical industry. As a result they identified a number of opportunities for further optimisation within the secondary pharmacology assessment of novel compounds. Read more.

Front cover

Ion Channels as Targets in Drug Discovery

Eddy Stevens, Metrion’s CSO, had the pleasure of working alongside Gary Stephens, University of Reading, to edit the ‘Ion Channels as Targets in Drug Discovery’ book. The publication examines current ion channel success stories and discusses major drug discovery programs in industry. It also explores cutting-edge translational aspects of current ion channel research. Read more.

Eddy Stevens and Ion Channels as Targets in Drug Discovery

Advanced In Vitro Screening of New Drugs for Proarrhythmic Activity

10% of drugs entering Phase I receive FDA approval, with unmanageable toxicity accounting for approximately 30% of IND application clinical failure, with cardiac safety-based discontinuation also being one of the most common reasons for withdrawal of marketed drugs. Read more.

GEN article header

Last year we worked alongside authors from Amgen and published data in support of refining the hERG testing strategy for silencing RNA (siRNA). Read more.

Front page 1

18th September 2024.

Find out more and register.

Web header

In-Vitro Assessment of Cardiac  Risk in Drug Discovery

Attendees learned how an hiPSC-CM model can help provide clear decision-making data for their project team, avoiding costly issues related to QTc and QRS cardiac liabilities in the clinic. Watch webinar recording and read the Q&A.

Recording web graphic

Development and Validation of a Dual Modality TREK-1 
Screening Assay

Metrion scientists have developed a robust TREK-1 screening assay on the Qube 384 platform capable of 
identifying both activators and inhibitors of the TREK-1 channel. The optimized screening assay was employed in the successful screening of a venom library against TREK-1, detecting peptides with inhibitory and potentiating modalities. Read more and download application note.

RG lead gen 4

Assays Capable of Detecting TRPML1 Modulators for Drug Discovery

Metrion scientists have generated a stable cell line expressing the lysosomal channel TRPML1 at the cell surface. First we validated this on manual patch-clamp and went on to develop robust assays for our higher throughput screening platforms, Qube 384 and FLIPR Penta, which are capable of detecting TRPML1 modulators for drug discovery. Read more and download poster.

Molly TRPML1 4A image

An integrated calcium-imaging and patch-clamp system suitable for selecting specific subsets of neurons for electrophysiology recordings

We detail our collaboration with Scientifica on the optimisation and utilisation of the PatchScope Pro. We first targeted three different TRP channels in rat DRG. Subsequently we focused on TRPM8 which is a multimodal sensor present in 10-20% of DRGs neurons. Read more and download poster.

Federico at poster

Fluorescence-based Drug Repurposing Screen of the Potassium Channel, KV3.1 with V434L Mutation

We demonstrate how a cell line expressing the KCNC1 V434L mutation was generated and validated using biophysical and pharmacological methods, then used to screen approximately 6,800 compounds from The Broad Institute Repurposing Hub to identify inhibitors for potential use in the treatment of patients with this rare mutation. Read more and download poster.

IMG 6396 scaled

Cambridge Ion Channel Forum

Review of Cambridge Ion Channel Forum 2024

We review the Cambridge Ion Channel Forum (CICF) which took place in May. Read review.

Cambridge Ion Channel Forum 2025

Save the date: 15th May 2025

AstraZeneca DISC, UK

Why outsource to Metrion?

We don’t just deliver high quality data, our team uses their extensive experience to carefully interpret the experimental findings, communicate the results, provide recommendations, and support your decision making to best inform your screening strategy. Contact us to advance your preclinical discovery project.

Attention to detail with executing study and quality of reports