Progressing epitranscriptomic drug candidates

Gotham Therapeutics establishes advanced oncology profiling cascade with ProQinase

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NEW YORK & FREIBURG, Germany—Gotham Therapeutics, a biotechnology company developing a novel drug class targeting RNA-modifying proteins, and ProQinase GmbH, an early-stage drug-discovery company, recently announced that they have established an array of advanced biochemical and cellular assays to characterize epitranscriptomic-directed compounds.
“Establishing tailored target engagement, cell biology, phenotypic and in-vivo assays to evaluate compounds originating from our three most advanced epitranscriptomic programs in parallel is a crucial next step to develop our broad pipeline towards the clinic,” said Dr. Gerhard Müller, chief scientific officer of Gotham Therapeutics. “By pursuing the full range of the reader-writer-eraser continuum, we are able to focus on targets with the most compelling links to disease and advance those programs in tandem.”
“Combining our high proficiency in providing customized solutions as early-stage drug-discovery services—including tailor-made biochemical and cell-based assays—with Gotham’s expertise in epitranscriptomics, we were able to establish in a very short time a set of customized enzymatic and cellular assays for compounds addressing three different mRNA-modifying targets,” added Dr. Sebastian Dempe, CEO of ProQinase. “We look forward to supporting Gotham as the company advances its programs into lead optimization, and to continued work with the Gotham team assisting the company to advance its broad pipeline in a time-effective manner.”
In addition to establishing a tailor-made profiling cascade for compounds from its three most advanced programs, Gotham has also made progress in strengthening its drug discovery engine and developing its candidate base. Gotham previously completed the gene-to-lead phase for its drug discovery project targeting the METTL3/METTL14 complex and established a robust discovery process as a platform for future projects. The company has also generated a library of high-quality compounds tailor-made for accelerated hit generation and hit-to-lead expansion against large parts of the epitranscriptomic target space. This library includes a collection of over 2,000 analogues covering over 80 distinct chemotypes that will be used to further accelerate Gotham’s drug discovery efforts as it expands its pipeline.
Gotham notes that by changing the activity of proteins that modify messenger RNA, “we aim to develop new treatment options for patients suffering from cancers, autoimmune and neurodegenerative diseases. We are applying a 360-degree approach to small-molecule drug design to build a pipeline based on the promise of this rapidly emerging biopharmaceutical field.”
Germany-based ProQinase GmbH, which was recently acquired by Malvern, Pa.-based Reaction Biology Corp, considers itself an industry leader and innovator for early-stage drug discovery. The combined company specializes in biochemical and cell-based assay services, protein production, and immune-oncology in-vivo animal models, with more than 1,500 clients worldwide. As a major provider of kinase-based discovery services, with 660 kinases covered in what the company says is the industry's largest global offering of its kind, the global service portfolio reportedly offers an end-to-end solution, including partnering for integrated drug discovery projects

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