18 July 2019 - - US-based biotechnology company Gotham Therapeutics and Dutch contract research organisation Mercachem have launched a compound library tailor-made for accelerated hit generation and hit-to-lead expansion against large parts of the epitranscriptomic target space, the companies said.
Using this library will further accelerate Gotham's drug discovery efforts as the company expands its epitranscriptomics pipeline beyond the current lead program targeting the METTL3/METTL14 complex.
As a result of the collaboration, over 2,000 analogues and over 80 distinct chemotypes have been produced, which clearly comprise several privileged structures for binding to epitranscriptomic targets, demonstrating and utilizing cross-target synergies within this target space.
The consistent utilisation of structure-based drug design combined with the excellence in scaffold design and library chemistry converged to yield several molecules with up to a thousand-fold increased affinity for some of the targets.
Gotham Therapeutics has assembled an exceptional team and network to establish a novel drug class targeting RNA-modifying proteins.
By changing the activity of proteins that modify messenger RNA, the company aims to develop new treatment options for patients suffering from cancers, auto-immune and neurodegenerative diseases.
It is applying a 360-degree approach to small molecule drug design to build a pipeline based on the promise of this rapidly emerging biopharmaceutical field.
Mercachem is part of MercachemSyncom, a European contract research organisation offering innovative chemistry, medicinal chemistry and early process research services, and GMP production to accelerate the drug discovery and development process.
MercachemSyncom offers integrated drug discovery services from hit to clinic.