Fragment-Based Drug Discovery — Hitting Targets Using the Right Chemistry and Expertise Alliances

Fragment-Based Drug Discovery (FBDD) has gained significant attention and importance in recent years as a method for identifying and optimizing hits for drug development. It has led to the development of approved therapeutics and numerous drug candidates, and has enabled the industry to tackle previously considered “undruggable” targets.

FBDD utilizes the benefits of biophysical, biostructural, and biochemical techniques to detect low molecular weight molecules, known as “fragments”, that bind to a target. This approach has several advantages over traditional high-throughput screening, including lower cost, greater chemical diversity, and wider sampling of potential follow-up compounds.

Experts in the field of FBDD will present case studies and the potential of various cutting-edge strategies for successful hit identification and optimization in this talk. Additionally, Dr. Nir London will present how electrophilic fragment screening can speed up the discovery of a new generation of covalent probes for challenging targets. He will also discuss the application of this method for the discovery of the first in-vivo active chemical probe for Pin1 proline isomerase and SARS-CoV-2 main protease.

Several discovery partners will provide key expertise, including 2bind, which offers a comprehensive service package for all types of projects and scientific questions, including fragment libraries, hit identification, hit validation, and biophysical assays for SAR and medicinal chemistry optimization. CrystalsFirst provides a state-of-the-art structural biology platform to unlock chemical matter for pharmaceutical and biotechnology companies in drug discovery. Its unique technology SmartSoak® stabilizes protein crystals for X-ray crystallography, providing rapid access to high-quality co-structures. Oncodesign is an expert in integrated drug discovery services, offering hit to lead optimization starting from identified fragments and full lead optimization with a dedicated multidisciplinary team.

Thu, 13 Oct 2022

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