Knowledge Library
Discovery Newsletter November 2022
WuXi AppTec Discovery Services
Delivering comprehensive end-to-end solutions for creating, identifying, and supporting preclinical candidates, from discovery to development, with our integrated chemistry and biology research platforms.
Quality Control for DNA-Encoded One-Bead-One-Compound (OBOC) Libraries
Integrating Practical Machine Learning and Quantum Mechanics Tools to Synthesis in Medicinal Chemistry
Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase
Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the replacement of a phenyl with a pyridyl moiety in the chemical structure revealed a new binding mode for the inhibitors with subtle conformational change of the …Read More >
Meeting Neurodegenerative Disease Head-On with Emerging Drug Discovery Strategies
Chronic neurodegenerative diseases encompass a variety of progressive conditions that affect neurons, including Huntington’s disease, Parkinson’s disease, Alzheimer’s disease, and other forms of dementia. They are among the most common and challenging central nervous system (CNS) diseases. “Many companies had stopped their research program into neurodegenerative diseases, but now sophisticated technology advances have became more broadly …Read More >
One-Stop Target-to-Hit Solutions
WuXi AppTec | Target-to-Hit Solutions Protein Production | All Target Classes and Challenging Proteins Biophysical & Biochemical Platforms | Ready-To-Go Assay for Broad Range of Drug Targets Structural Biology Platforms Covalent and non-covalent fragment libraries & Screening
DELpro: A New Method of Hit Discovery
DNA-Encoded Library (DEL) technology involves a novel affinity selection process that integrates chemistry, biology, bioinformatics and computational chemistry to facilitate a rapid drug discovery process, allowing access to more chemical space with lower cost. In contrast to high throughput screening, DEL requires a very small amount of target protein and minimum assay development. More importantly, …Read More >