Knowledge Library
Optimizing Drug Discovery Pipelines with Biophysical Methods
Discovery of RNA binding molecule using DNA-encoded library technology
Empowering Organic Syntheses with Quantum Mechanics Analyses
Syntheses of specifically functionalized molecules continue to be rate limiting steps (RLS) in drug discovery. Improvement in this RLS means investing only in reactions/synthetic sequences that are more likely to succeed. Structural diversifications, different substitution patterns or unique heterocyclic systems can often adversely impact the crucial step(s) of established synthetic sequences or development of feasible …Read More >
The Synthesis of an Entrepreneur: Merging a Passion for Biochemistry, Synthetic Chemistry, and Bioactive Molecules in Academia
INNOVATION THAT MATTERS By Rich Soll, Senior Advisor, Strategic Initiatives at WuXi AppTec (@richsollwx) Synthetic chemist Joseph Ready believes a huge amount of innovation in the drug industry comes from academia. Academic science is arguably the greatest source of innovation in our ecosystem, yet faces challenges when considering the transition from the lab to early stage …Read More >
Drug Hunter: Discovering New Frontiers in Cancer Treatments & Beyond
INNOVATION THAT MATTERS By Rich Soll, Senior Advisor, Strategic Initiatives at WuXi AppTec (@richsollwx) As a self-proclaimed drug hunter, Phil Jones is on a mission to identify the next generation of cancer medicines that improve the lives of patients with cancer. He leads a multi-disciplinary team of scientists at The University of Texas MD Anderson Cancer Center’s Institute …Read More >
Faster with high-speed fragment screening — Accelerate your drug discovery campaign
In the past, thousands of proteins were considered undruggable. The restricted number of chemical entities available and classical methods limited the exploration of this undevelopable area. Today, the combination of novel chemical modalities and advanced technical approaches has resulted in new clinical candidates from previously undruggable targets. To accelerate your drug discovery campaign, WuXi AppTec´s …Read More >
Unlocking the potential of DEL | Inspire Hit Discovery
March 4, 2020 – By going commercial, DNA Encoded Library (DEL) technology facilitates rapid discovery and provides access to more chemical entities at lower cost. Over the years, DEL has become a disruptive drug discovery technology in comparison to traditional high-throughput screening (HTS) where it allows expedition of early stage drug discovery. However, DEL platforms don’t succeed …Read More >
Enabling Technology for Targeted Protein Degradation
Summary Traditional small molecule therapeutic mechanisms have recently been augmented by a new strategy to specifically manipulate the levels of disease-related proteins. By employing bifunctional molecules, we can hijack endogenous cellular degradation mechanism for targeted degradation of a disease-related protein. Bifunctional molecules consisting of a ligand that binds to an E3 ligase, connected by a …Read More >
Establishment of KRAS-G12C inhibitor induced resistant tumor models enable the development of new generation KRAS-G12C inhibitors and combinatorial strategies
Activating KRAS mutations, including G12C and G12D, are detected in approximately 25% of human cancers. The most common KRAS mutation is G12C, which comprises nearly 15% of lung adenocarcinomas, 8% of colorectal carcinomas and 4% of pancreatic adenocarcinomas. AMG-510 from Amgen and MRTX849 from Mirati Therapeutics, both targeting the KRASG12C mutant, have shown encouraging results …Read More >