Lead Optimization Archives

Navigating the ADC Development Pathway

Antibody-drug conjugates (ADCs) hold great promise as targeted cancer therapeutics, but their complex structure poses significant development and safety challenges....

Rational Design and Optimization of a Potent IDO1 PROTAC

Indoleamine 2,3-dioxygenase 1 (IDO1) is an enzyme that metabolizes tryptophan, and its activity can lead to immunosuppression, thereby allowing tumors...

Small Molecule Reactivator of p53 Y220C Mutant

Mutant p53 is one of the most attractive targets for new anti-cancer drugs. Although traditionally regarded as difficult to drug,...

Strategies for Screening and Characterizing Targeted Covalent Inhibitors

With advancements in drug design, there is resurging interest in drugs that form covalent bonds with their targets, often referred...

Preclinical Evaluation of the SARS-CoV-2 Mpro Inhibitor RAY1216

WuXi AppTec scientists contributed to a research article in the journal Nature Microbiology, which characterized a peptidomimetic inhibitor of the...

PROTAC Optimization Strategies

What if a constructed PROTAC with a confirmed high-affinity warhead doesn’t work as expected? That means we need to take...

Addition of Covalent Warhead and DEL-Generated Hit Fragmentation Empower FBDD

Fragment-based drug discovery (FBDD) is one of the most well-developed approaches for projects starting from small, low-affinity compounds. At the...

One Stop Target-to-Hit Platform: CDKs and CDK-Cyclin Complexes

Cyclin-dependent kinases (CDKs) and their cyclin regulatory subunits form complexes that are essential for driving abnormal growth processes in cancer...

Biophysical and Structural Biology Methods Enable Fragment-Based Ligand Discovery

Powerful biophysical and structural biology tools enable the study of large numbers of fragments and are opening new possibilities in...

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