Knowledge Library

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 to evade the immune system. IDO1 can also suppress the immune response through mechanisms independent of its enzyme activity, and this may be difficult to target with current inhibitors.  Drugs targeting only IDO1 enzyme activity …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Discovery Chemistry, Lead Optimization, Oncology, Targeted Protein Degradation

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On-bead DEL Application and Case Study for Drug Discovery

DNA-encoded library (DEL) technology has been recognized as a major screening method with unique advantages for offering vast chemical diversity and multiplexed affinity-based screening. Recently, solid-phase On-bead DEL, also known as one bead one compound (OBOC), has been developed to further expand DEL screening from affinity-based screening into biochemical activity screening. At the 2025 SLAS …Read More >

Resource Type: Latest Science, Poster
Resource Topic: DNA-Encoded Library (DEL), Hit Finding, Hit-to-Lead, Targeted Protein Degradation

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Accelerating CIP Discovery with ASMS and DEL

Chemical inducers of proximity (CIPs) are small molecules that induce the proximity of two biological targets, usually proteins. Molecular glues and PROteolysis TArgeting Chimeras (PROTACs®) are among the best-known CIPs. These molecules utilize the endogenous E3-based proteolysis pathway to induce proximity between the target protein and E3 ligase, thereby triggering targeted protein degradation. At the …Read More >

Resource Type: Latest Science, Poster
Resource Topic: DNA-Encoded Library (DEL), Mass Spectrometry-based Assays, Targeted Protein Degradation

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Discovery of Molecular Glues: Challenges and Opportunities

Introduction: Molecular glues (MGs) are a class of small molecules that alter the surface properties of proteins to strengthen or induce protein-protein interactions (PPI), leading to specific biological effects like protein degradation, pathway inhibition, or activation. Their unique properties endow them with high selectivity and bioavailability, allowing for controlled drug release. Molecular glues show great …Read More >

Resource Type: Article, Blog
Resource Topic: Small Molecules, Targeted Protein Degradation

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Targeted Protein Degradation Platform

Targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. This technology is enabling researchers to pursue targets that were previously considered undruggable and to address the resistance issue of small molecule inhibitors. Since 2016, WuXi AppTec has built a comprehensive TPD discovery …Read More >

Resource Type: Latest Science, Poster
Resource Topic: Biochemical Assays, DNA-Encoded Library (DEL), Targeted Protein Degradation

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Discovery of a Specific CKIP-1 Ligand using DEL

Casein kinase 2-interacting protein-1 (CKIP-1) performs a critical negative role in the regulation of bone formation. Accumulated evidence strongly supports CKIP-1 as an attractive therapeutic target in osteoporosis.  As a scaffold protein lacking enzymatic activity, CKIP-1 seems to be an undruggable target, and the development of selective small molecule inhibitors targeting CKIP-1 has proven to …Read More >

Resource Type: Latest Science, Publication
Resource Topic: DNA-Encoded Library (DEL), Metabolic Diseases, Small Molecules, Targeted Protein Degradation

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Research Strategies for the Discovery of Targeted Protein Degraders

In this webinar, experts present research strategies for the discovery of targeted protein degraders. Over the past decade, targeted protein degradation (TPD) technology has become one of the most promising methods to remove specific disease-related proteins using cellular self-destruction mechanisms. Since 2016, WuXi AppTec has built a comprehensive TPD discovery service platform, adept in over 20 …Read More >

Resource Type: Webinar
Resource Topic: Targeted Protein Degradation

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USP7 Inhibitors Reveal a Differentiated Mechanism of p53-Driven Anti-Cancer Activity

Ubiquitin-specific protease 7 (USP7) is a deubiquitinating enzyme that cleaves ubiquitin from a range of substrates, shielding them from degradation by the proteasome. USP7 activity has been implicated in cancer progression and its overexpression is associated with tumor aggressiveness and poor prognosis in a variety of cancer types, making USP7 inhibition an attractive strategy for …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Cell-based Assays, Oncology, Structural Biology, Targeted Protein Degradation, Tumor Models

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CRBN Structural Biology Services

Targeted protein degradation of disease-causing proteins by the E3 ligase cereblon (CRBN) represents a new therapeutic strategy for addressing challenging-to-treat diseases. To support drug discovery programs, we have established off-the-shelf crystallization and cryo-EM systems to enable the determination of high-resolution X-ray crystal structures with a short turnaround time. Together with our protein production service and …Read More >

Resource Type: Presentation
Resource Topic: Biophysical Assays, Cryo-EM, Structural Biology, Targeted Protein Degradation, X-ray Crystallography

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Resource Topics
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