Knowledge Library

STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts

The contribution of the X-ray crystallography team from our WuXi AppTec site in Germany was acknowledged in a recent study published in the journal Cancer Discovery. In this study, the authors show that compound STX-478, an allosteric PI3Kα inhibitor, selectively targets prevalent PI3Kα helical- and kinase-domain mutant tumors. STX-478 demonstrated robust efficacy in human tumor …Read More >

Resource Type: Latest Science Publication
Resource Topic: Oncology Small Molecules Structural Biology Structural Biology X-ray Crystallography

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How to Accelerate the Synthesis of PROTACs: Strategies and Case Studies

Introduction: Targeted Protein Degradation (TPD) has emerged as a promising therapeutic modality due to its potential to develop therapeutics for previously undruggable targets and address the resistance issues of small molecule inhibitors. Central to this strategy is the novel protein-degradation approach represented by proteolysis-targeting-chimeras (PROTACs), which induce targeted protein degradation through the ubiquitin-proteasome system (UPS). …Read More >

Resource Type: Article Blog Case Study
Resource Topic: Discovery Chemistry Small Molecules Targeted Protein Degradation

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DEL Insight: Novel Applications with the Bifunctional Linker of DNA-encoded Molecules

Due to the special configuration of the DNA encoded library (DEL), each DEL molecule carries a DNA sequence encoding its identity through a bifunctional linker. The linkers that are considered “redundant” and “troublesome” in traditional drug discovery actually offer innate advantages in many application scenarios. In this article, we review how to utilize DNA-encoded libraries …Read More >

Resource Type: Article Blog
Resource Topic: DNA-Encoded Library (DEL) Hit Finding Small Molecules

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Emerging Drug Discovery Strategies for Targeted Protein Degradation

In the last 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.  In our latest White Paper, “Emerging Drug Discovery Strategies for Targeted Protein Degradation” we explore how DNA-encoded library (DEL) technology can be used for direct discovery of proteolysis-targeting chimeras …Read More >

Resource Type: Latest Science White Paper
Resource Topic: Discovery Chemistry DNA-Encoded Library (DEL) Targeted Protein Degradation

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OncoWuXi Express: Review of SITC 2023 Annual Meeting

Review of SITC 2023 Annual Meeting The 38th Annual Meeting of the Society for Immunotherapy of Cancer (SITC) was held this year in San Diego, CA, USA. As one of the most influential international conferences dedicated to cancer immunotherapy, SITC provides attendees with a cross-disciplinary educational and interactive platform. This meeting focuses on discussing and …Read More >

Resource Type: Article Blog
Resource Topic: Antibodies Autoimmune and Inflammatory Diseases Cell-based Assays in vivo Pharmacology Oligonucleotides Oncology

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Preclinical platform for nucleic acid drug evaluation: siRNA and mRNA therapeutics

SITC Poster #59: Since the emergence of the COVID-19 pandemic, numerous nucleic-acid therapeutics have been approved for clinical use. Distinguished from conventional protein-targeted therapy, nucleic acid therapeutics offer the potential for sustained effects via gene modification or inhibition. In this study, we conducted a comprehensive evaluation of the activity and anti-tumor effects of PKN3-targeted siRNA …Read More >

Resource Type: Latest Science Poster
Resource Topic: Antibodies Cell-based Assays Oligonucleotides Oncology Tumor Models

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Novel Approaches to Targeted Protein Degradation

In the last 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. As of now, over 20 targeted protein degraders have advanced into clinical development. WuXi AppTec has built a robust TPD discovery chemistry platform. We deliver synthetic and medicinal chemistry …Read More >

Resource Type: Video
Resource Topic: Discovery Chemistry Targeted Protein Degradation

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Pioneering Advanced Modalities in Early Drug Discovery

New modalities such as peptides, oligonucleotides, and cell and gene therapies have revolutionized healthcare industry innovation. To meet these evolving needs, WuXi Biology has proactively developed a broad range of capabilities, offering integrated solutions to global pharmaceutical and biotech companies for challenging targets. We have established major capabilities for new modalities in the early discovery …Read More >

Resource Type: Article
Resource Topic: Antibody Drug Conjugate CAR-T Cell Cell Therapies DNA-Encoded Library (DEL) Fragment-Based Drug Discovery Gene Therapies Oligonucleotides Oncolytic Viruses Targeted Protein Degradation

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Advances and Biological Evaluation of Oligonucleotide Drugs

Introduction: As a therapeutic modality, oligonucleotides have a target abundance, persistent efficacy, high specificity, greater success rate and shorter R/D development period compared to other therapeutic approaches. Recently, significant achievements have been made in the discovery of oligonucleotide drugs. Numerous oligonucleotide drugs have been marketed. However, there are still many challenges, including limited delivery efficiency …Read More >

Resource Type: Article Blog
Resource Topic: Oligonucleotides

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Resource Topics
× peptide, amino acid

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