Knowledge Library

Discovery and Characterization of Proteolysis Targeting Chimeras: Tissue Transglutaminase

Tissue transglutaminase (TG2) is a multifunctional enzyme activated in several pathological conditions, including cancer. WuXi AppTec recently contributed to a study which used a targeted protein degradation strategy to abolish TG2’s myriad of functions. The authors synthesized and characterized a series of VHL-based degraders that reduce TG2 in ovarian cancer cells in a proteasome-dependent manner.

Resource Type: Latest Science Publication
Resource Topic: Oncology Targeted Protein Degradation

VIEW

Emerging Modalities in Drug Discovery

In this webinar, we present the latest advances and challenges facing researchers focused on new and emerging modalities in drug discovery. Topics include targeted protein degradation, targeted covalent inhibitors, and nucleic acid therapeutics. Our expert speaker, Dr. Tao Guo, discusses solutions for addressing the complexities in designing, synthesizing, and optimizing these molecules, with an added …Read More >

Resource Type: Latest Science Webinar
Resource Topic: Discovery Chemistry Oligonucleotides Small Molecules Targeted Protein Degradation

VIEW

DDC 2023: Biophysical & Functional Characterization of Bifunctional Small Molecules Enables TPD Drug Discovery

Leverage our platform of biophysical methods to accelerate your research on targeted protein degradation. At DDC 2023, WuXi AppTec scientists presented an in-depth panel of assays to support the characterization of bifunctional small molecules. Our cutting-edge services include target protein ubiquitination and degradation assays, techniques to evaluate binary binding, and proximity assays to measure ternary …Read More >

Resource Type: Latest Science Poster
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Hit-to-Lead Lead Optimization Small Molecules Structural Biology Targeted Protein Degradation

VIEW

Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4

Expansion of the E3 ligase toolbox has the potential to dramatically advance the field of targeted protein degradation.  WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the discovery of novel small molecule binders of GID4, a substrate receptor in the human CTLH E3 ligase complex.  Researchers used …Read More >

Resource Type: Latest Science Publication
Resource Topic: DNA-Encoded Library (DEL) Fragment-Based Drug Discovery Targeted Protein Degradation

VIEW

Targeted Protein Degradation

WuXi AppTec utilizes state-of-the-art techniques to support drug discovery teams focused on targeted protein degradation. Our services include a broad range of ligand-finding methods, such as DEL, fragment screening, ASMS, and virtual screening. We provide custom linker design and complex synthesis for new linkers and E3 ligase ligands. To support lead optimization efforts, our platform …Read More >

Resource Type: Brochure Latest Science
Resource Topic: Biochemical Assays Biophysical Assays Cell-based Assays Mass Spectrometry-based Assays Oncology Small Molecules Structural Biology Targeted Protein Degradation

VIEW

Ligand Finding and Chemistry Workflows for Targeted Protein Degradation

This webinar will focus on aspects related to PROTAC discovery and chemistry workflows, such as ligand finding strategies, synthesis optimization, and linker design. Successful development of bifunctional molecules requires a deep understanding of multiple processes, including biophysical events which dictate induced proximity and how technologies such as DNA-encoded libraries (DEL) can be leveraged to identify …Read More >

Resource Type: Webinar
Resource Topic: Autoimmune and Inflammatory Diseases Biophysical Assays Cardiovascular & Metabolic Diseases Central Nervous System & Pain Discovery Chemistry DNA-Encoded Library (DEL) Hit Finding Hit-to-Lead Lead Optimization Oncology Small Molecules Structural Biology Target-Specific Assays Targeted Protein Degradation

VIEW

Biological Characterization and Development Workflows for Targeted Protein Degradation

This webinar will focus on PROTAC biology workflows, such as in vitro screening assays, in vivo testing, and optimization of DMPK properties. Topics will include the best use of biochemical assays to measure binary/ternary complex formation, cell-based assays to assess target engagement and degradation, strategies for enhancing drug delivery and formulation, and PK/PD evaluation of …Read More >

Resource Type: Webinar
Resource Topic: Autoimmune and Inflammatory Diseases Biochemical Assays Cardiovascular & Metabolic Diseases Cell-based Assays Central Nervous System & Pain Hit-to-Lead in vitro biology in vivo Pharmacology Lead Optimization Oncology Small Molecules Target Identification and Validation Target-Specific Assays Targeted Protein Degradation

VIEW

Discovery Newsletter Special New Year Edition 2023

Resource Type: Latest Science Newsletter
Resource Topic: Biophysical Assays Central Nervous System & Pain Discovery Chemistry DNA-Encoded Library (DEL) Hit-to-Lead in silico services Lead Optimization Quantum Mechanics Small Molecules Target Identification and Validation Targeted Protein Degradation

VIEW

Drugging the Undruggable: Leveraging the Right Screening Methods for Challenging Targets

Challenging targets, such as membrane proteins or protein-protein interactions were considered undruggable in the past. However, today a variety of screening methods can be used to help develop drugs against these formerly undruggable targets.

Resource Type: Infographic
Resource Topic: DNA-Encoded Library (DEL) Hit Finding in silico services Mass Spectrometry-based Assays Screening Services Small Molecules Structural Biology Target Identification and Validation Targeted Protein Degradation

VIEW


Resource Topics
× peptide, amino acid

Contact An Expert Today!