Knowledge Library

Discovery of Novel GST Inhibitors Identified from a DNA-Encoded Library

WuXi AppTec scientists recently contributed to a study which led to the discovery and optimization of a novel series of GST inhibitors. The authors used affinity mediated DEL selection against a privileged scaffold to identify a compound with potent inhibition against SjGST and GSTM2. SAR studies, coupled with X-ray crystallography and structural analysis, revealed that …Read More >

Resource Type: Latest Science Publication
Resource Topic: Biochemical Assays DNA-Encoded Library (DEL) Hit Finding Hit-to-Lead Lead Optimization Small Molecules Structural Biology

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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

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Translational Pharmacology of CNS and Metabolic Disorders for Testing New Modality Therapies

Animal studies may provide a close approximation to humans when addressing the key challenge of clinical translatability. In the preclinical setting, new insights into disease models and mechanisms are crucial to efficacy studies. In this webinar, Dr. Deming Xu, Chief Pharmacologist, Executive Director, and Head of In Vivo Pharmacology of WuXi AppTec Discovery Biology will …Read More >

Resource Type: Webinar
Resource Topic: Cardiovascular & Metabolic Diseases Central Nervous System & Pain in vivo Pharmacology Metabolic Diseases NASH Oligonucleotides

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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

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Oligonucleotide Therapeutics: Drug Discovery Through Tightly Coupled Chemistry and Biology

Designing effective oligonucleotide therapeutics for clinical applications involves understanding both the chemistry and biology of nucleic acids. In this white paper, learn about recent advances in chemical modifications for oligonucleotide therapeutics that improve stability and selectivity, biological screening assays to support lead optimization, and bioanalytical platforms that address the challenges of quantifying oligonucleotides. Check out …Read More >

Resource Type: Latest Science White Paper
Resource Topic: Oligonucleotides

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Oncolytic Virus Platform

Oncolytic viruses (OVs) are emerging as a promising therapeutic approach for treating cancer. OVs are capable of both tumor-specific cell lysis and immune stimulation and can be optimized for enhanced tumor selectivity.  WuXi AppTec offers a comprehensive platform of OV-related services, including virus engineering and validation, immune profiling and lysis assays, tumor cell selectivity assays, …Read More >

Resource Type: Latest Science Presentation
Resource Topic: Biochemical Assays Cell-based Assays Oncology Oncolytic Viruses Safety and Early Toxicity Tumor Models

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Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD)

WuXi AppTec scientists contributed to a study which identified a novel, indole-based, selective estrogen receptor degrader (SERD), designated LX-039. The authors show that LX-039 exhibits potent activity in ER degradation and proliferation assays. With favorable ADME/PK properties, LX-039 also exhibits higher efficacy in a tamoxifen-resistant MCF7 CDX model compared to fulvestrant, with up to 90% inhibition …Read More >

Resource Type: Latest Science Publication
Resource Topic: Biochemical Assays Cell-based Assays Discovery Chemistry Hit-to-Lead Lead Optimization Oncology Small Molecules

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Inhibition of the hERG potassium ion channel by non-nucleoside CMV polymerase antiviral inhibitors

WuXi AppTec scientists collaborated on a study to characterize a series of pyrroloquinoline derivatives that were designed and synthesized to understand the effect of various substitutions on human cytomegalovirus (HCMV) polymerase activity, antiviral activity, and hERG inhibition.  Results suggest that substitutions can be fine-tuned to reduce hERG inhibition while maintaining HCMV antiviral potency. The abstract …Read More >

Resource Type: Latest Science Publication
Resource Topic: Biochemical Assays Discovery Chemistry Hit-to-Lead Infectious Diseases Small Molecules

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Recent Advances in Library Synthesis to Accelerate Medicinal Chemistry Research

Learn how parallel medicinal chemistry (PMC) and high throughput experimentation (HTE) combined with machine learning can provide a more focused approach to target molecules, resulting in a more concentrated set of compounds to make the process of lead selection easier. Our experts show how PMC can shorten the turnaround time of the design-synthesis-test cycle, providing …Read More >

Resource Type: Webinar
Resource Topic: Discovery Chemistry Hit Finding Hit-to-Lead Small Molecules

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Resource Topics
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