Knowledge Library

Discovery of GuaB Inhibitors for the Treatment of Tuberculosis

Tuberculosis is the leading cause of death from an infectious disease and is caused by Mycobacterium tuberculosis (MTB). Inosine-5′-monophosphate dehydrogenase (GuaB) is an enzyme that performs the rate-limiting step in the de novo biosynthesis of guanine, which is critical for growth of bacteria, including MTB. The development of a novel antibiotic that inhibits GuaB could …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Discovery Chemistry, Hit Finding, Hit-to-Lead, Infectious Diseases

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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, several new strategies have recently become available for targeting the mutant protein. One of the most promising of these involves the use of low molecular weight compounds that promote refolding and reactivation of mutant p53 …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Discovery Chemistry, Hit-to-Lead, Lead Optimization, Oncology, Small Molecules

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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 to as targeted covalent inhibitors (TCIs).  In this webinar, experts discuss innovative approaches to screen for covalent binders, strategies for the synthesis of covalent warheads, and assays to optimize the ADME/DMPK properties of these molecules. …Read More >

Resource Type: Webinar
Resource Topic: Discovery Chemistry, DNA-Encoded Library (DEL), Lead Optimization, Small Molecules

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Recent Advances in HTE and Flow Chemistry

High throughput experimentation (HTE) is frequently employed to identify reaction conditions for challenging transformations, giving access to a diverse array of medicinal chemistry targets. In parallel to using conventional batch reactions, we also incorporate flow chemistry into early phase synthesis to help with reaction selectivity and optimization, up-scaling, and solving specific chemical problems. In this …Read More >

Resource Type: Webinar
Resource Topic: Discovery Chemistry, Small Molecules

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DNA-Compatible Cyclizations

The recent publication in the journal Organic Letters, ‘DNA-Compatible Cyclization Reaction to Access 1,3,4-Oxadiazoles & 1,2,4-Triazoles‘ by our WuXi Biology DEL team, introduces two novel DNA-compatible reactions, successfully incorporating bioactive cores 1,3,4-oxadiazoles and 1,2,4-triazoles into the DEL library. These cores are reported to show broad ranges of biological activities, such as antiviral, anti-inflammatory, anticancer, antifungal, …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Discovery Chemistry, DNA-Encoded Library (DEL), Small Molecules

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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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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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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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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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Resource Topics
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