Knowledge Library

Heme Oxygenase-1-Targeting Molecules

WuXi AppTec scientists published a study in the open access archive ChemRxiv describing the discovery of highly selective, novel, heme oxygenase-1 (HO-1) targeting molecules. HO-1, primarily a heme-degrading enzyme, has been identified as a potential therapeutic target in diseases such as cancer and neurodegenerative disorders. Here, we report the discovery of five series of novel …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Central Nervous System & Pain, DNA-Encoded Library (DEL), Hit Finding, in silico services, Oncology

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iMN041: Prodrug with a Unique Antitumor Immune Response

WuXi AppTec scientists contributed to a research article in the journal Translational Medicine Communications which characterized the antitumor immune responses generated by iMN041, a prodrug of a DNA methyl transferase/ribonucleotide reductase inhibitor.  This study also assessed the efficacy of iMN041 in mouse xenografts of human clear cell renal cell cancer, pancreatic cancer, and triple negative …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Cell-based Assays, Immunology, Oncology, Tumor Models

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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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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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TAAR1 as an Emerging Target for the Treatment of Psychiatric Disorders

A growing body of in vitro and in vivo evidence has demonstrated that trace amine-associated receptor 1 (TAAR1) could negatively modulate monoamine transmission and play a crucial role in many psychiatric disorders, including schizophrenia, depression, and anxiety. WuXi AppTec contributed to a review article in the journal Pharmacology & Therapeutics, discussing the current understanding of …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Central Nervous System & Pain

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Negative Allosteric Modulation of the µ-Opioid Receptor

DNA-encoded libraries from WuXi AppTec were used in a “steered” screening against either inactive or active μ-opioid receptors in parallel, to find novel negative allosteric modulators of this receptor. The molecule discovered via DEL screening not only shows direct and effective in vitro and in vivo potency, but also helps elucidate the mechanism of negative allosteric modulation of GPCRs. This discovery …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Central Nervous System & Pain, DNA-Encoded Library (DEL), Hit Finding, Small Molecules

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Discovery and Characterization of ZL-2201, a Potent, Highly Selective, and Orally Bioavailable Small-molecule DNA-PK Inhibitor

DNA-dependent protein kinase (DNA-PK) plays an important role in the overall survival and proliferation of cells, making this enzyme an intriguing target for the treatment of a variety of cancers.  In our latest publication, WuXi AppTec scientists contributed to the discovery and characterization of ZL-2201, a potent and highly selective small molecule DNA-PK inhibitor.  In …Read More >

Resource Type: Latest Science, Publication
Resource Topic: Cell-based Assays, Hit-to-Lead, Lead Optimization, Oncology, Tumor Models

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Control of the Antitumor Activity and Specificity of CAR T Cells via Organic Adapters Covalently Tethering the CAR to Tumor Cells

On-target, off-tumor toxicity is a specific type of toxic side effect that limits the anticancer applicability of chimeric antigen receptor (CAR) T cells. In our latest publication, WuXi AppTec scientists contributed to a study describing how the tumor-targeting specificity and activity of T cells with a CAR (consisting of an antibody that catalytically forms a …Read More >

Resource Type: Latest Science, Publication
Resource Topic: CAR-T Cell, Oncology

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Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors

The KRAS G12D mutation subtype is present in over 40% of pancreatic ductal adenocarcinomas (PDAC), making this an important drug target.  WuXi AppTec scientists recently contributed to a research article in ACS Med. Chem. Letters describing the optimization of a series of potent and selective KRAS G12D inhibitors through a structure-based drug design approach.  The …Read More >

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

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Resource Topics
× peptide, amino acid

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