Knowledge Library

Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase

Structure-based design was utilized to optimize 6,6-diaryl substituted dihydropyrone and hydroxylactam to obtain inhibitors of lactate dehydrogenase (LDH) with low nanomolar biochemical and single-digit micromolar cellular potencies. Surprisingly the replacement of a phenyl with a pyridyl moiety in the chemical structure revealed a new binding mode for the inhibitors with subtle conformational change of the …Read More >

Resource Type: Publication
Resource Topic: Chemical Biology and Proteomics Discovery Chemistry Hit-to-Lead Lead Optimization Oncology Small Molecules

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Drug Discovery: Screening Approaches for Rapid Assessment of Target Tractability

Resource Type: Webinar
Resource Topic: Biophysical Assays DNA-Encoded Library (DEL) Fragment-Based Drug Discovery Hit Finding Hit-to-Lead Screening Libraries Small Molecules Target Identification and Validation Target-Specific Assays

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HIJACKING CELLULAR MECHANISMS TO TREAT COMPLEX DISEASES

Resource Type: White Paper
Resource Topic: Biochemical Assays Biomarkers Biophysical Assays Cell-based Assays DRUG DISCOVERY AND INNOVATION in vitro biology Oligonucleotides Oncology Rare Diseases Target Identification and Validation Target-Specific Assays Targeted Protein Degradation

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RARE DISEASES: OPPORTUNITIES AND CHALLENGES FOR TREATMENTS DELIVERED BY ADENO-ASSOCIATED VIRUSES

Resource Type: White Paper
Resource Topic: Biomarkers Gene Therapies in vivo Pharmacology Rare Diseases Target Identification and Validation

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Optimizing Drug Pipelines With Biophysical Methods

Download our whitepaper on how using biophysical techniques can enhance and streamline processes throughout the drug discovery and validation cycle. Discover fresh opportunities to characterize challenging drug targets, examine biophysical screening methods, and look toward what’s next for biophysical methods in drug discovery.

Resource Type: White Paper
Resource Topic: Biochemical Assays Biophysical Assays Discovery Chemistry DNA-Encoded Library (DEL) Fragment-Based Drug Discovery Hit Finding Hit-to-Lead Mass Spectrometry-based Assays Screening Libraries Small Molecules Structural Biology Target Identification and Validation Target-Specific Assays

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Brain metastasis mouse models for the evaluation of multikinase inhibitors on ROS1-fusion-positive lung cancer

Lung cancer is the leading cause of cancer-related death worldwide.  Nearly 80% of lung cancers are non-small cell lung cancer (NSCLC) and 60% of them are diagnosed at the metastatic stage. Brain metastases affect more than 20% of NSCLC patients with poor prognosis and disabling symptoms. However, few therapies have been approved for the treatment …Read More >

Resource Type: Poster
Resource Topic: in vivo Pharmacology Lead Optimization Oncology Small Molecules Tumor Models

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Developing a panel of orthotopic syngeneic tumor models for IO drug discovery

The efficacy of immuno-oncology therapies needs to be evaluated in animal models with functional immune systems. Syngeneic tumor models are established by inoculating mouse cancer cell lines into immunocompetent mice with the same genetic background. The host mice have complete immune activity and show histocompatibility with homograft tumor tissues, which can maximize the simulation of …Read More >

Resource Type: Poster
Resource Topic: Antibodies in vivo Pharmacology Lead Optimization Oncology Target Identification and Validation Tumor Models

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Evaluation of the efficacy of ADC in vitro and in vivo

Abstract Antibody drug conjugates (ADCs) are promising complexes with therapeutic potential that aimed to the treatment of solid tumor and hematological malignancies. Compared with the therapeutic monoclonal antibody, an ADC-derived monoclonal antibody is conjugated with cytotoxic agents (payloads) which can deliver potent cellular toxins to targeted cancer cells specifically. We have established a state-of-the-art platform …Read More >

Resource Type: Poster
Resource Topic: Antibody Drug Conjugate Biochemical Assays Biomarkers Cell-based Assays Immunology in vitro biology Lead Optimization Oncology Tumor Models

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WuXi Discovery Services Newsletter: November 2021

Resource Type: Newsletter
Resource Topic: Biophysical Assays Central Nervous System & Pain Oligonucleotides Rare Diseases Targeted Protein Degradation

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Resource Topics
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