Drug Discovery Services
Inhibitor Screening Against 15-Lipoxygenase
Advance your anti-inflammatory and metabolic disease programs with recombinant 15-lipoxygenase (15-LOX) enzyme production, functional characterization, and inhibitor screening services. We provide the enzyme supply and high-throughput screening infrastructure needed to identify and characterize small molecule inhibitors of 15-LOX-1 and 15-LOX-2, enabling hit-to-lead programs targeting lipoxygenase pathways.
What Is 15-Lipoxygenase Inhibitor Screening?
15-lipoxygenases (15-LOX) are mammalian enzymes that oxygenate arachidonic acid and other polyunsaturated fatty acids, playing key regulatory roles in inflammatory and metabolic pathways. 15-LOX-1 has been implicated in CNS and inflammatory lung diseases, while 15-LOX-2 is a target in epithelial and metabolic contexts. Identifying selective small molecule inhibitors of these enzymes is a critical step in developing anti-inflammatory therapeutics.
Our inhibitor screening service combines recombinant enzyme production, activity-based assays, and screening workflows to support your hit-to-lead programs. We produce functional 15-LOX enzymes, run activity assays that detect hydroperoxides generated during lipoxygenation, and screen compound libraries to identify novel inhibitors. This integrated approach enables you to progress from target validation to lead optimization with confidence.
Screening strategies commonly used in the field include virtual screening of compound databases followed by biological assay validation, as well as high-throughput screening of commercial compound collections. Our service is designed to support both approaches, providing the enzyme supply and assay infrastructure needed to execute your screening campaign.
Recombinant 15-LOX Production
Reliable access to functional 15-LOX-1 and 15-LOX-2 enzymes is essential for screening programs. We produce recombinant enzymes with the quality and consistency needed for assay development and inhibitor screening.
- Mammalian arachidonic acid 15-lipoxygenase expression
- Purified enzyme suitable for activity assays
- Batch consistency for reproducible screening results
Activity-Based Screening Assays
Our assays detect hydroperoxides produced during the lipoxygenation reaction, providing a direct readout of enzyme activity and inhibition. This approach is widely used for 15-LOX inhibitor screening.
- Hydroperoxide detection for activity measurement
- Compatible with inhibitor screening workflows
- Designed for 15-LOX-1 and 15-LOX-2 isoforms
Hit Identification and Validation
From virtual screening hits to validated lead compounds, we support the identification and characterization of 15-LOX inhibitors through integrated screening and biological evaluation.
- Virtual screening combined with biological assays
- Compound library screening for novel inhibitor discovery
- Hit confirmation and preliminary characterization
Why Screen Against 15-Lipoxygenase?
15-lipoxygenases are emerging drug targets in inflammatory and metabolic diseases. 15-LOX-1 plays an important regulatory role in CNS and inflammatory lung conditions, while 15-LOX-2 has been studied in epithelial contexts. Inhibitors of these enzymes have potential therapeutic applications in conditions where lipoxygenase pathway activity drives pathology.
Recent research has identified novel 15-LOX inhibitors through various approaches, including virtual screening of compound databases, high-throughput screening of commercial libraries, and structure-based design. These efforts have yielded inhibitors with varying selectivity profiles across lipoxygenase isoforms, highlighting the importance of thorough screening and characterization in drug discovery programs.
| Target | Disease Relevance | Screening Approach | Key Considerations |
|---|---|---|---|
| 15-LOX-1 | CNS and inflammatory lung diseases | Virtual screening + biological assays | Selectivity over other lipoxygenase isoforms |
| 15-LOX-2 | Epithelial and metabolic contexts | Shape-based virtual screening | Isoform-specific inhibitor design |
| ALOX15 | Inflammatory and metabolic pathways | High-throughput screening of commercial compounds | Drug screening against ALOX15 targets |
| Soybean 15-LOX | Model system for inhibitor studies | Natural product screening | Polymethoxylated flavonoids as inhibitor scaffolds |
How Our Screening Service Works
Our 15-lipoxygenase inhibitor screening service follows a structured workflow designed to deliver actionable results for your drug discovery program. From enzyme production to hit characterization, each step is designed to support the identification and development of selective 15-LOX inhibitors.
Enzyme Expression and Purification
We produce recombinant 15-LOX-1 or 15-LOX-2 enzymes using mammalian expression systems. The purified enzyme is quality-checked for activity and stability, ensuring a reliable reagent for downstream screening assays.
Assay Development and Validation
Activity assays are developed to detect hydroperoxides produced during the lipoxygenation reaction. Assay conditions are optimized for sensitivity and reproducibility, providing a robust readout for inhibitor screening.
Compound Screening
Compound libraries are screened against the target enzyme using the validated assay. Screening can be configured for virtual screening hits, focused libraries, or broader collections depending on your program needs.
Hit Validation and Characterization
Primary hits are confirmed in dose-response experiments to determine potency. Selectivity profiling across related lipoxygenase isoforms helps identify compounds with the desired target specificity.
Customization Options
Every drug discovery program has unique requirements. We offer flexible service configurations to match your specific screening goals, target isoforms, and compound collections.
Our team works with you to design a screening campaign that fits your program's stage and objectives. Whether you need enzyme supply, full screening services, or support for virtual screening validation, we can tailor the service to your needs.
15-LOX-1 or 15-LOX-2
Choose the specific 15-lipoxygenase isoform relevant to your therapeutic area. Both enzymes are produced as recombinant proteins for screening applications.
- 15-LOX-1 for CNS and inflammatory lung programs
- 15-LOX-2 for epithelial and metabolic targets
- Custom isoform configurations on request
Assay Configuration
Assays can be configured to match your screening throughput needs, from focused validation studies to larger compound library screens.
- Hydroperoxide detection-based activity assays
- Compatible with virtual screening hit validation
- Flexible plate formats for screening campaigns
Results and Reporting
Comprehensive data packages support your decision-making, including raw data, analysis, and documentation suitable for internal review and further development.
- Dose-response curves and IC₅₀ determinations
- Selectivity data across lipoxygenase isoforms
- Documentation for program records
Screening Approaches We Support
The 15-LOX inhibitor field has employed multiple screening strategies to identify novel compounds. Our service is designed to support the approaches most commonly used in current drug discovery efforts.
Virtual screening has become a powerful tool for identifying 15-LOX inhibitors, with studies using shape-based matching, Bayesian classifier models, and structure-based approaches to filter compound databases. These computational hits require biological validation, which our enzyme and assay services provide.
| Approach | Application | Evidence | Our Support |
|---|---|---|---|
| Virtual Screening | Filter compound databases for potential inhibitors | Used for h15-LOX-2 inhibitor identification | Biological assay validation of computational hits |
| High-Throughput Screening | Screen large compound collections | Identified potent selective inhibitors of h15-LOX-1 | Enzyme supply and activity assays for HTS campaigns |
| Natural Product Screening | Discover inhibitors from natural sources | Identified 15-LOX inhibitors from Chinese herbal medicine | Assay support for natural product library screening |
| Fragment-Based Screening | Identify fragment hits for medicinal chemistry | Applied to nitrogen-containing fragment collections | Enzyme production for fragment screening assays |
Deliverables and Quality Control
Our service is designed to provide you with the data and reagents needed to advance your 15-LOX inhibitor program. Deliverables are structured to support internal decision-making and further development activities.
Quality control is integrated throughout the workflow, from enzyme production to final data reporting. Each step includes appropriate checks to ensure the reliability of your results.
| Deliverable | Description | QC Measure | Application |
|---|---|---|---|
| Recombinant Enzyme | Purified 15-LOX-1 or 15-LOX-2 protein | Activity verification post-purification | Assay development and screening |
| Assay Data | Activity measurements and inhibition curves | Positive and negative controls included | Hit identification and potency assessment |
| Screening Results | Compound screening outcomes | Replicate measurements for reproducibility | Hit list prioritization |
| Characterization Report | Potency and selectivity data | Cross-isoform comparison where applicable | Lead selection and optimization |
Applications in Drug Discovery
15-lipoxygenase inhibitor screening supports multiple stages of the drug discovery pipeline, from target validation through lead optimization. Our service is applicable to programs targeting inflammatory diseases, CNS conditions, and metabolic disorders.
The identification of selective 15-LOX inhibitors is an active area of research, with recent studies reporting novel inhibitor classes and screening methodologies. Our service provides the enzyme and assay infrastructure to support these efforts.
Lead Identification
Screen compound libraries to identify novel 15-LOX inhibitor scaffolds for medicinal chemistry optimization.
- Primary screening of focused or diverse libraries
- Hit confirmation and preliminary SAR
- Support for medicinal chemistry programs
Pathway Studies
Use selective inhibitors to probe 15-LOX function in disease-relevant models and validate target engagement.
- Tool compound generation support
- Selectivity assessment across LOX isoforms
- Mechanistic studies
Natural Product Screening
Evaluate natural product libraries for 15-LOX inhibitory activity, supporting natural product drug discovery programs.
- Screening of botanical and natural extracts
- Bioassay-guided fractionation support
- Active compound identification
Why Choose Our Service
Our 15-lipoxygenase inhibitor screening service combines enzyme production expertise with screening assay capabilities, providing an integrated solution for your drug discovery program. We understand the specific requirements of lipoxygenase-targeted screening and design our service to meet those needs.
We work collaboratively with your team to configure the service to your program's requirements. From enzyme supply to full screening campaigns, we provide the support you need to advance your 15-LOX inhibitor program.
Technical Considerations
15-lipoxygenase inhibitor screening requires careful attention to assay design and enzyme quality. Our service incorporates best practices from the field to ensure reliable results.
The lipoxygenase activity assay detects hydroperoxides produced during the lipoxygenation reaction, providing a direct measure of enzyme activity. This approach is well-established for inhibitor screening and is compatible with both purified enzyme and cellular assays.
FAQ
What 15-lipoxygenase isoforms can you screen against?
We provide screening services for both 15-LOX-1 and 15-LOX-2, the two main mammalian arachidonic acid 15-lipoxygenases. 15-LOX-1 is relevant to CNS and inflammatory lung disease programs, while 15-LOX-2 is studied in epithelial and metabolic contexts. The specific isoform configuration for your program can be discussed with our team.
What types of compound libraries can be screened?
Our screening service can accommodate various compound collections, including virtual screening hits, focused libraries, and larger collections. The screening format is configured based on your program's needs and the number of compounds to be evaluated. We work with you to design a screening campaign appropriate for your stage of drug discovery.
How is 15-LOX enzyme activity measured in the screening assay?
The screening assay detects hydroperoxides produced during the lipoxygenation reaction, providing a direct readout of enzyme activity. This approach is well-established for lipoxygenase inhibitor screening and allows for the measurement of inhibition in the presence of test compounds. Assay conditions are optimized for sensitivity and reproducibility.
Can you support both virtual screening validation and high-throughput screening?
Yes, our service is designed to support multiple screening approaches. We can validate hits from virtual screening campaigns using biological assays, and we can also support high-throughput screening of larger compound collections. The specific approach is tailored to your program's screening strategy and objectives.
What data will I receive from the screening service?
You will receive comprehensive data packages including enzyme activity measurements, dose-response curves for hit confirmation, and selectivity data where applicable. Raw data and analysis are provided to support your internal decision-making. Documentation is suitable for program records and further development activities.
References
- Li Y, Zhang Y, Wu X. Discovery of natural 15-LOX small molecule inhibitors from Chinese herbal medicine using virtual Screening, biological evaluation and molecular dynamics studies. Bioorg Chem 2021 Oct. View on PubMed
- Mahboubi-Rabbani M, Zarghi A. Lipoxygenase Inhibitors as Cancer Chemopreventives: Discovery, Recent Developments and Future Perspectives. Curr Med Chem 2021. View on PubMed
- Saeed A, Khan SU, Saeed M. Synthesis of novel hybrid pharmacophore of N-((4-sulfamoylphenyl)carbamothioyl)alkanamides as potent carbonic anhydrase-II and 15-lipoxygenase inhibitors. Drug Dev Res 2022 May. View on PubMed
- Yasin M, Shahid W, Ashraf M. Targeting new N-furfurylated 4-chlorophenyl-1,2,4-triazolepropionamide hybrids as potential 15-lipoxygenase inhibitors supported with in vitro and in silico studies. J Biomol Struct Dyn 2023 Jul. View on PubMed
- Identification of novel human 15-lipoxygenase-2 (h15-LOX .. by LG Viviani · 2024 · Cited by 11 — Using a virtual screening approach, they filtered a curated ZINC database for compounds with the potential to inhibit h15-LOX-2. View article
- Eleftheriadis N, Poelman H, Leus NGJ. Design of a novel thiophene inhibitor of 15-lipoxygenase-1 with both anti-inflammatory and neuroprotective properties. Eur J Med Chem 2016 Oct 21. View on PubMed
Advance Your 15-LOX Inhibitor Program
Contact our team to discuss how our 15-lipoxygenase inhibitor screening service can support your drug discovery program. We'll work with you to configure a service that meets your program's specific requirements.