Transporter Screening & Profiling Services
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Membrane transporters are critical proteins that regulate the absorption, distribution, and excretion of both endogenous substances and exogenous drugs. They are widely expressed in key tissues, including the intestine, liver, kidney, and blood-brain barrier. Based on structure and function, transporters are primarily classified into two major families: ATP-binding cassette (ABC) transporters (e.g., P-gp, BCRP, MRP2), which mediate drug efflux and reduce intracellular drug accumulation, and solute carrier (SLC) transporters (e.g., OATP, OCT, OAT, MATE), which facilitate drug uptake and influence tissue distribution and clearance.
Figure 1. Intrinsic and extrinsic factors modulate drug transporter function through mechanisms such as regulatory pathways or inhibition. (Galetin A, et al., 2024)
In drug development, determining whether a candidate compound is a substrate or inhibitor of specific transporters is essential for predicting pharmacokinetics, drug–drug interaction potential, and toxicity. Regulatory agencies such as the FDA, EMA, and ICH recommend systematic in vitro transporter studies early in development to assess potential transporter-mediated drug interactions.
Comprehensive Transporter Analysis Platform
Leveraging years of expertise in transporter biology, Creative Biogene has established an integrated screening and characterization platform covering major transporter targets, supporting end-to-end needs from early discovery to preclinical development.
ABC Transporters Screening and Profiling Assays
Our services evaluate key efflux transporters, including P-gp, BCRP, and MRP2:
- Membrane Vesicle Assays: Use high-expression vesicle systems to directly measure ATP-dependent substrate efflux.
- Bidirectional Transport Assays: Employ polarized cell models (e.g., Caco-2, MDCK-MDR1) to assess transcellular transport and efflux ratios.
- Accumulation Assays: Utilize fluorescent substrates (e.g., Calcein-AM, Rhodamine 123) to quantify the inhibitory effects of efflux modulators.
SLC Transporters Screening and Profiling Services
We cover major uptake transporters, including OATP1B1/1B3, OAT1/3, OCT2, MATE1/2-K:
- Stable Transfected Cell Lines: HEK293 or MDCK cells overexpressing single transporters for substrate uptake and inhibition studies.
- Primary Cell Models: Human hepatocytes or renal proximal tubule epithelial cells to simulate in vivo transporter environments.
- High-Content Screening: Automated uptake assays in multiwell formats, suitable for large-scale compound libraries.
Advanced Technologies
To meet complex drug development requirements, we continually integrate innovative technologies and model systems:
- Dual-Transfected Cell Models: Simultaneous expression of uptake and efflux transporters (e.g., MDCK-OCT2-MATE1) to mimic vectorial transport in kidney or liver, providing physiologically relevant clearance predictions.
- Gene-Edited Cell Lines: CRISPR/Cas9-mediated knockout (KO) or knockdown (KD) of transporters (e.g., Caco-2 P-gp KO) to eliminate endogenous transporter interference and enhance data specificity.
- Time-Dependent Inhibition Assessment: Pre-incubation studies for OATP1B, OAT, and OCT transporters to more accurately predict clinical DDI risk.
- Transporter Induction Studies: Using primary hepatocytes or intestinal epithelial cells to evaluate drug effects on transporter expression.
- Complex In Vitro Models: 3D spheroids, organoids, and microphysiological systems to study multi-transporter interactions under physiologically relevant conditions.
Technical Advantages and Service Assurance
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Comprehensive Target Coverage
Includes all major transporters recommended by ICH, with options for customized target development.
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Multiple Detection Modalities
Fluorescence, radiolabeling, and LC–MS/MS platforms to accommodate diverse compound properties.
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Standardization and Reproducibility
Strict adherence to regulatory guidelines, with validated workflows ensuring reliable and cross-platform comparable data.
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Expert Scientific Support
Our team combines deep transporter biology and drug metabolism expertise, providing full-cycle support from experimental design to data interpretation.
Collaboration Approach
Creative Biogene is committed to delivering flexible and efficient transporter screening and characterization solutions. Whether for routine screening or complex mechanistic studies, we can design customized experimental strategies tailored to project requirements. For further information or to discuss potential collaboration, please contact our scientific team.
* For research use only. Not intended for any clinical use.
