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Info
Catalogue Number | 157847 |
Antigen/Gene or Protein Targets | CLEFF4 |
Parental Line | Caco-2 |
Host | Human |
Tissue | Colon |
Model | Mutant |
Relevance |
Pharmaceutical drug development requires drug targets to be characterised against efflux transporters. An example is P-glycoprotein (P-gp) which prevents the uptake and trans-cellular transport of hundreds of drug groups. The standard model is to use Caco-2 cells as these can be induced to express high concentrations of P-gp. Said tight junction model can approximate the role of P-gp at the barrier sites in the body including the gastrointestinal tract and also the blood-brain-barrier. There are however limitations to the Caco-2 cell line, including taking 24 days to develop the characteristics required for P-gp-mediated efflux modelling. Further, other efflux proteins including BCRP and MRP2 are often present in Caco-2 cells, which add extra variables when characterising specific P-gp mediated effects. The CLEFF4 cell line is ready to use in just 5 days and has a 3-fold higher expression of P-gp cells at 5-7 days compared to Caco-2 cells at day 21, expressing no more MRP2 and less BCRP than the parent Caco-2 cells. This is a faster, more specific model for P-gp assays offering cost and time savings and which has reduced medium requirement (one can use standard not accelerated media). |
Research Area | Drug Discovery & Development |
References: 1 entry
P-Glycoprotein-Mediated Efflux Using a Rapidly Maturing Caco2 Clone (CLEFF4) in Only 5 Days without Requiring Modified Growth Medium
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References: 1 entry
P-Glycoprotein-Mediated Efflux Using a Rapidly Maturing Caco2 Clone (CLEFF4) in Only 5 Days without Requiring Modified Growth Medium
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