Creative Biogene is the leading biotechnology company offering the best services in SLC (Solute Carrier Transporters) transporters. With years of experiences in transporters-based drug discovery, our talented researches with abundant expertise provide a wide range of SLC transporters screening and profiling assays. Creative Biogene has confidence in accelerating your SLC transporters-based drug discovery with the most competitive price.
Creative Biogene provides a series of solute-linked carrier superfamily members, including proton dependent oligopeptide transporters (PEPT1, PEPT2, PHT1; SLC15A family), organic anion transporting polypeptides (OATPs; SLC21A), organic cation transporters (OCTs; SLC22A family), organic anion transporters (OATs; SLC22A), nucleoside transporters (CNT and ENT; SLC28A and 29A family), plasma membrane monoamine transporter (PMAT; SLC29 family), the monocarboxylate transporters (MCT; SLC16A family) and MATEs and the neurotransmitter transporters (Serotonin; Norepinephrine; Dopamine, Adenosine, GABA, Glutamate).
SLC transporters play an important role in intestinal absorption, blood-brain barrier penetration and excretion into the bile and urine. To evaluate whether a test compound is a substrate of these transporters, the accumulation of the transporter expressing cells and control cells is measured. By measuring the efficiency of the test compound to reduce the uptake of a probe substrate into the cells, inhibition is also evaluated.
Fig.1 Schematic model of the SLC transporters in major organs responsible for drug disposition (Qing, et al. 2014)
There are 11 known human OATPs, divided into six subfamilies based on their amino acid sequence similarities (Qing, et al. 2014). In OATPs families, two main organic anion transporting polypeptides, OATP1B1 (OATP-C, OAT2, SLCO1B1) and OATP1B3 (OATP-8, SLCO1B3) are mostly expressed in the liver and are involved in the distribution of drugs from the sinusoidal blood to hepatocytes. For OATP transporters, Pravastatin is a typical substrate and rifampin is a typical inhibitor.
There are two main members of this organic cation transporter family, which are OCT1 (SLCO22A1) and OCT2 (SLCO22A2). OCT is usually expressed on the sinusoidal membrane of hepatocytes and transport compounds from the blood into the liver. However, OCT2 is mainly expressed on the basolateral membrane of renal proximal tubules and transport compounds from the blood into proximal tubules. For OCT transporters, metformin is a typical substrate and cimetidine is a typical inhibitor.
OAT1 (SLC22A6) and OAT3 (SLC22A8) are organic anion transporters, mainly expressed in the kidney. In addition, they also transport compounds or drugs into the proximal tubules for further excretion into urine. Inhibitors of OAT might inhibit the excretion of neurotransmitter metabolites and some drugs causing adverse effects. For OAT1, acyclovir, cidovir and methotrexate are substrates. For OAT3, furosemide, estrone sulfate and NSAIDs are substrates. Probenecid and Novobiocin are inhibitors for both OAT1 and OAT3.
MATE1 (multidrug and Toxin Extrusion 1 or SLC47A1) and MATE2K (multidrug and Toxin Extrusion 2K or SLC47A2) are transporters which are mainly expressed in the renal proximal tubule and play function in the secretion of cations into the urine. MATE1 is also expressed at the canalicular membrane of hepatocytes involved in biliary excretion. MATE transporters have similar characters in substrate specificity and work in tandem with OCT transporters. For MATE, metformin and N-methylpyridinium are common substrates, and cimetidine and pyrimethamne are common inhibitors.
Neurotransmitter transporters are a class of neurons membrane transport proteins, function in carrying neurotransmitters across these membranes and to direct their further transport to specific intracellular locations. Neurotransmitter transporters have been a highly successful target class for clinical therapeutics. First generation Selective Serotonin Re-Uptake inhibitors (SSRIs) are one of the most recognized class of drugs to treat depression.
Creative Biogene is dedicating to assisting you to screen and profile compounds against SLC transporter targets in your drug discovery project. As a pioneer in this field, Creative Biogene can offer you an effective and advanced platform, with quick turnaround and the highest quality to screen the compounds with the greatest chance to succeed. Our goal is to become your reliable partner and tailor the best-fit method to meet your specific demands and facilitate your project research.
If you have any special requirements in SLC transporter assays, please feel free to contact us at email@example.com or 1-631-626-9181. We are looking forward to working together with your attractive projects.
Qing, L. and Yan, S. (2014) ‘Role of solute carriers in response to anticancer drugs’, Molecular and Cellular Therapies, 2, 15