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Gene Review

ABCC1  -  ATP-binding cassette, sub-family C...

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Disease relevance of ABCC1

  • CONCLUSIONS: HIV-1 protease inhibitors potently interact with both P-gp and MRP-related transporters in BBMEC [1].

High impact information on ABCC1

  • Similarly, ABCC1 transcript levels were induced in granulosa cells 12-39 h after hCG [2].
  • The objective of this study was to investigate the regulation of EST and ABCC1 during human chorionic gonadotropin (hCG)-induced ovulation/luteinization [2].
  • In contrast, no significant changes in either EST or ABCC1 were detected in theca interna samples after hCG [2].
  • The transcripts for EST and ABCC1 were cloned by RT-PCR, and the regulation of their mRNAs was studied in preovulatory follicles obtained during estrus at 0, 12, 24, 30, 33, 36, and 39 h after hCG [2].
  • The present study demonstrates that follicular luteinization is accompanied not only by a decrease in 17 beta-estradiol biosynthesis but also by an increase in expression of genes responsible for estrogen inactivation and elimination from granulosa cells, such as EST and ABCC1, respectively [2].

Biological context of ABCC1

  • Drugs demonstrating a significant effect were further quantitated using an expanded concentration range and a nonlinear regression curve fit to determine the potency (IC50) and efficacy (Imax) of the drug for P-gp and/or MRP [3].
  • These results likely reflect an interaction of the ester form with P-gp and BCRP during the initial accumulation process, and an interaction of the free acid form with MRP after hydrolysis in the cell [4].

Anatomical context of ABCC1


Associations of ABCC1 with chemical compounds

  • In the presence of inhibitors such as 2,4-dinitrophenol (1 mM) and quinidine (1 mM), etoposide showed an increase in Jm-s and a decrease in Js-m. The etoposide efflux was unaffected in the presence of a specific multiresistance associated protein 1 (MRP1) inhibitor (MK571) and methotrexate, a substrate for BCRP and MRP1-4 [7].
  • In the presence of metabolic inhibitors (ouabain and 2,4-dinitrophenol) and P-glycoprotein (P-gp)/multidrug resistance protein 1 (MRP1) inhibitors (quinidine and verapamil), the J(m-s) increased and J(s-m) decreased significantly [6].

Analytical, diagnostic and therapeutic context of ABCC1

  • Results obtained from RT-PCR/Southern blot analyses showed significant changes in steady-state levels of both EST and ABCC1 mRNA after hCG treatment (P < 0.05) [2].


  1. Quantitative assessment of HIV-1 protease inhibitor interactions with drug efflux transporters in the blood-brain barrier. Bachmeier, C.J., Spitzenberger, T.J., Elmquist, W.F., Miller, D.W. Pharm. Res. (2005) [Pubmed]
  2. Human chorionic gonadotropin-dependent up-regulation of genes responsible for estrogen sulfoconjugation and export in granulosa cells of luteinizing preovulatory follicles. Brown, K.A., Doré, M., Lussier, J.G., Sirois, J. Endocrinology (2006) [Pubmed]
  3. A fluorometric screening assay for drug efflux transporter activity in the blood-brain barrier. Bachmeier, C.J., Miller, D.W. Pharm. Res. (2005) [Pubmed]
  4. Drug efflux transport properties of 2',7'-bis(2-carboxyethyl)-5(6)-carboxyfluorescein acetoxymethyl ester (BCECF-AM) and its fluorescent free acid, BCECF. Bachmeier, C.J., Trickler, W.J., Miller, D.W. Journal of pharmaceutical sciences. (2004) [Pubmed]
  5. Plasma membrane localization of multidrug resistance-associated protein homologs in brain capillary endothelial cells. Zhang, Y., Schuetz, J.D., Elmquist, W.F., Miller, D.W. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  6. Carrier mediated transport of chlorpheniramine and chlorcyclizine across bovine olfactory mucosa: implications on nose-to-brain transport. Kandimalla, K.K., Donovan, M.D. Journal of pharmaceutical sciences. (2005) [Pubmed]
  7. Localization and differential activity of P-glycoprotein in the bovine olfactory and nasal respiratory mucosae. Kandimalla, K.K., Donovan, M.D. Pharm. Res. (2005) [Pubmed]
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