ABCB1 transports PREDN,PREDL out of kidney cells

Stable Identifier
Reaction [transition]
Homo sapiens
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ABCB1 (also known as MDR1, P-glycoprotein, or PGP) is the best characterized xenobiotic transporter of the ABC transporter family (Gottesman and Pastan 1988). The presence of 11-, 17-, and 21-hydroxyl groups appears to be a critical determinant for transport efficiency of steroids by ABCB1. Prednisone (PREDN) contains the 17-, and prednisolone (PREDL) both the 17- and 21-hydroxy group, and both molecules are effectively exported out of cells expressing ABCB1 with reduced intracellular accumulation and toxicity (Yates et al, 2003).
Literature References
PubMed ID Title Journal Year
2898143 A retrovirus carrying an MDR1 cDNA confers multidrug resistance and polarized expression of P-glycoprotein in MDCK cells

Gottesman, MM, Lovelace, E, Pastan, I, Ueda, K, Rutherford, AV, Willingham, MC

Proc. Natl. Acad. Sci. U.S.A. 1988
14661924 Structural determinants of P-glycoprotein-mediated transport of glucocorticoids

Swaan, PW, Schuetz, EG, Yates, CR, Yasuda, K, Chang, C, Dalton, JT, Miller, DD, Kearbey, JD

Pharm. Res. 2003
12379510 The role of the efflux transporter P-glycoprotein in brain penetration of prednisolone

De Boer, AG, Meijer, OC, Karssen, AM, De Lange, EC, de Kloet, ER, van der Sandt, IC

J. Endocrinol. 2002
Catalyst Activity

ATPase-coupled transmembrane transporter activity of ABCB1 [plasma membrane]

Orthologous Events
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