SERPINA6 binds PREDN

Stable Identifier
R-HSA-9757688
Type
Reaction [binding]
Species
Homo sapiens
Compartment
ReviewStatus
5/5
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Prednisone (PREDN) reversibly binds to transcortin (corticosteroid-binding globulin, CBG, SERPINA6) (Pugeat et al, 1981). The affinity of prednisolone (PREDL) to SERPINA6 is higher than that of PREDN, and PREDN is displaced by PREDL in concentrations above 5:1 excess of PREDL (Ferry and Wagner, 1987; Boudinot and Jusko, 1984). The binding sites for PREDN and PREDL are different (Legler and Benet, 1986). With therapeutic PREDN doses, PREDL plasma concentrations exceed those of PREDN by four to tenfold (Rose et al, 1981).

The capacity of SERPINA6 to bind PREDN and PREDL is limited, with albumin (ALB) weakly binding the excess. Steroids bound to SERPINA6 are released when local conditions, like the proteolytic milieu of inflamed tissue, change the allosteric configuration of SERPINA6 (Zhou et al, 2008; reviewed by Henley et al, 2016).
Literature References
PubMed ID Title Journal Year
27411675 Cortisol and CBG - Getting cortisol to the right place at the right time

Henley, D, Carrell, R, Lightman, S

Pharmacol Ther 2016
6492791 Plasma protein binding interaction of prednisone and prednisolone

Boudinot, FD, Jusko, WJ

J Steroid Biochem 1984
7195405 Transport of steroid hormones: interaction of 70 drugs with testosterone-binding globulin and corticosteroid-binding globulin in human plasma

Nisula, BC, Pugeat, MM, Dunn, JF

J Clin Endocrinol Metab 1981
18513745 The S-to-R transition of corticosteroid-binding globulin and the mechanism of hormone release

Stanley, PL, Read, RJ, Wei, Z, Carrell, RW, Stein, PE, Zhou, A

J Mol Biol 2008
3709632 The effect of prednisone and hydrocortisone on the plasma protein binding of prednisolone in man

Legler, UF, Benet, LZ

Eur J Clin Pharmacol 1986
7310640 Dose dependent pharmacokinetics of prednisone and prednisolone in man

Yurchak, AM, Jusko, WJ, Rose, JQ

J Pharmacokinet Biopharm 1981
3593903 The nonlinear pharmacokinetics of prednisone and prednisolone. II. Plasma protein binding of prednisone and prednisolone in rabbit and human plasma

Ferry, JJ, Wagner, JG

Biopharm Drug Dispos 1987
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