Template:Affinities of 5α-dihydroethisterone for steroid hormone proteins

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Affinities of 5α-dihydroethisterone for steroid hormone proteins

AR ERα ERβ PR GR SHBG
IC50 RBA IC50 RBA IC50 RBA IC50 RBA IC50 RBA Kd RBA
0.5–16 nM 38–100% 229 nM 3.5% >10,000 nM IA 130 nM 12% 7 nM 120% 0.18 nM 100%
Notes: IC50 values are for binding inhibition (affinity). Reference ligands for RBA (100%) were DHT for the AR, estradiol for the ERα and ERβ, progesterone for the PR, dexamethasone for the GR, and DHT for SHBG. Sources: [1][2][3][4][5]
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References

  1. Lemus AE, Enríquez J, García GA, Grillasca I, Pérez-Palacios G (January 1997). "5alpha-reduction of norethisterone enhances its binding affinity for androgen receptors but diminishes its androgenic potency". J. Steroid Biochem. Mol. Biol. 60 (1–2): 121–9. doi:10.1016/S0960-0760(96)00172-0. PMID 9182866.
  2. Ahlem C, Kennedy M, Page T, Bell D, Delorme E, Villegas S, Reading C, White S, Stickney D, Frincke J (February 2012). "17α-alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism". Invest New Drugs. 30 (1): 59–78. doi:10.1007/s10637-010-9517-0. PMID 20814732.
  3. Cunningham GR, Lobl TJ, Cockrell C, Shao TC, Tindall DJ (May 1983). "Characterization of steroid binding specificity of the androgen receptor in human foreskin fibroblasts". Steroids. 41 (5): 617–26. doi:10.1016/0039-128X(83)90027-2. PMID 6658893.
  4. Cunningham GR, Tindall DJ, Lobl TJ, Campbell JA, Means AR (September 1981). "Steroid structural requirements for high affinity binding to human sex steroid binding protein (SBP)". Steroids. 38 (3): 243–62. doi:10.1016/0039-128X(81)90061-1. PMID 7197818.
  5. Cherkasov A, Ban F, Santos-Filho O, Thorsteinson N, Fallahi M, Hammond GL (April 2008). "An updated steroid benchmark set and its application in the discovery of novel nanomolar ligands of sex hormone-binding globulin". J. Med. Chem. 51 (7): 2047–56. doi:10.1021/jm7011485. PMID 18330978.