439
Antitumor Steroids
Guy Leclercq
Institut J. Bordet, Universit´e Libre de Bruxelles, Brussels, Belgium
1
Background
440
2
Steroid Hormone Receptors
441
2.1
Structure and Conformation of the Hormone Binding Domains
441
2.2
Conformational Changes of Ligand-binding Domains Induced by
Agonists or Antagonists
442
3
Restrictive Conditions for EfFcient Targeting of Antitumor Estrogens
445
3.1
Main Structural Requirements for Estradiol Binding
446
3.1.1
A-ring
446
3.1.2
B-ring
446
3.1.3
C-ring
446
3.1.4
D-ring
447
3.2
Nucleocytoplasmic Shuttle of Estrogen Receptors
447
3.3
Ligand-induced Regulation of Estrogen Binding Capacity
448
3.4
Ligand-induced Regulation of Estrogen Receptor Level
449
4
Antitumor Estrogens
449
4.1
Organometallic Estradiol Derivatives
450
4.1.1
A-ring Complexion
450
4.1.2
7
α
and 11
β
Derivatives
451
4.1.3
17
α
Derivatives
451
4.2
Radiolabeled Estradiol Derivatives
453
4.2.1
123
Iand
125
I Labeled Compounds
454
4.2.2
α
-Emitting Compounds
455
4.3
Electrophilic 11
β
Derivative
456
Bibliography
457
Books and Reviews
457
Primary Literature
457
Encyclopedia of Molecular Cell Biology and Molecular Medicine, 2nd Edition
. Edited by Robert A. Meyers.
Copyright
2004 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
ISBN: 3-527-30543-2
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