title: Structural characteristics of anabolic androgenic steroids contributing to binding to the androgen receptor and to their anabolic and androgenic activities. Applied modifications in the steroidal structure.
abstract: Anabolic androgenic steroids (AAS) are synthetic derivatives of testosterone introduced for therapeutic purposes providing enhanced anabolic potency with reduced androgenic effects. Androgens mediate their action through their binding to the androgen receptor (AR) which is mainly expressed in androgen target tissues, such as the prostate, skeletal muscle, liver and central nervous system. This paper reviews some of the wide spectrum of testosterone and synthetic AAS structure modifications related to the intended enhancement in anabolic activity. The structural features of steroids necessary for effective binding to the AR and those which contribute to the stipulation of the androgenic and anabolic activities are also presented.
authors.affiliation: Doping Control Laboratory of Athens, Olympic Athletic Center of Athens Spyros Louis, Kifisias 37, 15123 Maroussi, Greece.
authors.forename: A G
authors.initials: AG
authors.lastname: Fragkaki
authors.forename: Y S
authors.initials: YS
authors.lastname: Angelis
authors.forename: M
authors.initials: M
authors.lastname: Koupparis
authors.forename: A
authors.initials: A
authors.lastname: Tsantili-Kakoulidou
authors.forename: G
authors.initials: G
authors.lastname: Kokotos
authors.forename: C
authors.initials: C
authors.lastname: Georgakopoulos
mesh_terms: D045930:Anabolic Agents / Q000737:chemistry* / Q000378:metabolism*; D000728:Androgens / Q000737:chemistry* / Q000378:metabolism*; D000818:Animals; D006801:Humans; D011485:Protein Binding; D011944:Receptors, Androgen / Q000378:metabolism*; D013256:Steroids / Q000737:chemistry* / Q000378:metabolism*
chemical_list: D045930:Anabolic Agents; D000728:Androgens; D011944:Receptors, Androgen; D013256:Steroids