Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator

@article{Piu2008PharmacologicalCO,
  title={Pharmacological characterization of AC-262536, a novel selective androgen receptor modulator},
  author={Fabrice Piu and Luis R. Gardell and Thomas Son and Nathalie Schlienger and Birgitte W Lund and Hans H. Schiffer and Kimberly E. Vanover and Robert E Davis and Roger Olsson and Stefania Risso Bradley},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2008},
  volume={109},
  pages={129-137}
}
  • F. Piu, L. Gardell, S. Bradley
  • Published 1 March 2008
  • Biology, Medicine
  • The Journal of Steroid Biochemistry and Molecular Biology
Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators.
TLDR
The discovery of ACP-105 (1), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone, is described.
Recent advances in the development of selective androgen receptor modulators
TLDR
A new class of molecules targeting androgen receptors called selective androgen receptor modulators is being developed, analogous to the clinically successful and at present marketed selective estrogen receptors modulators.
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A novel synthetic androgen receptor ligand, S42, works as a selective androgen receptor modulator and possesses metabolic effects with little impact on the prostate.
TLDR
Results of the whole-cell binding assay indicated that S42 specifically binds to AR and progesterone receptor, and this effect of S42 was associated with suppression of the SRBP-1c-mediated lipogenic and insulin-desensitizing pathway in the liver and visceral fat.
Deciphering the selective androgen receptor modulators paradigm
TLDR
The aim of the present paper is to summarize the current standing of research and development of SARMs and plausible molecular mechanisms underlying the potential for selective modulation of androgen receptor (AR) by different ligands and provides an update on SARM discovery paradigms for preclinical evaluations.
Synthesis and biological evaluation of second-generation tropanol-based androgen receptor modulators.
TLDR
This study has identified small yet potent tropanol-based ligands possessing significant antiandrogenic activity with both wild-type AR and the two most common AR ligand binding domain (LBD) mutants.
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
TLDR
This Award Address attempts to chronicle the landmark discoveries, organize the SARM landscape into clinically relevant bins, and provide insight into the clinical prospects for SARMs.
Recent developments in antiandrogens and selective androgen receptor modulators
Equine metabolism of the selective androgen receptor modulator AC-262536 in vitro and in urine, plasma and hair following oral administration.
TLDR
The aim of this study was to investigate the metabolism of AC-262536 in the horse following in vitro incubation and oral administration to two Thoroughbred horses, in order to identify the most appropriate analytical targets for doping control laboratories.
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