Research Overview
What a selective androgen receptor modulator is
The androgen receptor is a ligand-activated transcription factor. When bound, it translocates to the nucleus, dimerises and engages androgen response elements, recruiting coactivators and corepressors whose availability differs from tissue to tissue. Steroidal androgens are also substrates for 5-alpha-reductase and aromatase, generating dihydrotestosterone and oestradiol respectively. Non-steroidal ligands such as ACP-105 sidestep those conversions entirely, and the resulting difference in receptor conformation is the mechanistic basis on which tissue-selective effects were pursued.
Where ACP-105 sits in the class
Typical laboratory readouts
- Competitive binding affinity and transactivation potency in AR-reporter cell lines
- Tissue-weight endpoints in castrated rodent models: levator ani and prostate compared side by side
- Bone mineral density and microarchitecture by micro-CT
- Target gene expression panels distinguishing muscle from prostate transcriptional programmes
- Behavioural and cognitive batteries where central androgen receptor signalling is the variable