Non-steroidal steroid receptor modulators.
The last ten years much attention has been focused on the finding of non-steroidal ligands for steroidal nuclear receptors for reasons such as diminishing cross-reactivity to eliminate side effect profiles, changing physicochemical properties which might cause different tissue distribution profiles and altering binding modes which influence the binding of cofactors. Compounds with a selective functionality profile are referred to as selective nuclear receptor modulators (e.g., SARMs or SPRMs). In the following paragraphs non-steroidal ligands which have full or partial agonistic activity will be described for the following receptors: PR, GR, AR, LXR and FXR.
Buijsman
Rogier C
RC
N.V. Organon, Medicinal Chemistry Department, P.O. Box 20, 5340 BH, Oss, The Netherlands.
Hermkens
Pedro H H
PH
van Rijn
Rachel D
RD
Stock
H Thijs
HT
Teerhuis
N Miranda
NM
D059002:Androgen Receptor Antagonists; D000728:Androgens; D004268:DNA-Binding Proteins / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology; D006801:Humans; D008024:Ligands; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D011401:Promoter Regions, Genetic; D011944:Receptors, Androgen / Q000502:physiology; D018160:Receptors, Cytoplasmic and Nuclear / Q000502:physiology*; D011960:Receptors, Estrogen / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology; D011965:Receptors, Glucocorticoid / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology; D011980:Receptors, Progesterone / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology; D020845:Selective Estrogen Receptor Modulators / Q000494:pharmacology*; D014157:Transcription Factors / Q000819:agonists / Q000037:antagonists & inhibitors / Q000502:physiology*; D000099150:Receptor, Farnesoid X-Activated
D059002:Androgen Receptor Antagonists; D000728:Androgens; D004268:DNA-Binding Proteins; D008024:Ligands; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D011944:Receptors, Androgen; D018160:Receptors, Cytoplasmic and Nuclear; D011960:Receptors, Estrogen; D011965:Receptors, Glucocorticoid; D011980:Receptors, Progesterone; D020845:Selective Estrogen Receptor Modulators; D014157:Transcription Factors; D000099150:Receptor, Farnesoid X-Activated