title: Discovery of novel intracellular receptor modulating drugs.
abstract: Utilizing the co-transfection assay as a guide to determining structure activity relationships, we have been pursuing the discovery of non-steroidal hPR modulators. Small molecule, non-steroidal lead structures have been identified. Optimization of these structures has yielded more potent hPR modulators. Improved cross-reactivity profiles with other intracellular receptors are a feature of these compounds owing to their non-steroidal nature.
authors.affiliation: Ligand Pharmaceuticals, Inc., San Diego, CA 92121, USA.
authors.forename: T K
authors.initials: TK
authors.lastname: Jones
authors.forename: C
authors.initials: C
authors.lastname: Pathirana
authors.forename: M E
authors.initials: ME
authors.lastname: Goldman
authors.forename: L G
authors.initials: LG
authors.lastname: Hamann
authors.forename: L J
authors.initials: LJ
authors.lastname: Farmer
authors.forename: T
authors.initials: T
authors.lastname: Ianiro
authors.forename: M G
authors.initials: MG
authors.lastname: Johnson
authors.forename: S L
authors.initials: SL
authors.lastname: Bender
authors.forename: D E
authors.initials: DE
authors.lastname: Mais
authors.forename: R B
authors.initials: RB
authors.lastname: Stein
mesh_terms: D000818:Animals; D000840:Anisoles / Q000737:chemistry / Q000493:pharmacokinetics; D002522:Chlorocebus aethiops; D000460:Chlorophyta / Q000737:chemistry; D003510:Cyclohexanes / Q000737:chemistry / Q000493:pharmacokinetics; D015195:Drug Design; D015914:Estrogen Replacement Therapy; D005260:Female; D006067:Gonanes / Q000737:chemistry / Q000493:pharmacokinetics; D006727:Hormone Antagonists / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D015735:Mifepristone / Q000737:chemistry / Q000493:pharmacokinetics; D015394:Molecular Structure; D045167:Progesterone Congeners / Q000009:adverse effects* / Q000493:pharmacokinetics; D018079:Receptors, GABA / Q000187:drug effects / Q000502:physiology; D011980:Receptors, Progesterone / Q000187:drug effects* / Q000378:metabolism; D011987:Receptors, Steroid / Q000187:drug effects / Q000378:metabolism; D011994:Recombinant Proteins / Q000187:drug effects; D012894:Sleep Stages / Q000187:drug effects; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: D000840:Anisoles; D003510:Cyclohexanes; D006067:Gonanes; D006727:Hormone Antagonists; C092755:LG 100127; D045167:Progesterone Congeners; D018079:Receptors, GABA; D011980:Receptors, Progesterone; D011987:Receptors, Steroid; D011994:Recombinant Proteins; D015735:Mifepristone; C053238:onapristone