Discovery of novel intracellular receptor modulating drugs.
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.
Jones
T K
TK
Ligand Pharmaceuticals, Inc., San Diego, CA 92121, USA.
Pathirana
C
C
Goldman
M E
ME
Hamann
L G
LG
Farmer
L J
LJ
Ianiro
T
T
Johnson
M G
MG
Bender
S L
SL
Mais
D E
DE
Stein
R B
RB
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
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