title: Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.
abstract: Continuing studies on tetrahydroquinoline glucocorticoid receptor anti-inflammatory agents lead to the identification of several tetrahydroquinolin-3-yl carbamates that exhibited steroid-like activity in in vitro transrepression assays with reduced transactivation of phosphoenol pyruvate carboxykinase (PEPCK), a key enzyme in the gluconeogenesis pathway.
authors.affiliation: Discovery Research, Ligand Pharmaceuticals, La Jolla, CA 92037, USA. sroach@ligand.com
authors.forename: Steven L
authors.initials: SL
authors.lastname: Roach
authors.forename: Robert I
authors.initials: RI
authors.lastname: Higuchi
authors.forename: Andrew R
authors.initials: AR
authors.lastname: Hudson
authors.forename: Angie
authors.initials: A
authors.lastname: Vassar
authors.forename: Virginia H S
authors.initials: VH
authors.lastname: Grant
authors.forename: Ryan
authors.initials: R
authors.lastname: Lamer
authors.forename: Charlene
authors.initials: C
authors.lastname: Hooper
authors.forename: Deepa
authors.initials: D
authors.lastname: Rungta
authors.forename: Peter M
authors.initials: PM
authors.lastname: Syka
authors.forename: Dale E
authors.initials: DE
authors.lastname: Mais
authors.forename: Keith B
authors.initials: KB
authors.lastname: Marschke
authors.forename: Lin
authors.initials: L
authors.lastname: Zhi
mesh_terms: D002262:Carboxy-Lyases / Q000378:metabolism*; D004789:Enzyme Activation; D011804:Quinolines / Q000494:pharmacology*; D011965:Receptors, Glucocorticoid / Q000819:agonists*
chemical_list: D011804:Quinolines; D011965:Receptors, Glucocorticoid; C542964:1,2,3,4-tetrahydroquinoline; D002262:Carboxy-Lyases