title: Orally available and efficacious α4β1/α4β7 integrin inhibitors.
abstract: A series of potent α4β1/α4β7 integrin inhibitors is reported, including an inhibitor 12d with remarkable oral exposure and efficacy in rat models of rheumatoid arthritis and Crohn's disease.
authors.affiliation: Elan Pharmaceuticals, 180 Oyster Point Blvd., South San Francisco, CA 94080, United States.
authors.forename: Ying-zi
authors.initials: YZ
authors.lastname: Xu
authors.forename: Jenifer L
authors.initials: JL
authors.lastname: Smith
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Semko
authors.forename: Kassandra I
authors.initials: KI
authors.lastname: Rossiter
authors.forename: Juri Y
authors.initials: JY
authors.lastname: Fukuda
authors.forename: Michael S
authors.initials: MS
authors.lastname: Dappen
authors.forename: David A
authors.initials: DA
authors.lastname: Quincy
authors.forename: Andrei W
authors.initials: AW
authors.lastname: Konradi
authors.forename: Wenxian
authors.initials: W
authors.lastname: Mao
authors.forename: Brent
authors.initials: B
authors.lastname: Welch
authors.forename: Mark L
authors.initials: ML
authors.lastname: Dreyer
authors.forename: Bhushan
authors.initials: B
authors.lastname: Samant
authors.forename: Hongbin
authors.initials: H
authors.lastname: Zhang
authors.forename: Judevin
authors.initials: J
authors.lastname: Lugar
authors.forename: Zhenmei
authors.initials: Z
authors.lastname: Liao
authors.forename: Carrol
authors.initials: C
authors.lastname: Henschel
authors.forename: Eric
authors.initials: E
authors.lastname: Petersen
authors.forename: Christopher
authors.initials: C
authors.lastname: Vandevert
authors.forename: Mark
authors.initials: M
authors.lastname: Shoemaker
authors.forename: Nancy
authors.initials: N
authors.lastname: Wehner
authors.forename: Linda
authors.initials: L
authors.lastname: Mutter
authors.forename: George
authors.initials: G
authors.lastname: Shopp
authors.forename: Michael
authors.initials: M
authors.lastname: Krimm
authors.forename: Linda
authors.initials: L
authors.lastname: Chen
authors.forename: Brian
authors.initials: B
authors.lastname: Wipke
authors.forename: Lilibeth
authors.initials: L
authors.lastname: Dofiles
authors.forename: Ian
authors.initials: I
authors.lastname: Gallager
authors.forename: John-Michael
authors.initials: JM
authors.lastname: Sauer
authors.forename: Elizabeth K
authors.initials: EK
authors.lastname: Messersmith
authors.forename: Michael A
authors.initials: MA
authors.lastname: Pleiss
authors.forename: Frederique
authors.initials: F
authors.lastname: Bard
authors.forename: Ted A
authors.initials: TA
authors.lastname: Yednock
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001172:Arthritis, Rheumatoid / Q000139:chemically induced / Q000188:drug therapy; D003424:Crohn Disease / Q000188:drug therapy; D004195:Disease Models, Animal; D006207:Half-Life; D006801:Humans; D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D016023:Integrins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D019169:Jurkat Cells; D008862:Microsomes, Liver / Q000378:metabolism; D051381:Rats
chemical_list: D039041:Integrin alpha4beta1; D016023:Integrins; C071777:integrin alpha4beta7