Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Maxine Norman"'
Autor:
Gary Salmon, Harvey Wong, Maxine Norman, Adrian Barnard, Aihe Zhou, Julie Hawkins, Benjamin Fauber, Adam R. Johnson, Arunima Ganguli, Yuzhong Deng, Susan Summerhill, Kirk Robarge, Celine Eidenschenk, Wenjun Ouyang, Christine Everett, Jianhua Cao, Wei Tang, Hank La, Alberto Gobbi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2907-2912
The nuclear receptor (NR) retinoic acid receptor-related orphan receptor gamma (RORγ, RORc, or NR1F3) is a promising target for the treatment of autoimmune diseases. RORc is a critical regulator in the production of the pro-inflammatory cytokine int
Autor:
Adam R. Johnson, Justin Lesch, Christine Everett, Harvey Wong, Susan Summerhill, Peter Lockey, Arunima Ganguli, Julie Hawkins, Benjamin Fauber, Jason DeVoss, Olivier Rene, Maxine Norman, Hank La, Yuzhong Deng, Celine Eidenschenk, Wenjun Ouyang, Alberto Gobbi
Publikováno v:
Journal of Medicinal Chemistry. 58:5308-5322
Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse ag
Autor:
Sarah G. Hymowitz, Alberto Gobbi, Gladys de Leon Boenig, Adam R. Johnson, Benjamin Fauber, Marya Liimatta, Celine Eidenschenk, Olivier Rene, Wenjun Ouyang, Peter Lockey, James R. Kiefer, Christine Everett, Heidi J.A. Wallweber, Brenda Burton, Harvey Wong, Maxine Norman
Publikováno v:
ACS Medicinal Chemistry Letters. 6:276-281
A minor structural change to tertiary sulfonamide RORc ligands led to distinct mechanisms of action. Co-crystal structures of two compounds revealed mechanistically consistent protein conformational changes. Optimized phenylsulfonamides were identifi
Autor:
Maxine Norman, Julie Hawkins, Olivier Rene, Benjamin Fauber, Adam R. Johnson, Peter Lockey, Marya Liimatta, Brenda Burton, Alberto Gobbi, Christine Everett, Harvey Wong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2182-2187
Screening a nuclear receptor compound subset in a RORc biochemical binding assay revealed a benzylic tertiary sulfonamide hit. Herein, we describe the identification of compounds with improved RORc biochemical inverse agonist activity and cellular po
Autor:
Harvey Wong, Celine Eidenschenk, Peter Lockey, Sarah G. Hymowitz, Christine Everett, Olivier Rene, Wenjun Ouyang, Maxine Norman, Marya Liimatta, Adam R. Johnson, Alberto Gobbi, Benjamin Fauber, Gladys de Leon Boenig, Brenda Burton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6604-6609
The structure-activity relationships of T0901317 analogs were explored as RORc inverse agonists using the principles of property- and structure-based drug design. An X-ray co-crystal structure of T0901317 and RORc was obtained and provided molecular
Autor:
Brenda Burton, Peter Lockey, Maxine Norman, Gary Jones, Adam R. Johnson, Olivier Rene, Stephen Bowerman, Harvey Wong, Gareth Harrold, Annerley Flynn, Adam Colebrook, Benjamin Fauber, Steve Huhn
Publikováno v:
Journal of Labelled Compounds and Radiopharmaceuticals. 57:57-60
The synthesis and characterization of [3H2]T0901317 and a structural isomer are described. The structural assignments of the closely related labeled compounds were primarily accomplished via 19F NMR analyses of the corresponding ethanolic compound di
Autor:
Yuzhong Deng, Susan Summerhill, Benjamin Fauber, Maxine Norman, Alberto Gobbi, Adrian Barnard, Kerry Chapman, Adam R. Johnson, Olivier Rene, Harvey Wong, Christine Everett, Hank La, Gary Salmon, Celine Eidenschenk
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(18)
Modification of the δ-sultam ring of RORc inverse agonist 2 led to the discovery of more polar oxa-sultam 65. The less lipophilic inverse agonist (65) displayed high potency in a biochemical assay, which translated into inhibition of IL-17 productio
Autor:
Harvey Wong, Christine Everett, Alberto Gobbi, Yuzhong Deng, Hank La, Adam R. Johnson, Maxine Norman, Benjamin Fauber, Peter Lockey, Pascal Savy, Brenda Burton
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(19)
A high-throughput screen of the Genentech/Roche compound collection using a retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) biochemical assay revealed a N-sulfonyl-tetrahydroquinoline hit. Herein, we describe the hit-to-lead
Autor:
Harvey Wong, Arunima Ganguli, Peter Lockey, Monique Bodil Van Niel, James R. Kiefer, Jonathan C. Killen, Julie Hawkins, Hank La, Nicole Wakes, Adam R. Johnson, Alberto Gobbi, Ann Qin, Celine Eidenschenk, Bohdan Waszkowycz, Benjamin Fauber, Wenjun Ouyang, Stuart Ward, Gladys de Leon Boenig, Emanuela Gancia, Simon Gaines, Christine Everett, Matthew W. Cartwright, Olivier Rene, Yuzhong Deng, Maxine Norman
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(24)
The identification of a new series of RORc inverse agonists is described. Comprehensive structure-activity relationship studies of this reversed sulfonamide series identified potent RORc inverse agonists in biochemical and cellular assays which were
Autor:
Maxine Norman, Weiru Wang, Brenda Burton, Sarah G. Hymowitz, Olivier Rene, Adam R. Johnson, Yuzhong Deng, Celine Eidenschenk, Christine Everett, Marya Liimatta, Harvey Wong, Wenjun Ouyang, Peter Lockey, Hank La, Gladys de Leon Boenig, Benjamin Fauber, Alberto Gobbi
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(16)
Using structure-based drug design principles, we identified opportunities to reduce the lipophilicity of our tertiary sulfonamide RORc inverse agonists. The new analogs possessed improved RORc cellular potencies with >77-fold selectivity for RORc ove