Zobrazeno 1 - 10
of 52
pro vyhledávání: '"Olaf Kinzel"'
Autor:
Xiaohua Xue, Aimee De Leon-Tabaldo, Rosa Luna-Roman, Glenda Castro, Michael Albers, Freddy Schoetens, Samuel DePrimo, Damayanthi Devineni, Thomas Wilde, Steve Goldberg, Olaf Kinzel, Thomas Hoffmann, Anne M. Fourie, Robin L. Thurmond
Publikováno v:
Scientific Reports, Vol 12, Iss 1, Pp 1-2 (2022)
Externí odkaz:
https://doaj.org/article/8350d4860faf488fa4942f7353c6f062
Autor:
Ulrich Deuschle, Julia Schüler, Andreas Schulz, Thomas Schlüter, Olaf Kinzel, Ulrich Abel, Claus Kremoser
Publikováno v:
PLoS ONE, Vol 7, Iss 10, p e43044 (2012)
The farnesoid X receptor (FXR) is expressed predominantly in tissues exposed to high levels of bile acids and controls bile acid and lipid homeostasis. FXR(-/-) mice develop hepatocellular carcinoma (HCC) and show an increased prevalence for intestin
Externí odkaz:
https://doaj.org/article/a1a6e167c9be4d74b5fd477793a71f22
Autor:
Xiaohua Xue, Aimee De Leon-Tabaldo, Rosa Luna-Roman, Glenda Castro, Michael Albers, Freddy Schoetens, Samuel DePrimo, Damayanthi Devineni, Thomas Wilde, Steve Goldberg, Olaf Kinzel, Thomas Hoffmann, Anne M. Fourie, Robin L. Thurmond
Publikováno v:
Scientific Reports, Vol 11, Iss 1, Pp 1-14 (2021)
Scientific Reports
Scientific Reports
The nuclear receptor retinoid-related orphan receptor gamma t (RORγt) plays a critical role in driving Th17 cell differentiation and expansion, as well as IL-17 production in innate and adaptive immune cells. The IL-23/IL-17 axis is implicated in se
Autor:
Barbara Morschhaeuser, Thomas J. Hoffmann, Sheena Pinto, Martin Hornberger, Michael Albers, Christoph Steeneck, Simon Anderhub, Olaf Kinzel, Christina Sonnek, Marta Czekańska
Publikováno v:
Bioorganicmedicinal chemistry letters. 33
Since the advent of antibody checkpoint inhibitors as highly efficient drugs for cancer treatment, the development of immunomodulating small molecules in oncology has gained great attention. Drug candidates targeting IDO1, a key enzyme in tryptophan
Autor:
Floriane Braun, Olaf Kinzel, Simon Anderhub, Martin Hornberger, Gerald Kleymann, Barbara Morschhaeuser, Thomas J. Hoffmann, Sheena Pinto, Christoph Steeneck
Publikováno v:
ACS Med Chem Lett
[Image: see text] Following the impressive success of checkpoint inhibitors in the treatment of cancer, combinations of IDO1 inhibitors with PD-1/PD-L1 antibodies are in clinical development aiming to increase response rates. Using the hydroxyamidine
Autor:
Anne M. Fourie, Steven D. Goldberg, Maxwell D. Cummings, Christoph Steeneck, Thomas Hoffmann, Xiaohua Xue, Michael Albers, Christian Gege, John Spurlino, Kristi A. Leonard, Marina I. Nelen, Cindy Milligan, James P. Edwards, Gerald Kleymann, Olaf Kinzel, Thomas Schlüter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1446-1455
The nuclear receptor retinoic acid receptor-related orphan receptor gamma t (RORγt) is a transcription factor that drives Th17 cell differentiation and IL-17 production in both innate and adaptive immune cells. The IL-23/IL-17 pathway is implicated
Publikováno v:
Handbook of experimental pharmacology. 256
FXR agonists have demonstrated very promising clinical results in the treatment of liver disorders such as primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH). NASH, in particular, is one of
Autor:
Christoph Steeneck, Olaf Kinzel, Simon Anderhub, Aurélie Mallinger, Marta Czekańska, Sheena Pinto, Barbara Morschhaeuser, Christina Sonnek, Martin Hornberger, Thomas J. Hoffmann, Michael Albers, Yansong Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 33:127738
Through structural modification of an oxalamide derived chemotype, a novel class of highly potent, orally bioavailable IDO1-specific inhibitors was identified. Representative compound 18 inhibited human IDO1 with IC50 values of 3.9 nM and 52 nM in a
Autor:
Xiaohua Xue, Christian Gege, Christoph Steeneck, Andreas Schulz, Kristi A. Leonard, Gerald Kleymann, Michael Albers, Steven D. Goldberg, Olaf Kinzel, Thomas J. Hoffmann, Thomas Schlüter, Maxwell D. Cummings, James P. Edwards, Anne M. Fourie, Brian Scott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127174
Starting from previously identified thiazole-2-carboxamides exemplified by compound 1/6, two new series of RORγt inverse agonists with significantly improved aqueous solubility, ADME parameters and oral PK properties were discovered. These scaffolds
Autor:
Olaf Kinzel, Michael Albers, Brian Scott, John Spurlino, Gerald Kleymann, James P. Edwards, Thomas Schlüter, Dan Pippel, Xiaohua Xue, Christian Gege, Thomas J. Hoffmann, Kristi A. Leonard, Christoph Steeneck, Anne M. Fourie, Maxwell D. Cummings, Cynthia M. Milligan, Steven D. Goldberg, Kevin J. Coe
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127205
The nuclear receptor retinoic acid receptor-related orphan receptor gamma t (RORγt) is a transcription factor that drives Th17 cell differentiation and IL-17 production in both innate and adaptive immune cells. The IL-23/IL-17 pathway is implicated