Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Konrad F. Koehler"'
Autor:
Wei B. Emond, Rajiv Sawant, Matthis Geitmann, Johan Winquist, Peter Brandt, Ulf Bremberg, Per Källblad, Vendela Parrow, Claes Andersson, Kristin Blom, Nasrin Najafi, Tobias Bergström, Fredrik J. Swartling, Mats Hellström, Konrad F. Koehler
Publikováno v:
Cancer Research. 83:705-705
LSD1 has emerged as a potential therapeutic target to increase the effectiveness of cancer immunotherapy. We have developed a series of novel small molecules, exemplified by the lead substance BEA-17, that modulates LSD1 via binding to an allosteric
Autor:
Martin Hegen, David C. Wood, Patrik Rhönnstad, Felix Vajdos, Atli Thorarensen, Mark E. Schnute, Timothy Braden, Kimberly Crouse, Maria Sjöberg, John I. Trujillo, Ravi G. Kurumbail, Bolette Husman, Konrad F. Koehler, Mattias Wennerstål, Tomas Bonn, Joakim Löfstedt, Eva Backström-Rydin, Bo Carlsson, Aron Sundell, Ming Z. Chen, Steven E. Heasley, John David Trzupek, Annika Goos-Nilsson, Carol A. Menard, Peter Harris, James R. Kiefer, Martin Bengtsson, Leon P. Collis, Michael J. Prinsen, Philippe Nuhant, Jennifer Alley, Scott A. Long, Alexander E. Hromockyj, Andrew C. Flick, Johnny Sandberg, Christoph W. Zapf, Edouard Zamaratski, Xiao Hu, Lee Napierata, Björn Kauppi, Nicole Caspers, Kimberly F. Fennell, Robert E. Kyne, Gabriel Berstein, Neelu Kaila, Lars Kruger, Wei Li, Li Xing, Ray Unwalla, Elisabet Kallin, Matthew J. Pelc, Susan Fish, James Robert Blinn, Hjalmar Gullberg, Marvin J. Meyers, Scot Richard Mente, Chulho Choi, Falgun Shah, Mathias Färnegårdh, Dean Messing, Peter G. Jones, Yajuan Zhao, Alexandria P. Taylor, Maria Sandström, Charles W. Bolten, Daniel Nöteberg, Robin A. Weinberg, Tomasz Janosik, John D. Knafels, Anna Wilhelmsson
Publikováno v:
Journal of medicinal chemistry. 61(23)
The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production
Publikováno v:
Nature Reviews Drug Discovery. 10:778-792
The two oestrogen receptor subtypes α and β are hormone-regulated modulators of intracellular signalling and gene expression. Regulation of oestrogen receptor activity is crucial not only for development and homeostasis but also for the treatment o
Publikováno v:
Bulletin des Sociétés Chimiques Belges. 92:811-817
A new method for the preparation of β-lactams has been developed. The protocol involves 1,3-dipolar cycloaddition of nitrones with nitro substituted alkenes followed by a subsequent reorganization of the resulting 5-nitroisoxazolidine isomer. The ut
Publikováno v:
Molecular Endocrinology. 19:1960-1977
Two-point mutations in the human glucocorticoid receptor have been studied by computer simulations to rationalize experimental data, where mutants comprising the V571M substitution improve both transcriptional activity and affinity for aldosterone de
Autor:
Margaret Warner, Konrad F. Koehler, Lars Arne Haldosén, Luisa A. Helguero, Jan-Åke Gustafsson
Publikováno v:
Endocrine Reviews. 26:465-478
We have known for many years that estrogen is more than the female hormone. It is essential in the male gonads, and in both sexes, estrogen has functions in the skeleton and central nervous system, on behavior, and in the cardiovascular and immune sy
Autor:
Bo Carlsson, Lars-Göran Bladh, Marlena Grynfarb, Theresa Appelqvist, Konrad F. Koehler, Asa Hedfors, Chris Litten, Johan Malm, Peter Agback
Publikováno v:
Journal of Medicinal Chemistry. 48:3114-3117
Based on the recently described concept of "indirect antagonism" of nuclear receptors, a series of thyroid hormone receptor (TR) antagonists were prepared, in which the outer ring of a thyromimetic was replaced with alkyl chains of variable length an
Autor:
Konrad F. Koehler, Raffaele De Francesco, Uwe Koch, Victor G. Matassa, Mirko Brunetti, Frank Narjes, Sergio Altamura, Stefania Colarusso, Benjamin Gerlach, Christian Steinkühler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:701-704
The difluoromethyl group was designed by computational chemistry methods as a mimetic of the canonical P1 cysteine thiol for inhibitors of the hepatitis C virus NS3 protease. This modification led to the development of competitive, non-covalent inhib
Autor:
Mikael Gillner, Anthony P. H. Wright, Paulette Greenidge, Konrad F. Koehler, Jan Carlstedt-Duke, Ulrika Lind
Publikováno v:
Journal of Biological Chemistry. 275:19041-19049
To elucidate which amino acids in the glucocorticoid receptor ligand-binding domain might be involved in determining steroid binding specificity by interaction with the D-ring of glucocorticoids, we have performed site-directed mutagenesis of the fou