K
Karl Welzenbach
Researcher at Novartis
Publications - 29
Citations - 2241
Karl Welzenbach is an academic researcher from Novartis. The author has contributed to research in topics: Allosteric regulation & Kinase. The author has an hindex of 16, co-authored 29 publications receiving 2136 citations.
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Journal ArticleDOI
Statins selectively inhibit leukocyte function antigen-1 by binding to a novel regulatory integrin site.
Gabriele Weitz-Schmidt,Karl Welzenbach,Volker Brinkmann,Tetsji Kamata,Joerg Kallen,Christian Bruns,Sylvain Cottens,Yoshikazu Takada,Ulrich Hommel +8 more
TL;DR: Targeting of the statin-binding site of LFA-1 could be used to treat diseases such as psoriasis, rheumatoid arthritis, ischemia/reperfusion injury and transplant rejection.
Journal ArticleDOI
Structural basis for LFA-1 inhibition upon lovastatin binding to the CD11a I-domain.
Jörg Kallen,Karl Welzenbach,Paul Ramage,Dieter Geyl,Richard W. Kriwacki,Glen B. Legge,Sylvain Cottens,Gabriele Weitz-Schmidt,Ulrich Hommel +8 more
TL;DR: L lovastatin, a drug clinically used for lowering cholesterol levels, inhibits the interaction of human LFA-1 with its counter-receptor intercellular adhesion molecule-1, and the first three-dimensional structure of an integrin inhibitor bound to its receptor is revealed.
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Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.
Rainer Albert,Klaus Hinterding,Volker Brinkmann,Danilo Guerini,Constanze Müller-Hartwieg,Helmut Knecht,Corinne Simeon,Markus Streiff,Trixie Wagner,Karl Welzenbach,Frédéric Zecri,Markus Zollinger,Nigel Graham Cooke,Eric Francotte +13 more
TL;DR: In vivo phosphorylation of FTY720 in rats and humans resulted exclusively in the biologically active (S)-configured enantiomer, which was proven by an ex vivo o-phthaldialdehyde derivatization protocol especially elaborated for phosphates of 1.
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The potent protein kinase C selective inhibitor AEB071 (Sotrastaurin)represents a new class of immunosuppressive agents affecting early T cell activation
Jean-Pierre Evenou,Jürgen Wagner,Gerhard Zenke,Volker Brinkmann,Kathrin Wagner,Jiri Kovarik,Karl Welzenbach,Gabriele Weitz-Schmidt,Christine Guntermann,Harry Towbin,Sylvain Cottens,Sandra Kaminski,Thomas Letschka,Christina Lutz-Nicoladoni,Thomas Gruber,Natascha Hermann-Kleiter,Nikolaus Thuille,Gottfried Baier +17 more
TL;DR: In primary human and mouse T cells, AEB071 treatment effectively abrogated at low nanomolar concentration markers of early T-cell activation, such as interleukin-2 secretion and CD25 expression.
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Small molecule inhibitors induce conformational changes in the I domain and the I-like domain of lymphocyte function-associated antigen-1. Molecular insights into integrin inhibition.
TL;DR: For the first time, strong evidence is provided that the I-like domain represents a target for allosteric LFA-1 inhibition similar to the well established regulatory L-site on the I domain of L FA-1.