Zobrazeno 1 - 10
of 42
pro vyhledávání: '"Eric A. Kitas"'
Autor:
Christophe Schweitzer, Christoph Patsch, Joerg Hoernschemeyer, Eric A. Kitas, Eike Hoffmann, Jens Niewoehner, Nadine Ruderisch, Karlheinz Baumann, Sylwia Huber, Per-Ola Freskgard, Hansruedi Loetscher, Jörg Benz, Achim Gärtner, Arne C. Rufer, Carlo Cusulin, Tina Bülau, Andreas Kuglstatter, Wolfgang Guba, Daniel Schlatter
Publikováno v:
EBioMedicine
EBioMedicine, Vol 24, Iss C, Pp 76-92 (2017)
EBioMedicine, Vol 24, Iss C, Pp 76-92 (2017)
Therapeutic approaches to fight Alzheimer's disease include anti-Amyloidβ (Aβ) antibodies and secretase inhibitors. However, the blood-brain barrier (BBB) limits the brain exposure of biologics and the chemical space for small molecules to be BBB p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84ad5bf832352c9060ecd331ea0b6c7b
https://doi.org/10.1016/j.ebiom.2017.09.004
https://doi.org/10.1016/j.ebiom.2017.09.004
Autor:
David B. Rozema, So C. Wong, Vladimir S. Trubetskoy, Almeida Lauren J, Jonathan D. Benson, Julia Hegge, Darren H. Wakefield, Holly Hamilton, Jeffrey C. Carlson, Jon A. Wolff, Eric A. Kitas, David L. Lewis, Qili Chu, Jason Klein, Anthony Nicholas, Collin M. Hagen, Andrei V. Blokhin
Publikováno v:
Journal of Controlled Release. 209:57-66
The safe and efficacious delivery of membrane impermeable therapeutics requires cytoplasmic access without the toxicity of nonspecific cytoplasmic membrane lysis. We have developed a mechanism for control of cytoplasmic release which utilizes endogen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::06bffbd8f8ab16c71a0a150c958e0822
Publikováno v:
Biochimica et Biophysica Acta (BBA) - Biomembranes. 1838(3):968-977
Melittin is an amphipathic peptide which has received much attention as a model peptide for peptide–membrane interactions. It is however not suited as a transfection agent due to its cytolytic and toxicological effects. Retro-inverso-melittin, when
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b01580cca83d5636a6444998ae6b3b8a
Autor:
Stephan Kirchner, Paul Hebeisen, Eric A. Kitas, Effie Tozzo, Bernd Kuhn, Marcel Gubler, Armin Ruf, Hans Peter Wessel, Ulrich Zutter, Wolfgang Haap, Catherine Joseph, Peter Mohr, Rubén Alvarez-Sánchez, Jörg Benz, Agnès Bénardeau, Brigitte Schott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3237-3242
A novel sulfonylureido pyridine series exemplified by compound 19 yielded potent inhibitors of FBPase showing significant glucose reduction and modest glycogen lowering in the acute db/db mouse model for Type-2 diabetes. Our inhibitors occupy the all
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4388584265f0ac68a801ab2793b185c3
https://doi.org/10.1016/j.bmcl.2011.04.044
https://doi.org/10.1016/j.bmcl.2011.04.044
Autor:
Axel Paehler, Hans Peter Wessel, Armin Ruf, Jörg Benz, Catherine Joseph, Marcel Gubler, Eric A. Kitas, Brigitte Schott, Bernd Kuhn, Peter Mohr, Effie Tozzo, Agnès Bénardeau, Paul Hebeisen, Walter Huber, Ruben Alvarez Sanchez, Wolfgang Haap
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:594-599
Sulfonylureido thiazoles were identified from a HTS campaign and optimized through a combination of structure-activity studies, X-ray crystallography and molecular modeling to yield potent inhibitors of fructose-1,6-bisphosphatase. Compound 12 showed
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba14e44d2fe82d84bf408ab6efc043d4
https://doi.org/10.1016/j.bmcl.2009.11.093
https://doi.org/10.1016/j.bmcl.2009.11.093
Autor:
Brigitte Schott, Bernd Kuhn, Eric A. Kitas, Paul Hebeisen, Kohler Philipp Christoph, Marcel Gubler, Armin Ruf, Jörg Benz, Walter Huber, Catherine Joseph
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4708-4712
Human fructose-1,6-bisphosphatase (FBPase, EC 3.1.3.11) is a key gluconeogenic enzyme, responsible for the hydrolysis of fructose-1,6-bisphosphate to fructose-6-phosphate, and thus presents an opportunity for the development of novel therapeutics foc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6975f1f1f7b7b2839502166d90ce4a1a
https://doi.org/10.1016/j.bmcl.2008.06.103
https://doi.org/10.1016/j.bmcl.2008.06.103
Autor:
Alexander Flohr, Pascale David-Pierson, Eric A. Kitas, Wolfgang Wostl, Harald Mauser, André Alker, Guido Galley, Dieter P. Reinhardt, Helmut Jacobsen, Laurence Ozmen, Roland Jakob-Roetne, Christian Czech
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:304-308
A hydroxamic acid screening hit 1 was elaborated to 5,5-dimethyl-2-oxoazepane derivatives exhibiting low nanomolar inhibition of γ-secretase, a key proteolytic enzyme involved in Alzheimer’s disease. Early ADME data showed a high metabolic clearan
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78b6f51a292ea3a0364da0ecb41fd68f
https://doi.org/10.1016/j.bmcl.2007.10.074
https://doi.org/10.1016/j.bmcl.2007.10.074
Autor:
Roland Schmucki, Hansruedi Loetscher, Helmut Jacobsen, Ulrich Certa, Martin Ebeling, Nadine Ruderisch, Eduard Urich, Eric A. Kitas, Christophe Schweitzer, Alessandra Bergadano, Per-Ola Freskgard
Publikováno v:
Scientific Reports
The blood-brain barrier and the blood-cerebrospinal fluid barrier prevent access of biotherapeutics to their targets in the central nervous system and therefore prohibit the effective treatment of neurological disorders. In an attempt to discover nov
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24a6a0f2ebf0ddc82b5e563c5c507a7f
https://doi.org/10.1038/srep14104
https://doi.org/10.1038/srep14104
Publikováno v:
Biochemistry. 45:3086-3094
Melittin is an amphipathic cationic peptide derived from honeybee venom with well-known cytolytic and antimicrobial properties. When coupled to cationic polymers or lipid molecules, it forms conjugates with high transfection efficiency and low toxici
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c1814c9fcf57478d044d9d3f7e85649
https://doi.org/10.1021/bi052221t
https://doi.org/10.1021/bi052221t
Autor:
Bernd-Michael Löffler, Johannes Aebi, Lucienne Juillerat-Jeanneret, Eric A. Kitas, Henrietta Dehmlow, Denise Blum-Kaelin, Yann Berger
Publikováno v:
Journal of Medicinal Chemistry. 48:483-498
Endothelin-1 (ET-1) is mitogenic and/or antiapoptotic in human cancers, and antagonists to ET-1 receptors are under evaluation for cancer treatment. Inhibition of ET-1 activation by the endothelin-converting enzymes 1(a)(-)(d) (ECE-1(a)(-)(d); EC 3.4
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c7bf69be97812c9ac781edfb3e969e4
https://doi.org/10.1021/jm040857x
https://doi.org/10.1021/jm040857x