Výsledky vyhledávání - "Elisabeth Defossa"

Akademický článek

Molecular basis for inhibiting human glucose transporters by exofacial inhibitors

Autor: Nan Wang, Shuo Zhang, Yafei Yuan, Hanwen Xu, Elisabeth Defossa, Hans Matter, Melissa Besenius, Volker Derdau, Matthias Dreyer, Nis Halland, Kaihui Hu He, Stefan Petry, Michael Podeschwa, Norbert Tennagels, Xin Jiang, Nieng Yan

Publikováno v: Nature Communications, Vol 13, Iss 1, Pp 1-10 (2022)

Human glucose transporters (GLUTs), particularly GLUT1 and GLUT3, are potential anticancer therapy targets. Here, Nan Wang et al. use an engineered GLUT 3 variant to identify an exofacial GLUT3 inhibitor, SA47, and elucidate the drug’s inhibitory m

Externí odkaz: https://doaj.org/article/838595b279b94ca5b2244bbb0e9ea054

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Molecular basis for inhibiting human glucose transporters by exofacial inhibitors

Publikováno v: Nature communications. 13(1)

Human glucose transporters (GLUTs) are responsible for cellular uptake of hexoses. Elevated expression of GLUTs, particularly GLUT1 and GLUT3, is required to fuel the hyperproliferation of cancer cells, making GLUT inhibitors potential anticancer the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13cf0f8ec33788632d037a0b888d3098
https://pubmed.ncbi.nlm.nih.gov/35552392

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Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R)

Autor: Elisabeth Defossa, Matthias Löhn, Matthias Schäfer, Pavel Safar, Dietmar Weitz, Kristin Breitschopf, Matthias Lohmann, María Méndez, David S Thorpe, Jens Riedel, Nils Rackelmann, Hartmut Mors, Hans Matter, Michael Kurz, Ziyu Li, Michael Podeschwa, Sylvain Lebreton

Publikováno v: Journal of Medicinal Chemistry. 63:2292-2307

The therapeutic success of peptidic GLP-1 receptor agonists for treatment of type 2 diabetes mellitus (T2DM) motivated our search for orally bioavailable small molecules that can activate the GLP-1 receptor (GLP-1R) as a well-validated target for T2D

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9dde87dac749897ba8532f58a4dc0ec6
https://doi.org/10.1021/acs.jmedchem.9b01071

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Mechanistic investigations of the liver toxicity of the free fatty acid receptor 1 agonist fasiglifam (TAK875) and its primary metabolites

Autor: Jens Atzrodt, Friedemann Schmidt, Kerstin Wäse, Jacquelyn Dwyer, Wolfgang Holla, Martina Dorau, Alexander Amberg, Volker Derdau, József Pánczél, Angela Dudda, Ulrich Kürzel, Dietmar Weitz, Elisabeth Defossa, Catherine Arabeyre, Markus Kohlmann, Timothy Ackerson, Jens Riedel, Thomas Kissner, Shibani Rajanna

Publikováno v: Journal of Biochemical and Molecular Toxicology. 33

For fasiglifam (TAK875) and its metabolites the substance-specific mechanisms of liver toxicity were studied. Metabolism studies were run to identify a putatively reactive acyl glucuronide metabolite. In vitro cytotoxicity and caspase 3/7 activation

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56f2228bb7b27785702d8052feb6867b
https://doi.org/10.1002/jbt.22345

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Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus

Autor: Michael Wagner, Elisabeth Defossa

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:2991-3000

Despite the availability of established medication for treatment of type 2 diabetes mellitus (T2DM) there still remains a significant unmet need for new effective, oral antidiabetic agents that improve glycemic control while maintaining an excellent

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afa6eb80ac06d7192412d091fb909dee
https://doi.org/10.1016/j.bmcl.2014.05.019

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Design and Quantitative Structure−Activity Relationship of 3-Amidinobenzyl-1H-indole-2-carboxamides as Potent, Nonchiral, and Selective Inhibitors of Blood Coagulation Factor Xa

Autor: Armin Walser, Silke Herok, Uwe Heinelt, Peter-Michael Blohm, Hans Matter, Detlev Schneider, Volker Brachvogel, Petra Lönze, Alexander Liesum, Elisabeth Defossa, Andrea Müller, Herman Schreuder, Peter Wildgoose, Fahad Al-Obeidi

Publikováno v: Journal of Medicinal Chemistry. 45:2749-2769

A series of 138 nonchiral 3-amidinobenzyl-1H-indole-2-carboxamides and analogues as inhibitors of the blood coagulation enzyme factor Xa (fXa) were designed, synthesized, and investigated by X-ray structure analysis and 3D quantitative structure-acti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a726565af642ccfaba27630b1476d74a
https://doi.org/10.1021/jm0111346

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Synthesis of HR 916 K: An Efficient Route to the Pure Diastereomers of the 1-(Pivaloyloxy)ethyl Esters of Cephalosporins

Autor: Norbert Krass, Dieter Isert, Rolf Horlein, Fischer Gerd, Theo Wollmann, Uwe Gerlach, Ulrich Stache, Elisabeth Defoßa, Rudolf Lattrell

Publikováno v: Liebigs Annalen. 1996:1743-1749

HR 916 K (5), the 1-(S)-(pivaloyloxy)ethyl prodrug ester of the cephalosporin cefdaloxime, exhibits a significantly higher oral bioavailability than the 1-(R) diastereomer HR 916 J. An efficient synthesis of HR 916 K was developed. The separation of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7ced9b6c375c1c441b4b7c9c015448a6
https://doi.org/10.1002/jlac.199619961107

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Acyl ureas as human liver glycogen phosphorylase inhibitors for the treatment of type 2 diabetes

Autor: Karl Dr. Schönafinger, Magda Kosmopoulou, Hans-Jörg Burger, Dieter Schmoll, Erich Von Roedern, Andreas W. Herling, K. Ulrich Wendt, Elisabeth Defossa, Edoardo Sarubbi, Nikos G. Oikonomakos, Volker Brachvogel, Dieter Kadereit, Thomas Klabunde

Publikováno v: Journal of Medicinal Chemistry 48:20(Oct2005):6178-6193

Using a focused screening approach, acyl ureas have been discovered as a new class of inhibitors of human liver glycogen phosphorylase (hlGPa). The X-ray structure of screening hit 1 (IC50 = 2 microM) in a complex with rabbit muscle glycogen phosphor

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76e59b8d272785d03edb8ac1015f3c9c
http://helios-eie.ekt.gr/EIE/handle/10442/7970

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Crystallographic studies on acyl ureas, a new class of glycogen phosphorylase inhibitors, as potential antidiabetic drugs

Autor: Ioannis D. Kostas, Thomas Klabunde, Evangelia D. Chrysina, K. Ulrich Wendt, Magda Kosmopoulou, Nikos G. Oikonomakos, Demetres D. Leonidas, Elisabeth Defossa

Publikováno v: Protein Science 14:7(Jul2005):1760-1771

Acyl ureas were discovered as a novel class of inhibitors for glycogen phosphorylase, a molecular target to control hyperglycemia in type 2 diabetics. This series is exemplified by 6-{2,6-Dichloro- 4-[3-(2-chloro-benzoyl)-ureido]-phenoxy}-hexanoic ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6348014fe906247d50c028398c86fd4
https://europepmc.org/articles/PMC2253349/

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