Výsledky vyhledávání - "Markus Boehringer"

Akademický článek

Disease Modeling and Phenotypic Drug Screening for Diabetic Cardiomyopathy using Human Induced Pluripotent Stem Cells

Publikováno v: Cell Reports, Vol 9, Iss 3, Pp 810-820 (2014)

Diabetic cardiomyopathy is a complication of type 2 diabetes, with known contributions of lifestyle and genetics. We develop environmentally and genetically driven in vitro models of the condition using human-induced-pluripotent-stem-cell-derived car

Externí odkaz: https://doaj.org/article/5c9b6de352664d9d8293bead68a1b522

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Disease Modeling and Phenotypic Drug Screening for Diabetic Cardiomyopathy using Human Induced Pluripotent Stem Cells

Publikováno v: Cell Reports, Vol 9, Iss 3, Pp 810-820 (2014)

SummaryDiabetic cardiomyopathy is a complication of type 2 diabetes, with known contributions of lifestyle and genetics. We develop environmentally and genetically driven in vitro models of the condition using human-induced-pluripotent-stem-cell-deri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a26b637572ad429b507d1eb74ef6b11b

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Selective Elimination of Human Pluripotent Stem Cells by an Oleate Synthesis Inhibitor Discovered in a High-Throughput Screen

Autor: Ofra Yanuka, Markus Boehringer, Alicia Leikin-Frenkel, Uri Ben-David, Martin Graf, Yifat S. Oren, Payal Arora, Ralph Garippa, Qing-Fen Gan, Tamar Golan-Lev, Gianni Gromo, Nissim Benvenisty

Publikováno v: Cell Stem Cell. 12(2):167-179

SummaryThe use of human pluripotent stem cells (hPSCs) in cell therapy is hindered by the tumorigenic risk from residual undifferentiated cells. Here we performed a high-throughput screen of over 52,000 small molecules and identified 15 pluripotent c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::686394d68fd2ff6a1e658db77f1924eb

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Discovery of carmegliptin: A potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Autor: Patrizio Mattei, Joerg Huwyler, Patrick Di Giorgio, Buelent Kocer, Robert Narquizian, Etienne Rauber, Bernd Michael Loeffler, Alexander Macdonald, Michael Hennig, Elena Sebokova, Markus Boehringer, Holger Fischer, Bernd Kuhn, Urs Sprecher

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:1109-1113

Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin (8p), was chosen for clinical developme

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbb33eea5f814185d0336f4ee525ec31
https://doi.org/10.1016/j.bmcl.2009.12.024

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Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes

Autor: Agnès Bénardeau, Daniel Schlatter, Peter Mohr, Markus Boehringer, Denise Blum, Kurt Püntener, Uwe Grether, Hans Peter Märki, Bernd Kuhn, Susanne Raab, Armin Ruf, Hans Hilpert, Jörg Benz, Alfred Binggeli, Markus Meyer

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:2468-2473

Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPARalphagamma coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98a2820d83808e1a2305a6c942bdc5fb
https://doi.org/10.1016/j.bmcl.2009.03.036

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Elimination of undifferentiated cancer cells by pluripotent stem cell inhibitors

Autor: Uri Ben-David, Markus Boehringer, Eran Meshorer, Nissim Benvenisty, Christel Herold-Mende, Paola Scaffidi, Alva Biran

Publikováno v: Journal of molecular cell biology. 6(3)

Dear Editor, According to the cancer stem cell (CSC) hypothesis, cancer cells are organized in a hierarchical manner (Reya et al., 2001). Indeed, the differentiation state of cancer cells has been linked to their proliferative potential, drug respons

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::053e87546cda4b94350e5c615dd103e0
https://pubmed.ncbi.nlm.nih.gov/24683201

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The Tetrahymena Ribozyme Cleaves a 5‘-Methylene Phosphonate Monoester ∼102-fold Faster Than a Normal Phosphate Diester: Implications for Enzyme Catalysis of Phosphoryl Transfer Reactions

Autor: Marvin H. Caruthers, Jessica F. Curley, Michael Hsu, Joseph A. Piccirilli, Markus Boehringer, Xiangmin Liao, P. S. R. Anjaneyulu

Publikováno v: Biochemistry. 40:10911-10926

Single-atom substrate modifications have revealed an intricate network of transition state interactions in the Tetrahymena ribozyme reaction. So far, these studies have targeted virtually every oxygen atom near the reaction center, except one, the 5'

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::896e757fe4b519728d8f1736ef470151
https://doi.org/10.1021/bi010801u

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Aminomethylpyridines as DPP-IV inhibitors

Autor: Matthias Steger, Daniel Zimmerli, Silja Weber, Bernd-Michael Loeffler, Stéphane Kritter, Markus Boehringer, Jens-Uwe Peters, Peter Weiss, Angelina Wallier

Publikováno v: Bioorganicmedicinal chemistry letters. 14(13)

In a novel series of DPP-IV inhibitors, a large increase of inhibitory activity was achieved by optimisation of aromatic substituents and conformational restriction.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd74ed35478e0931212ec915c54f97f4
https://pubmed.ncbi.nlm.nih.gov/15177478

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An aminomethylpyrimidine DPP-IV inhibitor with improved properties

Autor: Bernd-Michael Loeffler, Aranka Müller, Jens-Uwe Peters, Miklos Csato, Markus Boehringer, Fabienne Ricklin, Daniel Hunziker, Holger Fischer, Silja Weber, Manfred Kansy, Angelina Wallier, Sonia Poli, Stéphane Kritter

Publikováno v: Bioorganicmedicinal chemistry letters. 14(13)

A recently identified DPP-IV inhibitor (1) was found to induce phospholipidosis and to inhibit CYP3A4. A small series of less lipophilic and less amphiphilic analogues was synthesized in an effort to overcome these issues. One compound from this seri

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3180fe93b65a1e511ad5e02a2eca20b6
https://pubmed.ncbi.nlm.nih.gov/15177477

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Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents

Autor: Jens-Uwe Peters, Bernd-Michael Loeffler, Bernd Kuhn, Stéphane Kritter, Peter Weiss, Silja Weber, Michael Hennig, Angelina Wallier, Markus Boehringer

Publikováno v: Bioorganicmedicinal chemistry letters. 14(6)

The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry program.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c69ca3f9804c7cbc6e6fab8873dea49
https://pubmed.ncbi.nlm.nih.gov/15006388

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