Zobrazeno 1 - 10 of 12 pro vyhledávání: '"Mihiret T. Sisay"'
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New Cathepsin Inhibitors to Explore the Fluorophilic Properties of the S 2 Pocket of Cathepsin B: Design, Synthesis, and Biological Evaluation
Autor: Joaquín Timoneda, Michael Gütschow, F. Javier Cañada, Luis P. Calle, Vanessa Rodrigo, Jesús Jiménez-Barbero, Carlos del Pozo, María Sánchez-Roselló, Santos Fustero, Mihiret T. Sisay, Jürgen Bajorath, Maxim Frizler
Publikováno v: Digital.CSIC. Repositorio Institucional del CSIC
instname
CHEMISTRY-A EUROPEAN JOURNAL
r-CIPF: Repositorio Institucional Producción Científica del Centro de Investigación Principe Felipe (CIPF)
Centro de Investigación Principe Felipe (CIPF)
r-CIPF. Repositorio Institucional Producción Científica del Centro de Investigación Principe Felipe (CIPF)
5 páginas, 1 figura, 2 tablas -- PAGS nros. 5256-5260
Fluor-in or out? Based on β,β-difluorinated cycloaliphatic amino acids, a library of new dipeptide nitriles was evaluated as human cathepsin inhibitors. The orientation of the fluorinated
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::451389dc7c7bbe351438a6cfc7efe598
https://doi.org/10.1002/chem.201100113
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3
Identification of the First Low-Molecular-Weight Inhibitors of Matriptase-2
Autor: Jürgen Bajorath, Michael Gütschow, Torsten Steinmetzer, Mihiret T. Sisay, Eva Maurer, Marit Stirnberg, Maya Hammami
Publikováno v: Journal of Medicinal Chemistry. 53:5523-5535
As recently discovered, matriptase-2, a type II transmembrane serine protease, plays a crucial role in body iron homeostasis by down-regulating hepcidin expression, which results in increased iron levels. Thus, matriptase-2 represents a novel target
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::862f089a3da38a2b3d0d869abf30645f
https://doi.org/10.1021/jm100183e
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4
Structural Interpretation of Activity Cliffs Revealed by Systematic Analysis of Structure−Activity Relationships in Analog Series
Autor: Jürgen Bajorath, Mihiret T. Sisay, Lisa Peltason
Publikováno v: Journal of Chemical Information and Modeling. 49:2179-2189
Discontinuity in structure-activity relationships (SARs) is caused by so-called activity cliffs and represents one of the major caveats in SAR modeling and lead optimization. At activity cliffs, small structural modifications of compounds lead to sub
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b20d0d6d5c1e7e1f074db8cb49bd54f
https://doi.org/10.1021/ci900243a
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6
Allosteric modulation of caspases
Autor: Mihiret T. Sisay, Hans-Georg Häcker, Michael Gütschow
Publikováno v: Pharmacologytherapeutics. 132(2)
Caspases are proteolytic enzymes mainly involved in the induction and execution phases of apoptosis. This type of programmed cell death is an essential regulatory process required to maintain the integrity and homeostasis of multicellular organisms.
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22a14aab2811558acedff03d1d4c24c8
https://pubmed.ncbi.nlm.nih.gov/21807025
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8
Development of nitrile-based peptidic inhibitors of cysteine cathepsins
Autor: Marit Stirnberg, Mihiret T. Sisay, Michael Gütschow, Maxim Frizler
Publikováno v: Current topics in medicinal chemistry. 10(3)
It is now becoming clear that several papain-like cysteine cathepsins are involved in the pathophysiology of diseases such as osteoporosis, autoimmune disorders, and cancer. Therefore, the development of potent and selective cathepsin inhibitors is a
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::57452dc3de847419a7660258fc7404c8
https://pubmed.ncbi.nlm.nih.gov/20166952
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