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  1. AU="Koeberle, Andreas"
  2. AU="Giller, M"
  3. AU="Ludhova, L"
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  6. AU="Rodriguez-Galan, Maria C"
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  9. AU="von Meißner, Wolfgang C G"
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  11. AU="Newby, R. J."
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  14. AU="Belella, Carissa"
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  1. Book ; Thesis: Identification and characterization of microsomal Prostaglandin E 2 Synthase-1 inhibitors

    Koeberle, Andreas

    = Identifizierung und Charakterisierung von Hemmstoffen der mikrosomalen Prostaglandin-E 2-Synthase-1

    2009  

    Title variant Identifizierung und Charakterisierung von Hemmstoffen der mikrosomalen Prostaglandin-E 2-Synthase-1
    Author's details vorgelegt von Andreas Koeberle
    Language English
    Size XII, 186 S. : graph. Darst.
    Publishing country Germany
    Document type Book ; Thesis
    Thesis / German Habilitation thesis Tübingen, Univ., Diss., 2009
    HBZ-ID HT015936399
    Database Catalogue ZB MED Medicine, Health

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    Shelf markLoan statusLocation
    2010 D 1357 order for loan Magazin

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  2. Article ; Online: Regulation and targeting of SREBP-1 in hepatocellular carcinoma.

    Su, Fengting / Koeberle, Andreas

    Cancer metastasis reviews

    2023  

    Abstract: Hepatocellular carcinoma (HCC) is an increasing burden on global public health and is associated with enhanced lipogenesis, fatty acid uptake, and lipid metabolic reprogramming. De novo lipogenesis is under the control of the transcription factor sterol ... ...

    Abstract Hepatocellular carcinoma (HCC) is an increasing burden on global public health and is associated with enhanced lipogenesis, fatty acid uptake, and lipid metabolic reprogramming. De novo lipogenesis is under the control of the transcription factor sterol regulatory element-binding protein 1 (SREBP-1) and essentially contributes to HCC progression. Here, we summarize the current knowledge on the regulation of SREBP-1 isoforms in HCC based on cellular, animal, and clinical data. Specifically, we (i) address the overarching mechanisms for regulating SREBP-1 transcription, proteolytic processing, nuclear stability, and transactivation and (ii) critically discuss their impact on HCC, taking into account (iii) insights from pharmacological approaches. Emphasis is placed on cross-talk with the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (Akt)-mechanistic target of rapamycin (mTOR) axis, AMP-activated protein kinase (AMPK), protein kinase A (PKA), and other kinases that directly phosphorylate SREBP-1; transcription factors, such as liver X receptor (LXR), peroxisome proliferator-activated receptors (PPARs), proliferator-activated receptor γ co-activator 1 (PGC-1), signal transducers and activators of transcription (STATs), and Myc; epigenetic mechanisms; post-translational modifications of SREBP-1; and SREBP-1-regulatory metabolites such as oxysterols and polyunsaturated fatty acids. By carefully scrutinizing the role of SREBP-1 in HCC development, progression, metastasis, and therapy resistance, we shed light on the potential of SREBP-1-targeting strategies in HCC prevention and treatment.
    Language English
    Publishing date 2023-12-01
    Publishing country Netherlands
    Document type Journal Article ; Review
    ZDB-ID 604857-2
    ISSN 1573-7233 ; 0167-7659
    ISSN (online) 1573-7233
    ISSN 0167-7659
    DOI 10.1007/s10555-023-10156-5
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    Zs.A 1812: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
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  3. Article: Developmental stage-dependent regulation of spine formation by calcium-calmodulin-dependent protein kinase IIα and Rap1

    Kuriu, Toshihiko / Koeberle, Andreas / Schulz, Alexander / Morrison, Helen / Okabe, Shigeo

    Scientific reports, 7:13409

    2017  

    Abstract: The roles of calcium-calmodulin-dependent protein kinase II-alpha (CaMKIIα) in the expression of long-term synaptic plasticity in the adult brain have been extensively studied. However, how increased CaMKIIα activity controls the maturation of neuronal ... ...

    Institution Leibniz-Institut für Alternsforschung
    Abstract The roles of calcium-calmodulin-dependent protein kinase II-alpha (CaMKIIα) in the expression of long-term synaptic plasticity in the adult brain have been extensively studied. However, how increased CaMKIIα activity controls the maturation of neuronal circuits remains incompletely understood. Herein, we show that pyramidal neurons without CaMKIIα activity upregulate the rate of spine addition, resulting in elevated spine density. Genetic elimination of CaMKIIα activity specifically eliminated the observed maturation-dependent suppression of spine formation. Enhanced spine formation was associated with the stabilization of actin in the spine and could be reversed by increasing the activity of the small GTPase Rap1. CaMKIIα activity was critical in the phosphorylation of synaptic Ras GTPase-activating protein (synGAP), the dispersion of synGAP from postsynaptic sites, and the activation of postsynaptic Rap1. CaMKIIα is already known to be essential in learning and memory, but our findings suggest that CaMKIIα plays an important activity-dependent role in restricting spine density during postnatal development.
    Keywords Cellular neuroscience ; Molecular neuroscience
    Language English
    Document type Article
    Database Repository for Life Sciences

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  4. Article ; Online: Target identification and lead discovery by functional lipidomics.

    Koeberle, Andreas

    Future medicinal chemistry

    2016  Volume 8, Issue 18, Page(s) 2169–2171

    Language English
    Publishing date 2016-12
    Publishing country England
    Document type Journal Article
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2016-0182
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  5. Article ; Online: Ferroptosis-modulating small molecules for targeting drug-resistant cancer: Challenges and opportunities in manipulating redox signaling.

    Koeberle, Solveigh C / Kipp, Anna P / Stuppner, Hermann / Koeberle, Andreas

    Medicinal research reviews

    2023  Volume 43, Issue 3, Page(s) 614–682

    Abstract: Ferroptosis is an iron-dependent cell death program that is characterized by excessive lipid peroxidation. Triggering ferroptosis has been proposed as a promising strategy to fight cancer and overcome drug resistance in antitumor therapy. Understanding ... ...

    Abstract Ferroptosis is an iron-dependent cell death program that is characterized by excessive lipid peroxidation. Triggering ferroptosis has been proposed as a promising strategy to fight cancer and overcome drug resistance in antitumor therapy. Understanding the molecular interactions and structural features of ferroptosis-inducing compounds might therefore open the door to efficient pharmacological strategies against aggressive, metastatic, and therapy-resistant cancer. We here summarize the molecular mechanisms and structural requirements of ferroptosis-inducing small molecules that target central players in ferroptosis. Focus is placed on (i) glutathione peroxidase (GPX) 4, the only GPX isoenzyme that detoxifies complex membrane-bound lipid hydroperoxides, (ii) the cystine/glutamate antiporter system X
    MeSH term(s) Humans ; Ferroptosis ; Reactive Oxygen Species/metabolism ; Neoplasms/drug therapy ; Neoplasms/metabolism ; Oxidation-Reduction ; Iron/metabolism
    Chemical Substances Reactive Oxygen Species ; Iron (E1UOL152H7)
    Language English
    Publishing date 2023-01-19
    Publishing country United States
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 603210-2
    ISSN 1098-1128 ; 0198-6325
    ISSN (online) 1098-1128
    ISSN 0198-6325
    DOI 10.1002/med.21933
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    Zs.A 1764: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
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  6. Article ; Online: Formulating elafibranor and obeticholic acid with phospholipids decreases drug-induced association of SPARC to extracellular vesicles from LX-2 human hepatic stellate cells.

    Zivko, Cristina / Witt, Finja / Koeberle, Andreas / Fuhrmann, Gregor / Luciani, Paola

    European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

    2022  Volume 182, Page(s) 32–40

    Abstract: Chronic hepatic diseases often compromise liver function and are directly responsible for up to two million yearly deaths world-wide. There are yet no treatment options to solve this global medical need. Experimental drugs elafibranor (Ela) and ... ...

    Abstract Chronic hepatic diseases often compromise liver function and are directly responsible for up to two million yearly deaths world-wide. There are yet no treatment options to solve this global medical need. Experimental drugs elafibranor (Ela) and obeticholic acid (OA) appeared promising in numerous earlier studies, but they recently struggled to show significant benefits in patients. Little is known on the drugs' impact on hepatic stellate cells (HSCs), key players in liver fibrogenesis. We recently reported a beneficial effect of polyenylphosphatidylcholines (PPCs)-rich formulations in reverting fibrogenic features of HSCs, including differences in their extracellular vesicles (EVs). Here, we newly formulated Ela and OA in PPC liposomes and evaluated their performance on the LX-2 (human HSC) cell line through our rigorous methods of EV-analysis, now expanded to include lipidomics. We show that direct treatments with Ela and OA increase EV-associated secreted protein acidic and cysteine rich (SPARC), a matricellular protein overexpressed in fibrogenesis. However, our results suggest that this potentially damaging drugs' action to HSCs could be mitigated when delivering them with lipid-based formulations, most notably with a PPC-rich phospholipid inducing specific changes in the cellular and EV phospholipid composition. Thus, EV analysis substantially deepens evaluations of drug performances and delivery strategies.
    MeSH term(s) Humans ; Hepatic Stellate Cells ; Liver Cirrhosis/drug therapy ; Phospholipids/metabolism ; Extracellular Vesicles/metabolism ; Osteonectin/metabolism
    Chemical Substances 2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxo-1-propenyl)phenoxyl)-2-methylpropanoic acid ; Phospholipids ; obeticholic acid (0462Z4S4OZ) ; SPARC protein, human ; Osteonectin
    Language English
    Publishing date 2022-12-02
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1065368-5
    ISSN 1873-3441 ; 0939-6411
    ISSN (online) 1873-3441
    ISSN 0939-6411
    DOI 10.1016/j.ejpb.2022.11.025
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    Zs.B 1651: Show issues Location:
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  7. Book ; Online ; Thesis: Metabolic reprogramming and targeting ferroptosis in breast cancer

    Su, Fengting [Verfasser] / Koeberle, Andreas [Gutachter] / Lorkowski, Stefan [Gutachter] / Kühn, Hartmut [Gutachter]

    2023  

    Author's details Fengting Su ; Gutachter: Andreas Koeberle, Stefan Lorkowski, Hartmut Kühn
    Keywords Biowissenschaften, Biologie ; Life Science, Biology
    Subject code sg570
    Language English
    Publisher Friedrich-Schiller-Universität Jena
    Publishing place Jena
    Document type Book ; Online ; Thesis
    Database Digital theses on the web

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  8. Article: Phytochemical Characterization of Cannabis sativa L. Chemotype V Reveals Three New Dihydrophenanthrenoids That Favorably Reprogram Lipid Mediator Biosynthesis in Macrophages

    Salamone, Stefano / Waltl, Lorenz / Pompignan, Anna / Grassi, Gianpaolo / Chianese, Giuseppina / Koeberle, Andreas / Pollastro, Federica

    Plants. 2022 Aug. 16, v. 11, no. 16

    2022  

    Abstract: The growing general interest surrounding Cannabis sativa L. has led to a renewal in breeding and resulted in an impressive variability of chemotypical characteristics that required the division of cannabis into different recognized chemotypes. The ... ...

    Abstract The growing general interest surrounding Cannabis sativa L. has led to a renewal in breeding and resulted in an impressive variability of chemotypical characteristics that required the division of cannabis into different recognized chemotypes. The chemotype V has been overlooked in terms of phytochemical composition due to the almost total absence of cannabinoids, on which biomedical attention is focused. Systematic approaches addressing diverse chemotypes are, however, needed to discriminate and define phytochemical aspects beyond cannabinoids. Such thoroughly characterized chemotypes guarantee blinding in controlled studies by mimicking the sensory properties of hemp and may help to unravel the “entourage effect”. Capitalizing on the ability of cannabis to synthesize a large number of non-cannabinoid phenolic compounds, we here investigated, for the first time, the composition of the Ermo chemotype V and identified new compounds: two dihydrophenanthrenes and the methoxy-dihydrodenbinobin. All three compounds suppress pro-inflammatory leukotriene biosynthesis in activated macrophage subtypes by targeting 5-lipoxygenase, but substantially differ in their capacity to elevate the levels of specialized pro-resolving lipid mediators and their precursors in M2 macrophages. We conclude that the discovered compounds likely contribute to the anti-inflammatory properties of Cannabis sativa L. chemotype V and might promote inflammation resolution by promoting a lipid mediator class switch.
    Keywords Cannabis sativa ; biosynthesis ; cannabinoids ; chemical constituents of plants ; chemotypes ; hemp ; inflammation ; lipids ; macrophages ; phytochemicals
    Language English
    Dates of publication 2022-0816
    Publishing place Multidisciplinary Digital Publishing Institute
    Document type Article
    ZDB-ID 2704341-1
    ISSN 2223-7747
    ISSN 2223-7747
    DOI 10.3390/plants11162130
    Database NAL-Catalogue (AGRICOLA)

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  9. Article ; Online: Natural products as inhibitors of prostaglandin E

    Koeberle, Andreas / Werz, Oliver

    Biotechnology advances

    2018  Volume 36, Issue 6, Page(s) 1709–1723

    Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit prostanoid formation and represent prevalent therapeutics for treatment of inflammatory disorders. However, NSAIDs are afflicted with severe side effects, which might be circumvented by more ... ...

    Abstract Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit prostanoid formation and represent prevalent therapeutics for treatment of inflammatory disorders. However, NSAIDs are afflicted with severe side effects, which might be circumvented by more selective suppression of pro-inflammatory eicosanoid biosynthesis. This concept led to dual inhibitors of microsomal prostaglandin E
    MeSH term(s) Animals ; Arachidonate 5-Lipoxygenase/metabolism ; Biological Products ; Humans ; Lipoxygenase Inhibitors ; Mice ; Prostaglandin-E Synthases/antagonists & inhibitors ; Prostaglandin-E Synthases/metabolism
    Chemical Substances Biological Products ; Lipoxygenase Inhibitors ; Arachidonate 5-Lipoxygenase (EC 1.13.11.34) ; Prostaglandin-E Synthases (EC 5.3.99.3)
    Language English
    Publishing date 2018-02-15
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 47165-3
    ISSN 1873-1899 ; 0734-9750
    ISSN (online) 1873-1899
    ISSN 0734-9750
    DOI 10.1016/j.biotechadv.2018.02.010
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    Zs.A 3730: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (2.OG)
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  10. Article: Natural products as inhibitors of prostaglandin E2 and pro-inflammatory 5-lipoxygenase-derived lipid mediator biosynthesis

    Koeberle, Andreas / Oliver Werz

    Biotechnology advances. 2018 Nov. 01, v. 36, no. 6

    2018  

    Abstract: Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit prostanoid formation and represent prevalent therapeutics for treatment of inflammatory disorders. However, NSAIDs are afflicted with severe side effects, which might be circumvented by more ... ...

    Abstract Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit prostanoid formation and represent prevalent therapeutics for treatment of inflammatory disorders. However, NSAIDs are afflicted with severe side effects, which might be circumvented by more selective suppression of pro-inflammatory eicosanoid biosynthesis. This concept led to dual inhibitors of microsomal prostaglandin E2 synthase (mPGES)-1 and 5-lipoxygenase that are crucial enzymes in the biosynthesis of pro-inflammatory prostaglandin E2 and leukotrienes. The potential of their dual inhibition in light of superior efficacy and safety is discussed. Focus is placed on natural products, for which direct inhibition of mPGES-1 and leukotriene biosynthesis has been confirmed.
    Keywords adverse effects ; biosynthesis ; leukotrienes ; nonsteroidal anti-inflammatory agents ; prostaglandin-E synthase ; prostaglandins ; therapeutics
    Language English
    Dates of publication 2018-1101
    Size p. 1709-1723.
    Publishing place Elsevier Inc.
    Document type Article
    ZDB-ID 47165-3
    ISSN 0734-9750
    ISSN 0734-9750
    DOI 10.1016/j.biotechadv.2018.02.010
    Database NAL-Catalogue (AGRICOLA)

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    In stock of ZB MED Cologne/Königswinter

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