Zobrazeno 1 - 10 of 18 pro vyhledávání: '"Emre F, Bülbül"'
1
Akademický článek
Application of Ligand- and Structure-Based Prediction Models for the Design of Alkylhydrazide-Based HDAC3 Inhibitors as Novel Anti-Cancer Compounds
Autor: Emre F. Bülbül, Dina Robaa, Ping Sun, Fereshteh Mahmoudi, Jelena Melesina, Matthes Zessin, Mike Schutkowski, Wolfgang Sippl
Publikováno v: Pharmaceuticals, Vol 16, Iss 7, p 968 (2023)
Histone deacetylases (HDAC) represent promising epigenetic targets for several diseases including different cancer types. The HDAC inhibitors approved to date are pan-HDAC inhibitors and most show a poor selectivity profile, side effects, and in part
Externí odkaz: https://doaj.org/article/e3586201481146dc87ec379763db81a5
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2
Akademický článek
Docking, Binding Free Energy Calculations and In Vitro Characterization of Pyrazine Linked 2-Aminobenzamides as Novel Class I Histone Deacetylase (HDAC) Inhibitors
Autor: Emre F. Bülbül, Jelena Melesina, Hany S. Ibrahim, Mohamed Abdelsalam, Anita Vecchio, Dina Robaa, Matthes Zessin, Mike Schutkowski, Wolfgang Sippl
Publikováno v: Molecules, Vol 27, Iss 8, p 2526 (2022)
Class I histone deacetylases, HDAC1, HDAC2, and HDAC3, represent potential targets for cancer treatment. However, the development of isoform-selective drugs for these enzymes remains challenging due to their high sequence and structural similarity. I
Externí odkaz: https://doaj.org/article/05b8cc97c3804454871db793df609555
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3
Development of Alkylated Hydrazides as Highly Potent and Selective Class I Histone Deacetylase Inhibitors with T cell Modulatory Properties
Autor: Ping Sun, Jing Wang, Khadija S. Khan, Weiqin Yang, Billy Wai-Lung Ng, Nikita Ilment, Matthes Zessin, Emre F. Bülbül, Dina Robaa, Frank Erdmann, Matthias Schmidt, Christophe Romier, Mike Schutkowski, Alfred Sze-Lok Cheng, Wolfgang Sippl
Publikováno v: Journal of Medicinal Chemistry. 65:16313-16337
Histone deacetylases (HDACs) are epigenetic regulators and additionally control the activity of non-histone substrates. We recently demonstrated that inhibition of HDAC8 overexpressed in various of cancers reduces hepatocellular carcinoma tumorigenic
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9c985e4087f311b0e6b58dd9531d9764
https://doi.org/10.1021/acs.jmedchem.2c01132
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4
Application of Ligand- and Structure-Based Prediction Models for the Design of Alkylhydrazide-Based HDAC3 Inhibitors as Novel Anti-Cancer Compounds
Autor: Sippl, Emre F. Bülbül, Dina Robaa, Ping Sun, Fereshteh Mahmoudi, Jelena Melesina, Matthes Zessin, Mike Schutkowski, Wolfgang
Publikováno v: Pharmaceuticals; Volume 16; Issue 7; Pages: 968
Histone deacetylases (HDAC) represent promising epigenetic targets for several diseases including different cancer types. The HDAC inhibitors approved to date are pan-HDAC inhibitors and most show a poor selectivity profile, side effects, and in part
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=multidiscipl::9d7a408ec19a6e162b3a431e6126ef2a
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5
Application of Ligand- and Structure-Based Prediction Models for the Design of Alkylhydrazide-Based HDAC3 Inhibitors as Novel Anti-cancer Compounds
Autor: Emre f Bülbül, Dina Robaa, Ping Sun, Fereshteh Mahmoudi, Jelena Melesina, Matthes Zessin, Mike Schutkowski, Wolfgang Sippl
Histone deacetylases (HDAC) represent promising epigenetic targets for several diseases including different cancer types. The HDAC inhibitors approved to date are pan-HDAC inhibitors and most show a poor selectivity profile, side effects and especial
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fc89f169b7eadafd5f9416658e3c2a2c
https://doi.org/10.20944/preprints202305.1124.v1
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7
New chromanone derivatives containing thiazoles: Synthesis and antitumor activity evaluation on A549 lung cancer cell line
Autor: Mehmet Onur Aksoy, Halide Edip Temel, Emre F. Bülbül, Leyla Yurttaş, Gülşen Akalın Çiftçi
Publikováno v: Drug Development Research. 83:470-484
Novel 2-[2-(chroman-4-ylidene)hydrazinyl]-4/5-substituted thiazole derivatives (2a-i) were synthesized and investigated for their anticancer activity. Cytotoxic activity on A549 and NIH/3T3 cell lines was determined, most of the compounds exhibited h
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc1e1ff7ca5c8570acbd8c6e33aea4c0
https://doi.org/10.1002/ddr.21879
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9
Strategies To Design Selective Histone Deacetylase Inhibitors
Autor: Wolfgang Sippl, Jelena Melesina, Dina Robaa, Emre F. Bülbül, Conrad V. Simoben, Lucas Praetorius
Publikováno v: ChemMedChem. 16:1336-1359
This review classifies drug-design strategies successfully implemented in the development of histone deacetylase (HDAC) inhibitors, which have many applications including cancer treatment. Our focus is on especially demanded selective HDAC inhibitors
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fda2d0eb83ac634aca9d9def81ab7c8c
https://doi.org/10.1002/cmdc.202000934
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10
Chiral Pool Synthesis, Biological Evaluation and Molecular Docking Studies ofC‐Furanosidic LpxC Inhibitors
Autor: Ralph Holl, Alexander Dreger, Wolfgang Sippl, Oriana Agoglitta, Omar Kharwb, Emre F. Bülbül, Jelena Melesina
Publikováno v: ChemMedChem. 14:871-886
Inhibitors of the bacterial deacetylase LpxC are a promising class of novel antibiotics, being selectively active against Gram-negative bacteria. To improve the biological activity of reported C-furanosidic LpxC inhibitors, the stereochemistry at pos
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da8a8df119f21a883c5635b61d97bc58
https://doi.org/10.1002/cmdc.201900068
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