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Mike Schutkowski

Explore the profile of Mike Schutkowski including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 93
Citations 1877
Followers 0
Related Specialties
Biochemistry
Molecular Biology
Chemistry
Top 10 Co-Authors
Wolfgang Sippl
Marat Meleshin
Clemens Steegborn
Johannes Zerweck
Matthes Zessin
Cyril Barinka
Gunter Fischer
Ulf Reimer
Sebastian Hilscher
Antonia Masch
Published In
Methods Mol Biol
J Biol Chem
J Mol Biol
Angew Chem Int Ed Engl
Nat Commun
Affiliations
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Recent Articles
1.
Dona Flor and her two husbands: Discovery of novel HDAC6/AKT2 inhibitors for myeloid cancer treatment
Waitman K, Martin H, Carlos J, Braga R, Souza V, Melo-Filho C, et al.
bioRxiv . 2024 Dec; PMID: 39677737
Highlights: Novel kinase/HDAC inhibitors for cancer treatment were found using machine learning61 QSAR models for hematological cancers and its targets were built and validatedK562, MV4-11, MM1S, NB-4, U937, and HDAC6...
2.
Probing class I histone deacetylases (HDAC) with proteolysis targeting chimera (PROTAC) for the development of highly potent and selective degraders
Ibrahim H, Guo M, Hilscher S, Erdmann F, Schmidt M, Schutkowski M, et al.
Bioorg Chem . 2024 Oct; 153:107887. PMID: 39423771
Class I HDACs are considered promising targets for cancer due to their role in epigenetic modifications. The main challenges in developing a new, potent and non-toxic class I HDAC inhibitor...
3.
Development of new pyrazoles as class I HDAC inhibitors: Synthesis, molecular modeling, and biological characterization in leukemia cells
Berluti F, Baselious F, Hagemann S, Hilscher S, Schmidt M, Huttelmaier S, et al.
Arch Pharm (Weinheim) . 2024 Sep; 357(11):e2400437. PMID: 39291901
Class I histone deacetylases (HDACs) are considered promising targets in current cancer research. To obtain subtype-selective and potent HDAC inhibitors, we used the aminobenzamide scaffold as the zinc-binding group and...
4.
Utilization of an optimized AlphaFold protein model for structure-based design of a selective HDAC11 inhibitor with anti-neuroblastoma activity
Baselious F, Hilscher S, Hagemann S, Tripathee S, Robaa D, Barinka C, et al.
Arch Pharm (Weinheim) . 2024 Jul; 357(10):e2400486. PMID: 38996352
AlphaFold is an artificial intelligence approach for predicting the three-dimensional (3D) structures of proteins with atomic accuracy. One challenge that limits the use of AlphaFold models for drug discovery is...
5.
Epigenetic-based differentiation therapy for Acute Myeloid Leukemia
Jose-Eneriz E, Gimenez-Camino N, Rabal O, Garate L, Miranda E, Gomez-Echarte N, et al.
Nat Commun . 2024 Jul; 15(1):5570. PMID: 38956053
Despite the development of novel therapies for acute myeloid leukemia, outcomes remain poor for most patients, and therapeutic improvements are an urgent unmet need. Although treatment regimens promoting differentiation have...
6.
Key structural requirements of benzamide derivatives for histone deacetylase inhibition: design, synthesis and biological evaluation
Cheshmazar N, Hamzeh-Mivehroud M, Hemmati S, Abolhasani H, Heidari F, Nozad Charoudeh H, et al.
Future Med Chem . 2024 Apr; 16(9):859-872. PMID: 38623995
Histone deacetylase inhibitors (HDACIs) are important as anticancer agents. This study aimed to investigate some key structural features of HDACIs via the design, synthesis and biological evaluation of novel benzamide-based...
7.
Comparative Structure-Based Virtual Screening Utilizing Optimized AlphaFold Model Identifies Selective HDAC11 Inhibitor
Baselious F, Hilscher S, Robaa D, Barinka C, Schutkowski M, Sippl W
Int J Mol Sci . 2024 Jan; 25(2). PMID: 38279359
HDAC11 is a class IV histone deacylase with no crystal structure reported so far. The catalytic domain of HDAC11 shares low sequence identity with other HDAC isoforms, which makes conventional...
8.
1,3-Diphenylureido hydroxamate as a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors
Tavares M, Kruger A, Yan S, Waitman K, Gomes V, de Oliveira D, et al.
Sci Rep . 2023 Nov; 13(1):21006. PMID: 38030668
We report a series of 1,3-diphenylureido hydroxamate HDAC inhibitors evaluated against sensitive and drug-resistant P. falciparum strains. Compounds 8a-d show potent antiplasmodial activity, indicating that a phenyl spacer allows improved...
9.
Design and synthesis of bioreductive prodrugs of class I histone deacetylase inhibitors and their biological evaluation in virally transfected acute myeloid leukemia cells
Abdelsalam M, Zmyslia M, Schmidtkunz K, Vecchio A, Hilscher S, Ibrahim H, et al.
Arch Pharm (Weinheim) . 2023 Nov; 357(2):e2300536. PMID: 37932028
Although histone deacetylase (HDAC) inhibitors show promise in treating various types of hematologic malignancies, they have some limitations, including poor pharmacokinetics and off-target side effects. Prodrug design has shown promise...
10.
Development of First-in-Class Dual Sirt2/HDAC6 Inhibitors as Molecular Tools for Dual Inhibition of Tubulin Deacetylation
Sinatra L, Vogelmann A, Friedrich F, Tararina M, Neuwirt E, Colcerasa A, et al.
J Med Chem . 2023 Oct; 66(21):14787-14814. PMID: 37902787
Dysregulation of both tubulin deacetylases sirtuin 2 (Sirt2) and the histone deacetylase 6 (HDAC6) has been associated with the pathogenesis of cancer and neurodegeneration, thus making these two enzymes promising...