Holger Steuber
Overview
Explore the profile of Holger Steuber including associated specialties, affiliations and a list of published articles.
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Articles
37
Citations
731
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Recent Articles
1.
Graham K, Lienau P, Bader B, Prechtl S, Naujoks J, Lesche R, et al.
Cell Chem Biol
. 2024 Mar;
31(7):1247-1263.e16.
PMID: 38537632
This study describes the identification and target deconvolution of small molecule inhibitors of oncogenic Yes-associated protein (YAP1)/TAZ activity with potent anti-tumor activity in vivo. A high-throughput screen (HTS) of 3.8...
2.
Bothe U, Gunther J, Nubbemeyer R, Siebeneicher H, Ring S, Bomer U, et al.
J Med Chem
. 2024 Jan;
67(2):1225-1242.
PMID: 38228402
Interleukin-1 receptor-associated kinase 4 (IRAK4) plays a critical role in innate inflammatory processes. Here, we describe the discovery of two clinical candidate IRAK4 inhibitors, (zabedosertib) and , starting from a...
3.
Meibom D, Micus S, Andreevski A, Anlauf S, Bogner P, von Buehler C, et al.
J Med Chem
. 2022 Dec;
65(24):16420-16431.
PMID: 36475653
Despite advances in the treatment of heart failure in recent years, options for patients are still limited and the disease is associated with considerable morbidity and mortality. Modulating cyclic guanosine...
4.
Gradl S, Steuber H, Weiske J, Szewczyk M, Schmees N, Siegel S, et al.
SLAS Discov
. 2021 Jun;
26(8):947-960.
PMID: 34154424
SMYD3 (SET and MYND domain-containing protein 3) is a protein lysine methyltransferase that was initially described as an H3K4 methyltransferase involved in transcriptional regulation. SMYD3 has been reported to methylate...
5.
Sutherland M, Li A, Kaghad A, Panagopoulos D, Li F, Szewczyk M, et al.
ChemMedChem
. 2021 Jan;
16(7):1116-1125.
PMID: 33513288
Protein arginine N-methyl transferase 4 (PRMT4) asymmetrically dimethylates the arginine residues of histone H3 and nonhistone proteins. The overexpression of PRMT4 in several cancers has stimulated interest in the discovery...
6.
Lemos C, Schulze L, Weiske J, Meyer H, Braeuer N, Barak N, et al.
iScience
. 2020 Sep;
23(9):101517.
PMID: 32927263
Structural mutants of p53 induce global p53 protein destabilization and misfolding, followed by p53 protein aggregation. First evidence indicates that p53 can be part of protein condensates and that p53...
7.
Darolutamide is a potent androgen receptor antagonist with strong efficacy in prostate cancer models
Sugawara T, Baumgart S, Nevedomskaya E, Reichert K, Steuber H, Lejeune P, et al.
Int J Cancer
. 2019 Mar;
145(5):1382-1394.
PMID: 30828788
Darolutamide is a novel androgen receptor (AR) antagonist with a distinct chemical structure compared to other AR antagonists and currently in clinical Phase 3 trials for prostate cancer. Using cell-based...
8.
Johansson C, Velupillai S, Tumber A, Szykowska A, Hookway E, Nowak R, et al.
Nat Chem Biol
. 2016 May;
12(7):539-45.
PMID: 27214403
Members of the KDM5 (also known as JARID1) family are 2-oxoglutarate- and Fe(2+)-dependent oxygenases that act as histone H3K4 demethylases, thereby regulating cell proliferation and stem cell self-renewal and differentiation....
9.
Ferreira de Freitas R, Eram M, Szewczyk M, Steuber H, Smil D, Wu H, et al.
J Med Chem
. 2016 Jan;
59(3):1176-83.
PMID: 26824386
Protein methyltransferases (PMTs) are a promising target class in oncology and other disease areas. They are composed of SET domain methyltransferases and structurally unrelated Rossman-fold enzymes that include protein arginine...
10.
Vasbinder M, Alimzhanov M, Augustin M, Bebernitz G, Bell K, Chuaqui C, et al.
Bioorg Med Chem Lett
. 2015 Nov;
26(1):60-7.
PMID: 26614408
We have identified a class of azabenzimidazoles as potent and selective JAK1 inhibitors. Investigations into the SAR are presented along with the structural features required to achieve selectivity for JAK1...