Tobias Gabriel
Overview
Explore the profile of Tobias Gabriel including associated specialties, affiliations and a list of published articles.
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Articles
8
Citations
291
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0
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Recent Articles
1.
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob S, et al.
J Med Chem
. 2018 Aug;
61(18):8120-8135.
PMID: 30137981
Chronic myelogenous leukemia (CML) arises from the constitutive activity of the BCR-ABL1 oncoprotein. Tyrosine kinase inhibitors (TKIs) that target the ATP-binding site have transformed CML into a chronic manageable disease....
2.
Gabriel T, Rommel D, Scherm F, Gorywoda M, Glatzel U
Materials (Basel)
. 2017 Aug;
10(3).
PMID: 28772639
Laser cladding is a well-established process to apply coatings on metals. However, on substrates considerably thinner than 1 mm it is only rarely described in the literature. In this work...
3.
Huang Y, Zhang J, Yu Z, Zhang H, Wang Y, Lingel A, et al.
J Med Chem
. 2017 Jan;
60(6):2215-2226.
PMID: 28092155
Overexpression and somatic heterozygous mutations of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2), are associated with several tumor types. EZH2 inhibitor, EPZ-6438 (tazemetostat), demonstrated clinical efficacy in...
4.
Lingel A, Sendzik M, Huang Y, Shultz M, Cantwell J, Dillon M, et al.
J Med Chem
. 2016 Dec;
60(1):415-427.
PMID: 27992714
PRC2 is a multisubunit methyltransferase involved in epigenetic regulation of early embryonic development and cell growth. The catalytic subunit EZH2 methylates primarily lysine 27 of histone H3, leading to chromatin...
5.
Lou Y, Han X, Kuglstatter A, Kondru R, Sweeney Z, Soth M, et al.
J Med Chem
. 2014 Apr;
58(1):512-6.
PMID: 24712864
Structure-based drug design was used to guide the optimization of a series of selective BTK inhibitors as potential treatments for Rheumatoid arthritis. Highlights include the introduction of a benzyl alcohol...
6.
Soth M, Abbot S, Abubakari A, Arora N, Arzeno H, Billedeau R, et al.
Bioorg Med Chem Lett
. 2011 Apr;
21(11):3452-6.
PMID: 21515047
Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.
7.
Goldstein D, Soth M, Gabriel T, Dewdney N, Kuglstatter A, Arzeno H, et al.
J Med Chem
. 2011 Mar;
54(7):2255-65.
PMID: 21375264
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid...
8.
Goldstein D, Gabriel T
Curr Top Med Chem
. 2005 Sep;
5(10):1017-29.
PMID: 16178744
p38 mitogen activated protein (MAP) kinase remains the most compelling therapeutic target for oral drug intervention for a wide range of autoimmune disorders based on the central role this enzyme...