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Stephan Grzesiek

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Articles 98
Citations 2577
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Recent Articles
1.
Conflitti P, Lyman E, Sansom M, Hildebrand P, Gutierrez-de-Teran H, Carloni P, et al.
Nat Rev Drug Discov . 2025 Jan; PMID: 39747671
G protein-coupled receptors (GPCRs) are the largest human membrane protein family that transduce extracellular signals into cellular responses. They are major pharmacological targets, with approximately 26% of marketed drugs targeting...
2.
Petrovic I, Grzesiek S, Isaikina P
Biochem Soc Trans . 2024 Nov; 52(6):2333-2342. PMID: 39508463
Arrestins are essential proteins for the regulation of G protein-coupled receptors (GPCRs). They mediate GPCR desensitization after the activated receptor has been phosphorylated by G protein receptor kinases (GRKs). In...
3.
Paladini J, Maier A, Habazettl J, Hertel I, Sonti R, Grzesiek S
Elife . 2024 Apr; 12. PMID: 38588001
Abelson tyrosine kinase (Abl) is regulated by the arrangement of its regulatory core, consisting sequentially of the SH3, SH2, and kinase (KD) domains, where an assembled or disassembled core corresponds...
4.
Grzesiek S, Paladini J, Habazettl J, Sonti R
Magn Reson (Gott) . 2023 Oct; 3(1):91-99. PMID: 37905178
It was recently reported (Xie et al., 2022) that the Abelson tyrosine kinase (Abl) ATP-site inhibitor imatinib also binds to Abl's myristoyl binding pocket, which is the target of allosteric...
5.
Wu F, Kronenberg D, Hertel I, Grzesiek S
J Biol Chem . 2023 Aug; 299(10):105142. PMID: 37553040
Nuclear magnetic resonance studies of many physiologically important proteins have long been impeded by the necessity to express such proteins in isotope-labeled form in higher eukaryotic cells and the concomitant...
6.
Isaikina P, Petrovic I, Jakob R, Sarma P, Ranjan A, Baruah M, et al.
Mol Cell . 2023 May; 83(12):2108-2121.e7. PMID: 37244255
The two non-visual arrestins, arrestin2 and arrestin3, bind hundreds of GPCRs with different phosphorylation patterns, leading to distinct functional outcomes. Structural information on these interactions is available only for very...
7.
Wu F, Rieder P, Abiko L, Rossler P, Gossert A, Haussinger D, et al.
J Am Chem Soc . 2022 Nov; 144(47):21728-21740. PMID: 36394272
NMR chemical shift changes can report on the functional dynamics of biomacromolecules in solution with sizes >1 MDa. However, their interpretation requires chemical shift assignments to individual nuclei, which for...
8.
Jahnke W, Paladini J, Habazettl J, Wiget A, Loo A, Cowan Jacob S, et al.
Angew Chem Int Ed Engl . 2022 Oct; 61(46):e202117276. PMID: 36257909
Soellner published on the interplay between allosteric and adenosine triphosphate (ATP)-competitive inhibitors of ABL kinase, showing that the latter preferably binds to different conformational states of ABL compared to allosteric...
9.
Abiko L, Teixeira R, Engilberge S, Grahl A, Muhlethaler T, Sharpe T, et al.
Nat Chem . 2022 Aug; 14(10):1133-1141. PMID: 35953642
Recent high-pressure NMR results indicate that the preactive conformation of the β-adrenergic receptor (βAR) harbours completely empty cavities of ~100 Å volume, which disappear in the active conformation of the...
10.
Isaikina P, Tsai C, Petrovic I, Rogowski M, Durr A, Grzesiek S
Methods Cell Biol . 2022 May; 169:115-141. PMID: 35623699
The numerous chemokines and their cognate G protein-coupled chemokine receptors on the surface of leukocytes form a complex signaling network, which regulates the immune response and also other key physiological...