Publikationen

Apotheker / akad. Rat a. Z.

PD Dr. Steffen Pockes

Gebäude CH, Zi. 14.1.27/24.1.81
Telefon 0941 943-4825
Telefax 0941 943-4809
E-Mail steffen.pockes@ur.de

(* = Corresponding Author)

2023:

(33) Köck, Z.; Schnelle, K.; Persechino, M.; Umbach, S.; Schihada, H.; Dovile, J.; Parey, K.; Pockes, S.; Kolb, P.; Dötsch, V.; Möller, A.; Hilger, D.; Bernhard, F. Cryo-EM structure of cell-free synthesized human histamine H2 receptor coupled to heterotrimeric Gs protein in lipid environment. Nature Communications, in revision 2023. (Preprint BioRxiv, https://doi.org/10.1101/2023.07.27.550782).

(32) Nagl, M.; Mönnich, D.; Rosier, N.; Schihada, H.; Sirbu, A.; Konar, N.; Reyes-Resina, I.; Navarro, G.; Franco, R.; Kolb, P.; Annibale, P.; Pockes, S.* Fluorescent Tools for Imaging and Ligand Screening of Dopamine D2-Like Receptors. ChemBioChem 2023, accepted article e202300659. https://doi.org/10.1002/cbic.202300659. (Preprint BioRxiv, https://doi.org/10.1101/2023.09.25.559398).

(31) Rosier, N.; Mönnich, D.; Nagl, M.; Schihada, H.; Sirbu, A.; Konar, N.; Reyes-Resina, I.; Navarro, G.; Franco, R.; Kolb, P.; Annibale, P.; Pockes, S.* Shedding Light on the D1-Like Receptors: A Fluorescence-Based Toolbox for Visualization of the D1 and D5 Receptors. ChemBioChem 2023, accepted article e202300658. https://doi.org/10.1002/cbic.202300658. (Preprint BioRxiv, https://doi.org/10.1101/2023.09.25.559386).

(30) Bresinsky, M.; Shahraki, A.; Kolb, P.; Pockes, S.*; Schihada, H.* Development of fluorescent AF64394 analogs enables real-time binding studies for the orphan class A GPCR GPR3. Journal of Medicinal Chemistry 2023, 66 (21), 15025-15041. https://doi.org/10.1021/acs.jmedchem.3c01707.

(29) Mönnich, D.; Nagl, M.; Forster, L.; Rosier, N.; Igel, P.*; Pockes, S.* Discovery of a Tritiated Radioligand with High Affinity and Selectivity for the Histamine H3 Receptor. ACS Medicinal Chemistry Letters 2023, 14 (11), 1589-1595. https://doi.org/10.1021/acsmedchemlett.3c00413.

(28) Neumann, J.*; Pockes, S.; Humphrys, L. J.; Mönnich, D.; Forster, L.; Kirchhefer, U.; Hofmann, B.; Gergs, U. Clonidine stimulates force of contraction via histamine H2 receptors in the human atrium. Naunyn-Schmiedeberg's Archives of Pharmacology, published online July 25, 2023. https://doi.org/10.1007/s00210-023-02635-x.

(27) Cuellar, M. E.; Yang, M.; Karavadhi, S.; Zhang, Y.; Sun, H.; Shen, M.; Hall, M. D.; Patnaik, S.; Ashe, K. H.; Walters, M. A.*; Pockes, S.* An electrophilic fragment screening for the development of small molecules targeting caspase-2. European Journal of Medicinal Chemistry 2023, 259, 115632. https://doi.org/10.1016/j.ejmech.2023.115632.

(26) Szczepanska, K.; Karcz, T*.; Dichiara, M.; Mogilski, S.; Kalinowska-Tłuścik, J.; Pilarski, B.; Leniak, A.; Pietruś, W.; Podlewska, S.; Popiołek-Barczyk, K.; Humphrys, L.; Ruiz Cantero, M. C.; Reiner-Link, D.; Leitzbach, L.; Łażewska, D.; Pockes, S.; Górka, M.; Calmels, T.; Cobos, E.; Marrazzo, A.; Stark, H.; Bojarski, A.*; Amata, A.; Kiec-Kononowicz, K.* Dual piperidine-based histamine H3 and sigma-1 receptor ligands in the treatment of nociceptive and neuropathic pain. Journal of Medicinal Chemistry 2023, 66 (14), 9658-9683. https://doi.org/10.1021/acs.jmedchem.3c00430.

(25) Gergs, U.; Jakob, H.; Braekow, P.; Hofmann, B.; Pockes, S.; Humphrys, L. J.; Kirchhefer, U.; Fehse, C.; Neumann, J.* Lysergic acid diethylamide stimulates cardiac human H2 histamine receptors. Naunyn-Schmiedeberg's Archives of Pharmacology, published online July 4, 2023. https://doi.org/10.1007/s00210-023-02591-6.

(24) Jakob, H.; Braekow, P.; Hofmann, B.; Kirchhefer, U.; Forster, L.; Mönnich, D.; Humphrys, L. J.; Pockes, S.; Neumann, J.*; Gergs, U. Ergometrine stimulates histamine H2 receptors in the isolated human atrium. Naunyn-Schmiedeberg's Archives of Pharmacology, published online June 24, 2023. https://doi.org/10.1007/s00210-023-02573-8.

2022:

(23) Pockes, S.*; Walters, M. A.; Ashe, K. H.* Targeting caspase-2 interactions with tau in Alzheimer's disease and related dementias. Translational Science 2022, 254, 34-40. https://doi.org/10.1016/j.trsl.2022.10.009.

(22) Forster, L.*; Pockes, S.* Investigation of the ligand agonism and antagonism at the D2long receptor by dynamic mass redistribution. Scientific Reports 2022, 12 (1), 9637. https://doi.org/10.1038/s41598-022-14311-w.

(21) Bresinsky, M.; Strasser, J. M.; Hubmann, A.; Vallaster, B.; McCue, W. M.; Fuller, J.; Singh, G.; Nelson, K. M.; Cuellar, M. E.; Finzel, B. C.; Ashe, K. H.; Walters, M. A.*; Pockes, S.* Characterization of caspase-2 inhibitors based on specific sites of caspase-2-mediated proteolysis. Archiv der Pharmazie 2022, e2200095. https://doi.org/10.1002/ardp.202200095.

(20) Singh, G.; Liu, P.; Yao, K. R.; Strasser, J. M.; Hlynialuk, C.; Leinonen-Wright, K.; Teravskis, P. J.; Choquette, J. M.; Ikramuddin, J.; Bresinsky, M.; Nelson, K. M.; Liao, D.; Ashe, K. H.; Walters, M. A.*; Pockes, S.* A caspase-2 inhibitor blocks tau truncation and restores excitatory neurotransmission in neurons modeling FTDP-17 tauopathy. ACS Chemical Neuroscience 2022, 13 (10), 1549-1557. https://doi.org/10.1021/acschemneuro.2c00100.

(19) Bresinsky, M.; Strasser, J. M.; Vallaster, B.; Liu, P.; McCue, W. M.; Fuller, J.; Hubmann, A.; Singh, G.; Nelson, K. M.; Cuellar, M. E.; Wilmot, C. M.; Finzel, B. C.; Ashe, K. H.; Walters, M. A.*; Pockes, S.* Structure-Based Design and Biological Evaluation of Novel Caspase-2 Inhibitors Based on the Peptide AcVDVAD-CHO and the Caspase-2-Mediated Tau Cleavage Sequence YKPVD. ACS Pharmacology & Translational Science 2022, 5 (1), 20-40. https://doi.org/10.1021/acsptsci.1c00251.

(18) Szczepanska, K.; Podlewska, S.; Dichiara, M.; Gentile, D.; Patamia, V.; Rosier, N.; Mönnich, D.; Ruiz-Cantero, M. C.; Karcz, T.; Łażewska, D.; Pockes, S.; Siwek, A.; Cobos, E. J.; Marrazzo, A.; Stark, H.; Rescifina, A.; Bojarski, A. J.; Amata, E.*; Kieć-Kononowicz, K.* Structural and molecular insight into piperazine and piperidine derivatives as dual-acting histamine H3 and sigma-1 receptor antagonists with promising antinociceptive properties. ACS Chemical Neuroscience 2022, 13 (1), 1-15. https://doi.org/10.1021/acschemneuro.1c00435.

2021:

(17) Gergs, U.; Büxel, M.; Bresinsky, M.; Kirchhefer, U.; Fehse, C.; Hofmann, B.; Marusakova, M.; Čináková, A.; Schwarz, R.; Pockes, S.; Neumann, J.* Cardiac effects of novel histamine H2 receptor agonists. Journal of Pharmacology and Experimental Therapeutics 2021, 379 (3), 223-234. https://doi.org/10.1124/jpet.121.000822.

(16) Rosier, N.; Grätz, L.*; Schihada, H.; Möller, J.; Isbilir, A.; Nagl, M.; Seibel, U.; Lohse, M. J.; Pockes, S.* A Versatile Subnanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H3 Receptor. Journal of Medicinal Chemistry 2021, 64 (15), 11695-11708. https://doi.org/10.1021/acs.jmedchem.1c01089.

(15) Tropmann, K.; Bresinsky, M.; Forster, L.; Buschauer, A.; Wittmann, H.J.; Hübner, H.; Gmeiner, P.; Pockes, S.*; Strasser A.* Abolishing Dopamine D2long/D3 Receptor Affinity of Subtype-Selective Carbamoylguanidine-Type Histamine H2R Agonists. Journal of Medicinal Chemistry 2021, 64 (12), 8684-8709. https://doi.org/10.1021/acs.jmedchem.1c00692.

(14) Pockes, S.*; Tropmann, K. Histamine H2 Receptor Radioligands: Triumphs and Challenges. Future Medicinal Chemistry 2021, 13 (12), 1073-1081. https://doi.org/10.4155/fmc-2021-0058.

(13) Biselli, S.; Bresinsky, M.; Tropmann, K.; Forster, L.; Honisch, C.; Buschauer, A.; Bernhardt, G.; Pockes, S.* Pharmacological characterization of a new series of carbamoylguanidines reveals potent agonism at the H2R and D3R. European Journal of Medicinal Chemistry 2021, 214, 113190. https://doi.org/10.1016/j.ejmech.2021.113190.

2020:

(12) Szczepanska, K.; Pockes, S.*; Podlewska, S.; Höring, C.; Mika, K.; Latacz, G.; Bednarski, M; Siwek, A.; Karcz, T.; Nagl, M.; Bresinsky, M.; Mönnich, D.; Seibel, U.; Kuder, K.J.; Kotańska, M.; Stark, H.; Elz, S.; Kieć-Kononowicz, K.* Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent. European Journal of Medicinal Chemistry 2020, 213, 113041. https://doi.org/10.1016/j.ejmech.2020.113041.

(11) Höring, C.; Seibel, U.; Tropmann, K.; Grätz, L.; Mönnich, D.; Pitzl, S.; Bernhardt, G.; Pockes, S.; Strasser, A.* A dynamic, split-luciferase-based mini-G protein sensor to functionally characterize ligands at all four histamine receptor subtypes. International journal of molecular sciences 2020, 21 (22), 8440. https://doi.org/10.3390/ijms21228440.

(10) Tropmann, K.; Höring, C.; Plank, N.; Pockes, S.* Discovery of a G Protein-Biased Radioligand for the Histamine H2 Receptor with Reversible Binding Properties. Journal of Medicinal Chemistry 2020, 63 (21), 13090-13102. https://doi.org/10.1021/acs.jmedchem.0c01494.

(9) Forster, L.; Grätz, L.; Mönnich, D.; Bernhardt, G.; Pockes, S.* A Split Luciferase Complementation Assay for the Quantification of β-Arrestin2 Recruitment to Dopamine D2-like Receptors. International journal of molecular sciences 2020, 21 (17), 6103. https://doi.org/10.3390/ijms21176103.

(8) Grätz, L.; Tropmann, K.; Bresinsky, M.; Müller, C.; Bernhardt, G.; Pockes, S.* NanoBRET Binding Assay for Histamine H2 Receptor Ligands Using Live Recombinant HEK293T Cells. Scientific Reports 2020, 10 (1), 13288. https://doi.org/10.1038/s41598-020-70332-3.

(7) Schihada, H.*; Ma, X.; Zabel, U.; Vischer, H. F.; Schulte, G.; Leurs, R.; Pockes, S.; Lohse, M. J.* Development of a Conformational Histamine H3 Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists. ACS Sensors 2020, 5 (6), 1734–1742. https://doi.org/10.1021/acssensors.0c00397.

2019:

(6) Soliman, B.; Wang, N.; Zagotto, G.; Pockes, S.* Synthesis and Biological Evaluation of Heteroalicyclic Cyanoguanidines at Histamine Receptors. Archiv der Pharmazie 2019, 352, 1900107. https://doi.org/10.1002/ardp.201900107.

(5) Pockes, S.*; Wifling, D.; Buschauer, A.; Elz, S. Structure-Activity Relationship of Hetarylpropylguanidines Aiming at the Development of Selective Histamine Receptor Ligands. ChemistryOpen 2019, 8, 285-297. doi.org/10.1002/open.201900011.

(4) Rustler, K.; Pockes, S.* and König, B*. Light-switchable Antagonists for the Histamine H1 Receptor at the Isolated Guinea Pig Ileum. ChemMedChem 2019, 14, 636-644. https://doi.org/10.1002/cmdc.201800815.

2018:

(3) Pockes, S.*; Wifling, D.; Keller, M.; Buschauer, A.; Elz, S. Highly Potent, Stable, and Selective Dimeric Hetarylpropylguanidine-Type Histamine H2 Receptor Agonists. ACS Omega 2018, 3, 2865–2882. https://doi.org/10.1021/acsomega.8b00128.

2016:

(2) Sadek, B.; Khan, N.; Darras, F. H.; Pockes, S.; Decker, M.* The Dual-Acting AChE Inhibitor and H3 Receptor Antagonist UW-MD-72 Reverses Amnesia Induced by Scopolamine or Dizocilpine in Passive Avoidance Paradigm in Rats. Physiology & Behavior 2016, 165, 383–391. https://doi.org/10.1016/j.physbeh.2016.08.022.

2014:

(1) Darras, F. H.; Pockes, S.; Huang, G.; Wehle, S.; Strasser, A.; Wittmann, H.-J.; Nimczick, M.; Sotriffer, C. A.; Decker, M.* Synthesis, Biological Evaluation, and Computational Studies of Tri-and Tetracyclic Nitrogen-Bridgehead Compounds as Potent Dual-Acting AChE Inhibitors and hH3 Receptor Antagonists. ACS Chemical Neuroscience 2014, 5, 225–242. https://doi.org/10.1021/cn4002126.