New Smoothened ligands based on the purine scaffold as potential agents for treating pancreatic cancer.

C. Espinosa-Bustos, J. Bertrand, Alondra Villegas-Menares, Simón Guerrero, L. Di Marcotullio, Shirin Navacci, Gunnar Schulte, P. Kozielewicz, Nicolas Bloch, Valentina Villela, Margot Paulino, Marcelo J. Kogan, Jorge Cantero, Cristian O Salas

Bioorganic chemistry (Print), 2024

Frizzleds act as dynamic pharmacological entities.

Gunnar Schulte, Magdalena M. Scharf, J. Bous, Jan Hendrik Voss, Lukas Grätz, P. Kozielewicz

TIPS - Trends in Pharmacological Sciences, 2024

Application of FRET- and BRET-based live-cell biosensors in deorphanization and ligand discovery studies on orphan G protein-coupled receptors.

Joanna J. Sajkowska, Choi Har Tsang, P. Kozielewicz

SLAS discovery : advancing life sciences R & D, 2024

Structural and functional insight into the interaction of Clostridioides difficile toxin B and FZD7.

Julia Kinsolving, Julien Bous, P. Kozielewicz, Sara Košenina, Rawan Shekhani, Lukas Grätz, G. Masuyer, Yuankai Wang, P. Stenmark, Min Dong, Gunnar Schulte

Cell Reports, 2024

Progress on the development of Class A GPCR-biased ligands.

Paula Morales, Magdalena M Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K Hansen, Nadine Jagerovic, Jan Jakubík, György M Keserű, Dóra Judit Kiss, P. Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo-Abreu, Gemma Navarro, Rubén Prieto-Díaz, M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, L. Wingler

British Journal of Pharmacology, 2024

WNT stimulation induces dynamic conformational changes in the Frizzled-Dishevelled interaction

Carl-Fredrik Bowin, P. Kozielewicz, Lukas Grätz, Maria Kowalski-Jahn, Hannes Schihada, G. Schulte

Science Signaling, 2023

Class Frizzled GPCRs in GtoPdb v.2023.1 Class Frizzled GPCRs in GtoPdb v.2023.1

E. Arthofer, J. Dijksterhuis, Lukas Grätz, B. Hot, P. Kozielewicz, M. Lauth, J. Olofsson, J. Petersen, Tilman Polonio, G. Schulte, Kateřina Straková, Jana Valnohova, Shane C. Wright

2023

NanoBiT- and NanoBiT/BRET-based assays allow the analysis of binding kinetics of WNT-3A to endogenous Frizzled 7 in a colorectal cancer model.

Lukas Grätz, J. J. Sajkowska-Kozielewicz, Janine Wesslowski, Julia Kinsolving, L. Bridge, Katja Petzold, G. Davidson, G. Schulte, P. Kozielewicz

British Journal of Pharmacology, 2023

Pathway selectivity in Frizzleds is achieved by conserved micro-switches defining pathway-determining, active conformations

Lukas Grätz, Maria Kowalski-Jahn, Magdalena M. Scharf, P. Kozielewicz, Michael Jahn, J. Bous, N. Lambert, D. Gloriam, G. Schulte

Nature Communications, 2023

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors

Stephen P H Alexander, A. Christopoulos, Anthony P Davenport, E. Kelly, A. Mathie, John A Peters, E. Veale, J. Armstrong, E. Faccenda, S. Harding, J. Davies, M. Abbracchio, George Abraham, Alexander Agoulnik, Wayne Alexander, Khaled A. Al‐Hosaini, Magnus Bäck, Jillian G. Baker, Nicholas M. Barnes, Ross A. D. Bathgate, Jean‐Martin Beaulieu, Annette G. Beck-Sickinger, Maik Behrens, Kenneth E. Bernstein, Bernhard Bettler, Nigel J. M. Birdsall, V. Blaho, Franc¸ois Boulay, Corinne Bousquet, H. Bräuner‐Osborne, Geoffrey Burnstock, Girolamo Calo’, Justo P. Castaño, K. J. Catt, S. Ceruti, P. Chazot, Chia Nan, Bice Chini, Jerold Chun, A. Cianciulli, Olivier Civelli, L. Clapp, Réjean Couture, Helen M. Cox, Z. Csaba, Claes Dahlgren, Gordon Dent, Steven D. Douglas, Pascal Dournaud, Satoru Eguchi, Emanuel Escher, E. Filardo, Tung Fong, M. Fumagalli, R. Gainetdinov, Michael L Garelja, Marc Gasparo, Craig Gerard, M. Gershengorn, Fernand Junior Gobeil, T. Goodfriend, C. Goudet, Lukas Grätz, K. Gregory, A. L. Gundlach, Jörg Hamann, Julien Hanson, R. Hauger, Deborah L. Hay, A. Heinemann, D. Herr, M. Hollenberg, N. Holliday, M. Horiuchi, D. Hoyer, László Hunyady, Ahsan Husain, A. P. IJzerman, Tadashi Inagami, Kenneth A. Jacobson, R. Jensen, Ralf Jockers, Deepa Jonnalagadda, S. Karnik, K. Kaupmann, Jacqueline R. Kemp, Charles Kennedy, Yasuyuki Kihara, Takio Kitazawa, Paweł Kozielewicz, H. Kreienkamp, J. Kukkonen, T. Langenhan, D. Larhammar, K. Leach, D. Lecca, John D. Lee, Susan E. Leeman, Jérôme Leprince, Xaria X. Li, S. Lolait, A. Lupp, Robyn G. C. Macrae, J. Maguire, D. Malfacini, J. Mazella, C. McArdle, S. Melmed, Martin C. Michel, Laurence J. Miller, V. Mitolo, B. Mouillac, Christa E. Müller, P. M. Murphy, J. Nahon, Tony Ngo, Xavier Norel, Duuamene Nyimanu, A. O'Carroll, Stefan Offermanns, M. Panaro, Marc Parmentier, R. Pertwee, Jean-Philippe Pin, E. Prossnitz, Mark T. Quinn, R. Ramachandran, Manisha Ray, R. Reinscheid, P. Rondard, G. Rovati, C. Ruzza, Gareth J Sanger, Torsten Schöneberg, G. Schulte, Stefan Schulz, D. Segaloff, Charles N. Serhan, K. D. Singh, Craig M. Smith, Leigh A. Stoddart, Yukihiko Sugimoto, Roger Summers, Valerie Tan, D. Thal, Walter ( Wally) Thomas, Pieter B. M. W. M. Timmermans, Kalyan C. Tirupula, L. Toll, G. Tulipano, Hamiyet Unal, Thomas Unger, C. Valant, P. Vanderheyden, D. Vaudry, H. Vaudry, J. Vilardaga, Christopher Walker, Ji Ming Wang, Donald T. Ward, Hans-Juergen Wester, G. Willars, Tom Lloyd Williams, Trent M. Woodruff, Chengcan Yao, Richard D. Ye

British Journal of Pharmacology, 2023

NanoBRET and NanoBiT/BRET-Based Ligand Binding Assays Permit Quantitative Assessment of Small Molecule Ligand Binding to Smoothened.

P. Kozielewicz, G. Schulte

Methods in molecular biology, 2022

Residue 6.43 defines receptor function in class F GPCRs

Ainoleena Turku, Hannes Schihada, P. Kozielewicz, Carl-Fredrik Bowin, G. Schulte

Nature Communications, 2021

Cryo-EM structure of constitutively active human Frizzled 7 in complex with heterotrimeric Gs

Lu Xu, Bo Chen, Hannes Schihada, Shane C. Wright, Ainoleena Turku, Yiran Wu, G. Han, Maria Kowalski-Jahn, P. Kozielewicz, Carl-Fredrik Bowin, Xianjun Zhang, Chao Li, M. Bouvier, G. Schulte, Fei Xu

Cell Research, 2021

Employing Genetically Encoded, Biophysical Sensors to Understand WNT/Frizzled Interaction and Receptor Complex Activation.

P. Kozielewicz, Hannes Schihada, G. Schulte

Handbook of Experimental Pharmacology, 2021

Quantitative Profiling of WNT-3A Binding to All Human Frizzled Paralogues in HEK293 Cells by NanoBiT/BRET Assessments

P. Kozielewicz, Rawan Shekhani, Stefanie Moser, Carl-Fredrik Bowin, Janine Wesslowski, G. Davidson, G. Schulte

ACS Pharmacology & Translational Science, 2021

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors

Stephen P. H. Alexander, A. Christopoulos, A. Davenport, E. Kelly, A. Mathie, J. A. Peters, E. Veale, J. Armstrong, E. Faccenda, S. Harding, Adam J. Pawson, C. Southan, J. Davies, M. Abbracchio, Wayne Alexander, Khaled Al-hosaini, M. Bäck, N. Barnes, R. Bathgate, J. Beaulieu, K. Bernstein, B. Bettler, N. Birdsall, V. Blaho, F. Boulay, C. Bousquet, H. Bräuner‐Osborne, G. Burnstock, G. Calo’, J. Castaño, K. Catt, S. Ceruti, P. Chazot, N. Chiang, B. Chini, J. Chun, A. Cianciulli, O. Civelli, L. Clapp, R. Couture, Z. Csaba, C. Dahlgren, G. Dent, K. D. Singh, S. Douglas, P. Dournaud, S. Eguchi, E. Escher, E. Filardo, T. Fong, M. Fumagalli, R. Gainetdinov, M. Gasparo, C. Gerard, M. Gershengorn, F. Gobeil, T. Goodfriend, C. Goudet, K. Gregory, A. Gundlach, J. Hamann, J. Hanson, R. Hauger, D. Hay, A. Heinemann, M. Hollenberg, N. Holliday, M. Horiuchi, D. Hoyer, L. Hunyady, A. Husain, A. IJzerman, T. Inagami, K. Jacobson, R. Jensen, R. Jockers, Deepa Jonnalagadda, S. Karnik, K. Kaupmann, Jacqueline R. Kemp, C. Kennedy, Y. Kihara, T. Kitazawa, P. Kozielewicz, H. Kreienkamp, J. Kukkonen, T. Langenhan, K. Leach, D. Lecca, John D. Lee, S. Leeman, J. Leprince, Xaria X. Li, Thomas L. Williams, S. Lolait, A. Lupp, Robyn G. C. Macrae, J. Maguire, J. Mazella, C. McArdle, S. Melmed, M. Michel, L. Miller, V. Mitolo, B. Mouillac, C. Müller, Philip Murphy, J. Nahon, T. Ngo, X. Norel, Duuamene Nyimanu, A. O'Carroll, S. Offermanns, M. Panaro, M. Parmentier, R. Pertwee, J. Pin, E. Prossnitz, M. Quinn, R. Ramachandran, Manisha Ray, R. Reinscheid, P. Rondard, G. Rovati, C. Ruzza, G. Sanger, T. Schöneberg, G. Schulte, S. Schulz, D. Segaloff, C. Serhan, Leigh A. Stoddart, Y. Sugimoto, R. Summers, V. P. Tan, D. Thal, Walters Thomas, P. Timmermans, Kalyan C. Tirupula, G. Tulipano, Hamiyet Unal, T. Unger, C. Valant, P. Vanderheyden, D. Vaudry, H. Vaudry, J. Vilardaga, C. Walker, Ji Ming Wang, D. Ward, H. Wester, G. Willars, T. Woodruff, Chengcan Yao, R. Ye

British Journal of Pharmacology, 2021

Mitochondrial protein biogenesis in the synapse is supported by local translation

Bożena Kuźniewska, D. Cysewski, Michał Wasilewski, Paulina Sakowska, J. Miłek, Tomasz M. Kuliński, M. Winiarski, P. Kozielewicz, E. Knapska, M. Dadlez, A. Chacińska, A. Dziembowski, M. Dziembowska

EMBO Reports, 2020

eGFP-tagged Wnt-3a enables functional analysis of Wnt trafficking and signaling and kinetic assessment of Wnt binding to full-length Frizzled

Janine Wesslowski, P. Kozielewicz, Xianxian Wang, Haijun Cui, Hannes Schihada, Dominique Kranz, Pradhipa Karuna M, P. Levkin, J. Gross, M. Boutros, G. Schulte, G. Davidson

Journal of Biological Chemistry, 2020

Geissospermiculatine, a New Alkaloid from Geissospermum reticulatum Bark

J. J. Sajkowska-Kozielewicz, P. Kozielewicz, K. Makarova, Marcin Stocki, N. Barnes, K. Paradowska

Molecules, 2020

Structural insight into small molecule action on Frizzleds

P. Kozielewicz, Ainoleena Turku, Carl-Fredrik Bowin, J. Petersen, J. Valnohova, Maria Consuelo Alonso Cañizal, Yuki Ono, A. Inoue, C. Hoffmann, G. Schulte

Nature Communications, 2020

Molecular Pharmacology of Class F Receptor Activation

P. Kozielewicz, Ainoleena Turku, G. Schulte

Molecular Pharmacology, 2020

Mitochondria biogenesis in the synapse is supported by local translation

Bożena Kuźniewska, D. Cysewski, Michał Wasilewski, Paulina Sakowska, J. Miłek, Tomasz M. Kuliński, P. Kozielewicz, M. Dadlez, A. Chacińska, A. Dziembowski, M. Dziembowska

bioRxiv, 2019

Structural insight into Class F receptors - What have we learnt regarding agonist-induced activation?

G. Schulte, P. Kozielewicz

Basic & Clinical Pharmacology & Toxicology, 2019

Comment on: Triazoles bind the C-terminal domain of SMO: Illustration by docking and molecular dynamics simulations the binding between SMO and triazoles.

P. Kozielewicz

Life Science, 2019

A NanoBRET-Based Binding Assay for Smoothened Allows Real-time Analysis of Ligand Binding and Distinction of Two Binding Sites for BODIPY-cyclopamine

P. Kozielewicz, Carl-Fredrik Bowin, Ainoleena Turku, G. Schulte

Molecular Pharmacology, 2019

Overexpression of Orphan Receptor GPR61 Increases cAMP Levels upon Forskolin Stimulation in HEK293 Cells: in vitro and in silico Validation of 5-(Nonyloxy)Tryptamine as a Low-Affinity Inverse Agonist

P. Kozielewicz, G. Grafton, J. J. Sajkowska-Kozielewicz, N. Barnes

Pharmacology, 2019

A conserved molecular switch in Class F receptors regulates receptor activation and pathway selection

Shane C. Wright, P. Kozielewicz, Maria Kowalski-Jahn, J. Petersen, Carl-Fredrik Bowin, G. Slodkowicz, M. Marti-Solano, D. Rodríguez, B. Hot, Najeah Okashah, Kateřina Straková, J. Valnohova, M. Madan Babu, N. Lambert, Jens Carlsson, G. Schulte

Nature Communications, 2019

Naphthalene Peri Annelated N,N- and N,O-Heterocycles: The Effect of Heteroatom-Guided Peri -Fusion on Their Structure and Reactivity Profiles-A Theoretical Endoscopy

Demeter Tzeli, P. Kozielewicz, M. Zloh, Dyeison Antonow, P. Tsoungas, I. Petsalakis

ChemistrySelect, 2018

Intramolecular single H bonding vs bifurcation in tuning the conformation of 2,2′-dihydroxybenzophenone and its derivatives: a DFT insight

Demeter Tzeli, P. Tsoungas, I. Petsalakis, P. Kozielewicz

Structural Chemistry, 2017

N‐glycosylation and expression in human tissues of the orphan GPR61 receptor

P. Kozielewicz, Hatun A. Alomar, Syaratul Yusof, G. Grafton, A. Cooper, S. Curnow, J. Ironside, H. Pall, N. Barnes

FEBS Open Bio, 2017

2, 2′‐Dihydroxybenzophenones and Derivatives. Efficient Synthesis and Structure Endoscopy by DFT and NMR. Credentials as Potent Antiinflammatory Agents.

Demeter Tzeli, P. Kozielewicz, M. Zervou, C. Potamitis, Katerina Kokkotou, Benedikt Rak, A. Petrou, E. Tsolaki, A. Gavalas, A. Geronikaki, I. Petsalakis, P. Tsoungas

2016

Analysis of impact of cytotoxic and antioxidant activities of the Jerusalem Balsams using chemometric methods

JJ Sajkowska-Kozielewicz, P. Kozielewicz, K. Makarova, I. Wawer, K. Paradowska

Planta Medica, 2016

Antioxidant, Cytotoxic, and Antiproliferative Activities and Total Polyphenol Contents of the Extracts of Geissospermum reticulatum Bark

J. J. Sajkowska-Kozielewicz, P. Kozielewicz, N. Barnes, I. Wawer, K. Paradowska

Oxidative Medicine and Cellular Longevity, 2016

Cytotoxic, anti-radical and reducing properties of ethanol bark extracts of Geissospermum reticulatum

JJ Sajkowska-Kozielewicz, P. Kozielewicz, NM Barnes, I. Wawer, K. Paradowska

Planta Medica, 2016

Novel vitamin D analogues; cytotoxic and anti-proliferative activity against a diffuse large B-cell lymphoma cell line and B-cells from healthy donors

Paweł Kozielewicz, G. Grafton, A. Kutner, S. Curnow, J. Gordon, Nicholas M. Barnes, Paweł Kozielewicz, S. Curnow

Journal of Steroid Biochemistry and Molecular Biology, 2016

Intramolecular cyclization of β-nitroso-o-quinone methides: a theoretical endoscopy of a potentially useful innate ‘reclusive’ reaction

Demeter Tzeli, P. Tsoungas, I. Petsalakis, P. Kozielewicz, M. Zloh

2015

Arene-fused 1,2-oxazole N-oxides and derivatives. The impact of the N–O dipole and substitution on their aromatic character and reactivity profile. Can it be a useful structure in synthesis? A theoretical insight

P. Kozielewicz, Demeter Tzeli, P. Tsoungas, M. Zloh

Structural Chemistry, 2014

Insights into mechanism of anticancer activity of pentacyclic oxindole alkaloids of Uncaria tomentosa by means of a computational reverse virtual screening and molecular docking approach

P. Kozielewicz, K. Paradowska, Slavica Erić, I. Wawer, M. Zloh

Chemical Monthly, 2014

β-Nitroso-o-quinone methides: potent intermediates in organic chemistry and biology. The impact of the NO group on their structure and reactivity profile: a theoretical insight

P. Kozielewicz, P. Tsoungas, Demeter Tzeli, I. Petsalakis, M. Zloh

Structural Chemistry, 2014