We are developing enzyme inhibitors to be used as tool compounds as well as potential lead compounds for drug development.

Current targets include:

Rearranged during Transfection (RET), a transmembrane tyrosine-protein kinase

Collaborators include Andréasson, Lundbäck and CBCS.

Design and Development of Photoswitchable DFG-Out RET Kinase Inhibitors. Yongjin Xu, Chunxia Gao, Måns Andreasson, Liliana Håversen, Marta Carrasco,  Cassandra Fleming, Thomas Lundbäck,  Joakim Andréasson and Morten Grøtli. Eur. J. Med. Chem. 2022, 234, 114226.

Design and Development of a Photoswitchable DFG-Out Kinase Inhibitor. Yongjin Xu, Chunxia Gao, Liliana Håversen, Thomas Lundbäck, Joakim Andréasson and Morten Grøtli. Chem. Commun. 2021, 57, 10043.

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Lymphocyte-specific protein tyrosine kinase (LCK), a non-receptor tyrosine-protein kinase

Collaborators include Andréasson, Lundbäck and CBCS.

A Fluorescent LCK Inhibitor that Exhibits Diagnostic Changes in Emission Upon Binding the Kinase Enzyme, Cassandra Lee Fleming, Patrick A Sandoz, Tord Inghardt, Björn Önfelt, Morten Grøtli, Joakim Andreasson. Angew. Chem. Int. Ed.,  2019, 58, 15000 –15004.

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Pyruvate kinase liver isoform (PKL)

Collaborators include Mardinoglu, Boren and Hyvonen.

Anthraquinone derivatives as ADP-competitive inhibitors of liver pyruvate kinase. Amalyn Nain-Perez, Anders Foller Füchtbauer, Liliana Håversen, Aleksei Lulla, Chunxia Gao, Josipa Matic, Leticia Monjas, Alexandra Rodríguez, Paul Brear, Woonghee Kim, Marko Hyvönen, Jan Borén, Adil Mardinoglu, Mathias Uhlen and Morten Grøtli. Eur. J. Med. Chem. 2022, 234, 114270.

Tuning liver pyruvate kinase activity up or down with a new class of allosteric modulators. Amalyn Nain-Perez, Oscar Nilsson, Aleksei Lulla, Liliana Håversen, Paul Brear, Sara Liljenberg, Marko Hyvönen, Jan Borén and Morten Grøtli. Eur. J. Med. Chem. 2023, 250, 115177.

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N-myristoyltransferase (NMT), a glycylpeptide N-tetradecanoyltransferase

Collaborators include Staker,  Kaushansky and Sunnerhagen. 

Identification of potent and Selective N-myristoyltransferase inhibitors of Plasmodium vivax liver stage hypnozoites and schizonts. Diego Rodríguez-Hernández, Kamalakannan Vijayan, Rachael Zigweid, Michael K. Fenwick, Banumathi Sankaran, Wanlapa Roobsoong, Jetsumon Sattabongkot, Elizabeth K.K. Glennon, Peter J. Myler, Per Sunnerhagen, Bart L. Staker, Alexis Kaushansky, Morten Grøtli. Nat. Commun. 2023, 14, 5408.

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Aminoacyl-tRNA synthetases (AARSs), a group of cytoplasmic enzymes that catalyse the binding of tRNA to their respective amino acids

Collaborators include Torres-Larios.

Structural Insights into the Polyphyletic Origins of Glycyl tRNA Synthetases, Marco Igor Valencia-Sánchez, Annia Rodríguez-Hernández, Ruben Ferreira, Hugo Aníbal Santamaría-Suárez, Marcelino Arciniega-Castro, Anne-Catherine Dock-Bregeon, Dino Moras, Brice Beinsteiner, Haydyn Mertens, Dmitri Svergun, Luis Brieba de Castro, Morten Grøtli, Alfredo Torres-Larios, J. Biol. Chem. 2016, 291, 14430–14446.

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Bruton’s tyrosine kinase (BTK), a non-receptor tyrosine kinase.

Collaborators include Malmerberg and Janic.