Publications | Lead Discovery Center

2023

Discovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis

Yan S, Schope P C, Lewis J, Putzker K, Uhrig U, Specker E, von Kries J P, Lindemann P, Omran A, Sanchez-Ibarra H E, Unger A, Zischinsky M L, Klebl B, Walther W, Nazare M, Kobelt D and Stein U. Biomed Pharmacother. 2023; 168 115698. doi: 10.1016/j.biopha.2023.115698

Combined Treatment with Host-Directed and Anticytomegaloviral Kinase Inhibitors: Mechanisms, Synergisms and Drug Resistance Barriers

Wild M, Karner D, Eickhoff J, Wagner S, Kicuntod J, Chang W, Barry P, Jonjic S, Lenac Rovis T and Marschall M. Pharmaceutics. 2023; 15 (12): doi: 10.3390/pharmaceutics15122680

Inhibition of mammalian mtDNA transcription paradoxically activates liver fatty acid oxidation to reverse diet-induced hepatosteatosis and obesity

Jiang S, Yuan T, Kremer L S, Rosenberger F A, Hansen F M, Borg M, Rubalcava-Gracia D, Mennuni M, Filograna R, Alsina D, Misic J, Koolmeister C, Ren L, Andersson O, Unger A, Bergbrede T, Lucrezia R D, Wilbom R, Zierath J R, Krook A, Giavalisco P, Mann M and Larsson N-G. BioRxiv. 2023; doi: 10.1101/2023.09.22.558955

ComplexEye: a multi-lens array microscope for high-throughput embedded immune cell migration analysis

Cibir Z, Hassel J, Sonneck J, Kowitz L, Beer A, Kraus A, Hallekamp G, Rosenkranz M, Raffelberg P, Olfen S, Smilowski K, Burkard R, Helfrich I, Tuz A A, Singh V, Ghosh S, Sickmann A, Klebl A K, Eickhoff J E, Klebl B, Seidl K, Chen J, Grabmaier A, Viga R and Gunzer M. Nat Commun. 2023; 14 (1): 8103. doi: 10.1038/s41467-023-43765-3

Protection of pancreatic islets from oxidative cell death by a peripherally-active morphinan with increased drug safety

Scholz O, Huss E, Otter S, Herebian D, Hamacher A, Levy L M, Hristeva S, Sanz M, Ajani H, Puentes A R, Hoffmann T, Hogeback J, Unger A, Terheyden S, Reina do Fundo M, Dewidar B, Roden M and Lammert E. Mol Metab. 2023; 75 101775. doi: 10.1016/j.molmet.2023.101775

Assessment of Covalently Binding Warhead Compounds in the Validation of the Cytomegalovirus Nuclear Egress Complex as an Antiviral Target

Tillmanns J, Hage S, Borst E M, Wardin J, Eickhoff J, Klebl B, Wagner S, Wangen C, Hahn F, Socher E, Marschall M. Cells. 2023; 12 (8): doi: 10.3390/cells12081162

Cytomegalovirus Cyclin-Dependent Kinase Ortholog Vcdk/Pul97 Undergoes Regulatory Interaction with Human Cyclin H and Cdk7 to Codetermine Viral Replication Efficiency

Schutz M, Wangen C, Sommerer M, Kogler M, Eickhoff J, Degenhart C, Klebl B, Naing Z, Egilmezer E, Hamilton S T, Rawlinson W D, Sticht H, Marschall M. Virus Res. 2023; 335 199200. doi: 10.1016/j.virusres.2023.199200

Characterization of the Antibacterial Activity of Quinone-Based Compounds Originating from the Alnumycin Biosynthetic Gene Cluster of a Streptomyces Isolate

Sagurna L, Heinrich S, Kaufmann L S, Ruckert-Reed C, Busche T, Wolf A, Eickhoff J, Klebl B, Kalinowski J, Bandow J E. Antibiotics (Basel). 2023; 12 (7): doi: 10.3390/antibiotics12071116

A Reinvestigation of the Role of the Sorbic Acid Tail on the Antibacterial and Anti-Tuberculosis Properties of Moiramide B

Kollmorgen I, Bachmann N, Dal Molin M, Degenhart C, Zent E, Pareek V, Koch U, Rybniker J, Metzler-Nolte N, Stoll R, Klebl B, Bandow J E, Scherkenbeck J. ChemMedChem. 2023; 18 (11): e202200631. doi: 10.1002/cmdc.202200631

Functional Expression of the Atp-Gated P2x7 Receptor in Human Ipsc-Derived Astrocytes

Kesavan J, Watters O, de Diego-Garcia L, Mendez A M, Alves M, Dinkel K, Hamacher M, Prehn J H M, Henshall D C, Engel T. Purinergic Signal. 2023; doi: 10.1007/s11302-023-09957-8

Inhibiting the Glycerophosphodiesterase Edi3 in Er-Her2+ Breast Cancer Cells Resistant to Her2-Targeted Therapy Reduces Viability and Tumour Growth

Keller M, Rohlf K, Glotzbach A, Leonhardt G, Luke S, Derksen K, Demirci O, Gocener D, AlWahsh M, Lambert J, Lindskog C, Schmidt M, Brenner W, Baumann M, Zent E, Zischinsky M L, Hellwig B, Madjar K, Rahnenfuhrer J, Overbeck N, Reinders J, Cadenas C, Hengstler J G, Edlund K, Marchan R. J Exp Clin Cancer Res. 2023; 42 (1): 25. doi: 10.1186/s13046-022-02578-w

Ifn-α Primes Cancer Cells for Fusicoccin-Induced Cell Death Via 14-3-3 Ppi Stabilization

Andlovic B, Heilmann G, Ninck S, Andrei S A, Centorrino F, Higuchi Y, Kato N, Brunsveld L, Arkin M, Menninger S, Choidas A, Wolf A, Klebl B, Kaschani F, Kaiser M, Eickhoff J, Ottmann C. Cell Chem Biol. 2023; 30 (6): 573-590 e576. doi: 10.1016/j.chembiol.2023.04.005

Negishi Cross‐Coupling in the Preparation of Benzyl Substituted Pyrrolo[2,3‐D]Pyrimidine Based Csf1r Inhibitors

Aarjus T I, Teksum V, Unger A, Habenberger P, Wolf A, Eickhoff J, Klebl B, Wolowczyk C, Bjorkoy G, Sundby E, Hoff B H. European Journal of Organic Chemistry. 2023; 26 (12): 93-104. doi: 10.1002/ejoc.202300052

A Highly Selective Purine-Based Inhibitor of Csf1r Potently Inhibits Osteoclast Differentiation

Aarhus T I, Eickhoff J, Klebl B, Unger A, Boros J, Choidas A, Zischinsky M L, Wolowczyk C, Bjorkoy G, Sundby E, Hoff B H. Eur J Med Chem. 2023b; 255 115344. doi: 10.1016/j.ejmech.2023.115344

Synthesis and Development of Highly Selective Pyrrolo[2,3-d]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form

Aarhus TI, Bjornstad F, Wolowczyk C, Larsen KU, Rognstad L., Leithaug T., Unger A., Habenberger P, Wolf A, Bjorkoy G, Pridans C, Eickhoff J, Klebl B, Hoff BH, Sundby E. J Med Chem. 2023 May 25; 66(10), 6959-6980. doi: 10.1021/acs.jmedchem.3c00428.

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