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1,5-Disubstituted 1,2,3-triazoles as amide bond isosteres yield novel tumor-targeting minigastrin analogs
Grob, N. M., Schibli, R., Béhé, M., Valverde, I. E., & Mindt, T. L. (2021). 1,5-Disubstituted 1,2,3-triazoles as amide bond isosteres yield novel tumor-targeting minigastrin analogs. ACS Medicinal Chemistry Letters, 12(4), 585-592. https://doi.org/10.1021/acsmedchemlett.0c00636
Fibronectin fibers are highly tensed in healthy organs in contrast to tumors and virus-infected lymph nodes
Fonta, C. M., Arnoldini, S., Jaramillo, D., Moscaroli, A., Oxenius, A., Behe, M., & Vogel, V. (2020). Fibronectin fibers are highly tensed in healthy organs in contrast to tumors and virus-infected lymph nodes. Matrix Biology Plus, 8, 100046 (15 pp.). https://doi.org/10.1016/j.mbplus.2020.100046
Particle therapy in Europe
Grau, C., Durante, M., Georg, D., Langendijk, J. A., & Weber, D. C. (2020). Particle therapy in Europe. Molecular Oncology, 14(7), 1492-1499. https://doi.org/10.1002/1878-0261.12677
Complex crystal structures of EGFR with third-generation kinase inhibitors and simultaneously bound allosteric ligands
Niggenaber, J., Heyden, L., Grabe, T., Muller, M. P., Lategahn, J., & Rauh, D. (2020). Complex crystal structures of EGFR with third-generation kinase inhibitors and simultaneously bound allosteric ligands. ACS Medicinal Chemistry Letters, 11(12), 2484-2490. https://doi.org/10.1021/acsmedchemlett.0c00472
Proton therapy and the European Particle Therapy Network: the past, present and future
Weber, D. C., Langendijk, J. A., Grau, C., & Thariat, J. (2020). Proton therapy and the European Particle Therapy Network: the past, present and future. Cancer/Radiothérapie, 24(6-7), 687-690. https://doi.org/10.1016/j.canrad.2020.05.002
Lead optimization and biological evaluation of fragment-based cN-II inhibitors
Guillon, R., Rahimova, R., Preeti, P., Egron, D., Rouanet, S., Dumontet, C., … Peyrottes, S. (2019). Lead optimization and biological evaluation of fragment-based cN-II inhibitors. European Journal of Medicinal Chemistry, 168, 28-44. https://doi.org/10.1016/j.ejmech.2019.02.040
Structural insights into interaction mechanisms of alternative piperazine-urea YEATS domain binders in MLLT1
Ni, X., Heidenreich, D., Christott, T., Bennett, J., Moustakim, M., Brennan, P. E., … Chaikuad, A. (2019). Structural insights into interaction mechanisms of alternative piperazine-urea YEATS domain binders in MLLT1. ACS Medicinal Chemistry Letters, 10(12), 1661-1666. https://doi.org/10.1021/acsmedchemlett.9b00460
A novel biphenyl-based chemotype of retinoid X receptor ligands enables subtype and heterodimer preferences
Pollinger, J., Schierle, S., Gellrich, L., Ohrndorf, J., Kaiser, A., Heitel, P., … Merk, D. (2019). A novel biphenyl-based chemotype of retinoid X receptor ligands enables subtype and heterodimer preferences. ACS Medicinal Chemistry Letters, 10(9), 1346-1352. https://doi.org/10.1021/acsmedchemlett.9b00306
Covalent-allosteric inhibitors to achieve Akt isoform-selectivity
Quambusch, L., Landel, I., Depta, L., Weisner, J., Uhlenbrock, N., Müller, M. P., … Rauh, D. (2019). Covalent-allosteric inhibitors to achieve Akt isoform-selectivity. Angewandte Chemie International Edition, 58(52), 18823-18829. https://doi.org/10.1002/anie.201909857
Development of alkyl glycerone phosphate synthase inhibitors: structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells
Stazi, G., Battistelli, C., Piano, V., Mazzone, R., Marrocco, B., Marchese, S., … Valente, S. (2019). Development of alkyl glycerone phosphate synthase inhibitors: structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells. European Journal of Medicinal Chemistry, 163, 722-735. https://doi.org/10.1016/j.ejmech.2018.11.050
Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form
Nelp, M. T., Kates, P. A., Hunt, J. T., Newitt, J. A., Balog, A., Maley, D., … Groves, J. T. (2018). Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form. Proceedings of the National Academy of Sciences of the United States of America PNAS, 115(13), 3249-3254. https://doi.org/10.1073/pnas.1719190115
Binding motifs in the CBP bromodomain: an analysis of 20 crystal structures of complexes with small molecules
Zhu, J., Dong, J., Batiste, L., Unzue, A., Dolbois, A., Pascanu, V., … Caflisch, A. (2018). Binding motifs in the CBP bromodomain: an analysis of 20 crystal structures of complexes with small molecules. ACS Medicinal Chemistry Letters, 9(9), 929-934. https://doi.org/10.1021/acsmedchemlett.8b00286
Antivascular and antitumor properties of the tubulin-binding chalcone TUB091
Canela, M. D., Noppen, S., Bueno, O., Prota, A. E., Bargsten, K., Sáez-Calvo, G., … Liekens, S. (2017). Antivascular and antitumor properties of the tubulin-binding chalcone TUB091. Oncotarget, 8(9), 14325-14342. https://doi.org/10.18632/oncotarget.9527
Optimized 4,5-diarylimidazoles as potent/selective inhibitors of Protein Kinase CK1δ and their structural relation to P38α MAPK
Halekotte, J., Witt, L., Ianes, C., Krüger, M., Bührmann, M., Rauh, D., … Laufer, S. (2017). Optimized 4,5-diarylimidazoles as potent/selective inhibitors of Protein Kinase CK1δ and their structural relation to P38α MAPK. Molecules, 22(4), 522. https://doi.org/10.3390/molecules22040522
Myosin-1E interacts with FAK proline-rich region 1 to induce fibronectin-type matrix
Heim, J. B., Squirewell, E. J., Neu, A., Zocher, G., Sominidi-Damodaran, S., Wyles, S. P., … Meves, A. (2017). Myosin-1E interacts with FAK proline-rich region 1 to induce fibronectin-type matrix. Proceedings of the National Academy of Sciences of the United States of America PNAS, 114(15), 3933-3938. https://doi.org/10.1073/pnas.1614894114
Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6
Kerres, N., Steurer, S., Schlager, S., Bader, G., Berger, H., Caligiuri, M., … Koegl, M. (2017). Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6. Cell Reports, 20(12), 2860-2875. https://doi.org/10.1016/j.celrep.2017.08.081
Catalytic competence, structure and stability of the cancer-associated R139W variant of the human NAD(P)H:quinone oxidoreductase 1 (NQO1)
Lienhart, W. D., Strandback, E., Gudipati, V., Koch, K., Binter, A., Uhl, M. K., … Macheroux, P. (2017). Catalytic competence, structure and stability of the cancer-associated R139W variant of the human NAD(P)H:quinone oxidoreductase 1 (NQO1). FEBS Journal, 284(8), 1233-1245. https://doi.org/10.1111/febs.14051
Structural basis for the inhibition of AKR1B10 by the C3 brominated TTNPB derivative UVI2008
Ruiz, F. X., Crespo, I., Álvarez, S., Porté, S., Giménez-Dejoz, J., Cousido-Siah, A., … Farrés, J. (2017). Structural basis for the inhibition of AKR1B10 by the C3 brominated TTNPB derivative UVI2008. Chemico-Biological Interactions, 276, 174-181. https://doi.org/10.1016/j.cbi.2017.01.026
Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR
Engel, J., Becker, C., Lategahn, J., Keul, M., Ketzer, J., Mühlenberg, T., … Rauh, D. (2016). Insight into the Inhibition of Drug-Resistant Mutants of the Receptor Tyrosine Kinase EGFR. Angewandte Chemie International Edition, 55(36), 10909-10912. https://doi.org/10.1002/anie.201605011
Insights into the structure-activity relationships of chiral 1,2-diaminophenylalkane platinum(II) anticancer derivatives
Berger, G., Fusaro, L., Luhmer, M., Czapla-Masztafiak, J., Lipiec, E., Szlachetko, J., … Bombard, S. (2015). Insights into the structure-activity relationships of chiral 1,2-diaminophenylalkane platinum(II) anticancer derivatives. Journal of Biological Inorganic Chemistry, 20(5), 841-853. https://doi.org/10.1007/s00775-015-1270-6