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Development of a series of pyrrolopyridone MAT2A inhibitors
Atkinson, S. J., Bagal, S. K., Argyrou, A., Askin, S., Cheung, T., Chiarparin, E., … Williamson, B. (2024). Development of a series of pyrrolopyridone MAT2A inhibitors. Journal of Medicinal Chemistry, 67(6), 4541-4559. https://doi.org/10.1021/acs.jmedchem.3c01860
PROTACs targeting BRM (SMARCA2) afford selective <em>In vivo</em> degradation over BRG1 (SMARCA4) and are active in BRG1 mutant xenograft tumor models
Berlin, M., Cantley, J., Bookbinder, M., Bortolon, E., Broccatelli, F., Cadelina, G., … Dragovich, P. S. (2024). PROTACs targeting BRM (SMARCA2) afford selective In vivo degradation over BRG1 (SMARCA4) and are active in BRG1 mutant xenograft tumor models. Journal of Medicinal Chemistry, 67, 1262-1313. https://doi.org/10.1021/acs.jmedchem.3c01781
Evolution-inspired engineering of nonribosomal peptide synthetases
Bozhüyük, K. A. J., Präve, L., Kegler, C., Schenk, L., Kaiser, S., Schelhas, C., … Bode, H. B. (2024). Evolution-inspired engineering of nonribosomal peptide synthetases. Science, 383(6689), eadg4320 (11 pp.). https://doi.org/10.1126/science.adg4320
A novel <em>O-</em> and <em>S</em>-methyltransferase from <em>Pleurotus </em>sapidus is involved in flavor formation
Brescia, F. F., Korf, L., Essen, L. O., Zorn, H., & Ruehl, M. (2024). A novel O- and S-methyltransferase from Pleurotus sapidus is involved in flavor formation. Journal of Agricultural and Food Chemistry, 72(12), 6471-6480. https://doi.org/10.1021/acs.jafc.3c08849
Development of potent and selective monoacylglycerol lipase inhibitors. SARs, structural analysis, and biological characterization
Butini, S., Grether, U., Jung, K. M., Ligresti, A., Allarà, M., Postmus, A. G. J., … Campiani, G. (2024). Development of potent and selective monoacylglycerol lipase inhibitors. SARs, structural analysis, and biological characterization. Journal of Medicinal Chemistry, 67(3), 1758-1782. https://doi.org/10.1021/acs.jmedchem.3c01278
Discovery of alternative binding poses through fragment-based identification of DHODH inhibitors
DeRatt, L. G., Pietsch, E. C., Cisar, J. S., Jacoby, E., Kazmi, F., Matico, R., … Kuduk, S. D. (2024). Discovery of alternative binding poses through fragment-based identification of DHODH inhibitors. ACS Medicinal Chemistry Letters, 15(3), 381-387. https://doi.org/10.1021/acsmedchemlett.3c00543
Biochemical and structural characterization of a class A <em>β</em>-lactamase from <em>Nocardia cyriacigeorgica</em>
Feuillard, J., Couston, J., Benito, Y., Hodille, E., Dumitrescu, O., & Blaise, M. (2024). Biochemical and structural characterization of a class A β-lactamase from Nocardia cyriacigeorgica. Acta Crystallographica Section F: Structural Biology and Crystallization Communications, 80, 13-21. https://doi.org/10.1107/S2053230X23010671
Recording physiological history of cells with chemical labeling
Huppertz, M. C., Wilhelm, J., Grenier, V., Schneider, M. W., Falt, T., Porzberg, N., … Johnsson, K. (2024). Recording physiological history of cells with chemical labeling. Science, 383(6685), 890-897. https://doi.org/10.1126/science.adg0812
Synthesis, activity, and their relationships of 2,4-diaminonicotinamide derivatives as EGFR inhibitors targeting C797S mutation
Kageji, H., Momose, T., Nagamoto, Y., Togashi, N., Yasumatsu, I., Nishikawa, Y., … Naito, H. (2024). Synthesis, activity, and their relationships of 2,4-diaminonicotinamide derivatives as EGFR inhibitors targeting C797S mutation. Bioorganic and Medicinal Chemistry Letters, 98, 129575 (7 pp.). https://doi.org/10.1016/j.bmcl.2023.129575
Photosensitization enables Pauson-Khand-type reactions with nitrenes
Li, F., Zhu, W. F., Empel, C., Datsenko, O., Kumar, A., Xu, Y., … Koenigs, R. M. (2024). Photosensitization enables Pauson-Khand-type reactions with nitrenes. Science, 383(6682), 498-503. https://doi.org/10.1126/science.adm8095
Optical control of proteasomal protein degradation with a photoswitchable lipopeptide
Morstein, J., Amatuni, A., Shuster, A., Kuttenlochner, W., Ko, T., Abegg, D., … Trauner, D. H. (2024). Optical control of proteasomal protein degradation with a photoswitchable lipopeptide. Angewandte Chemie International Edition, 63(8), e202314791 (7 pp.). https://doi.org/10.1002/anie.202314791
Enzyme-catalyzed oxidative degradation of ergothioneine
Nalivaiko, E. Y., Vasseur, C. M., & Seebeck, F. P. (2024). Enzyme-catalyzed oxidative degradation of ergothioneine. Angewandte Chemie International Edition, 63(8), e202318445 (8 pp.). https://doi.org/10.1002/anie.202318445
Discovery and characterization of potent spiro-isoxazole-based cereblon ligands with a novel binding mode
Shevalev, R., Bischof, L., Sapegin, A., Bunev, A., Olga, G. 'eva, Kantin, G., … Hartmann, M. D. (2024). Discovery and characterization of potent spiro-isoxazole-based cereblon ligands with a novel binding mode. European Journal of Medicinal Chemistry, 270, 116328 (10 pp.). https://doi.org/10.1016/j.ejmech.2024.116328
Structure-guided elaboration of a fragment-like hit into an orally efficacious leukotriene A4 hydrolase inhibitor
Thoma, G., Miltz, W., Srinivas, H., Penno, C. A., Kiffe, M., Gajewska, M., … Röhn, T. A. (2024). Structure-guided elaboration of a fragment-like hit into an orally efficacious leukotriene A4 hydrolase inhibitor. Journal of Medicinal Chemistry, 67(6), 5093-5108. https://doi.org/10.1021/acs.jmedchem.4c00290