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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
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
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
Structure-based optimization and biological evaluation of potent and selective MMP-7 inhibitors for kidney fibrosis
Abe-Sato, K., Tabuse, H., Kanazawa, H., Kamitani, M., Endo, M., Tokura, S., … Oka, Y. (2023). Structure-based optimization and biological evaluation of potent and selective MMP-7 inhibitors for kidney fibrosis. Journal of Medicinal Chemistry, 66(21), 14653-14668. https://doi.org/10.1021/acs.jmedchem.3c01166
Discovery of the TLR7/8 antagonist MHV370 for treatment of systemic autoimmune diseases
Alper, P., Betschart, C., André, C., Boulay, T., Cheng, D., Deane, J., … Michellys, P. Y. (2023). Discovery of the TLR7/8 antagonist MHV370 for treatment of systemic autoimmune diseases. ACS Medicinal Chemistry Letters, 14(8), 1054-1062. https://doi.org/10.1021/acsmedchemlett.3c00136
Lipid exchange in crystal-confined fatty acid binding proteins: X-ray evidence and molecular dynamics explanation
Alvarez, H. A., Cousido-Siah, A., Espinosa, Y. R., Podjarny, A., Carlevaro, C. M., & Howard, E. (2023). Lipid exchange in crystal-confined fatty acid binding proteins: X-ray evidence and molecular dynamics explanation. Proteins, 91(11), 1525-1534. https://doi.org/10.1002/prot.26546
Fragment-based discovery of novel VE-PTP inhibitors using orthogonal biophysical techniques
Asano, W., Yamanaka, K., Ohara, Y., Uhara, T., Doi, S., Orita, T., … Hantani, Y. (2023). Fragment-based discovery of novel VE-PTP inhibitors using orthogonal biophysical techniques. Biochemistry, 62(14), 2161-2169. https://doi.org/10.1021/acs.biochem.3c00079
Light-driven C–O coupling of carboxylic acids and alkyl halides over a Ni single-atom catalyst
Bajada, M. A., Di Liberto, G., Tosoni, S., Ruta, V., Mino, L., Allasia, N., … Vilé, G. (2023). Light-driven C–O coupling of carboxylic acids and alkyl halides over a Ni single-atom catalyst. Nature Synthesis, 2, 1092-1103. https://doi.org/10.1038/s44160-023-00341-3
Development of a potent cyclic peptide inhibitor of the nNOS/PSD-95 interaction
Balboa, J. R., Essig, D. J., Ma, S., Karer, N., Clemmensen, L. S., Pedersen, S. W., … Strømgaard, K. (2023). Development of a potent cyclic peptide inhibitor of the nNOS/PSD-95 interaction. Journal of Medicinal Chemistry, 66(1), 976-990. https://doi.org/10.1021/acs.jmedchem.2c01803
Synthesis of thieno[2,3-<em>c</em>]pyridine derived GRK2 inhibitors
Balo, T., Sapi, A., Kiss, A., Raimbaud, E., Paysant, J., Cattin, M. E., … Faucher, N. (2023). Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors. Monatshefte für Chemie, 154, 1339-1357. https://doi.org/10.1007/s00706-021-02889-2
Identification of M4205 - a highly selective inhibitor of KIT mutations for treatment of unresectable metastatic or recurrent gastrointestinal stromal tumors
Blum, A., Dorsch, D., Linde, N., Brandstetter, S., Buchstaller, H. P., Busch, M., … Esdar, C. (2023). Identification of M4205 - a highly selective inhibitor of KIT mutations for treatment of unresectable metastatic or recurrent gastrointestinal stromal tumors. Journal of Medicinal Chemistry, 66(4), 2386-2395. https://doi.org/10.1021/acs.jmedchem.2c00851
Discovery of cycloalkyl[<em>c</em>]thiophenes as novel scaffolds for hypoxia-inducible factor-2<em>α</em> inhibitors
Buchstaller, H. P., Sala-Hojman, A., Leiendecker, M., Albers, J., Anlauf, U., Berges, N., … Zarębski, A. (2023). Discovery of cycloalkyl[c]thiophenes as novel scaffolds for hypoxia-inducible factor-2α inhibitors. Journal of Medicinal Chemistry, 66(13), 8666-8686. https://doi.org/10.1021/acs.jmedchem.3c00332
Oxygen-induced chromophore degradation in the photoswitchable red fluorescent protein rsCherry
Bui, T. Y. H., De Zitter, E., Moeyaert, B., Pecqueur, L., Srinivasu, B. Y., Economou, A., … Pedre, B. (2023). Oxygen-induced chromophore degradation in the photoswitchable red fluorescent protein rsCherry. International Journal of Biological Macromolecules, 239, 124179 (9 pp.). https://doi.org/10.1016/j.ijbiomac.2023.124179
Structural and functional characterization of the ureidoacrylate amidohydrolase RutB from <em>Escherichia coli</em>
Busch, M. R., Rajendran, C., & Sterner, R. (2023). Structural and functional characterization of the ureidoacrylate amidohydrolase RutB from Escherichia coli. Biochemistry, 62(3), 863-872. https://doi.org/10.1021/acs.biochem.2c00640
FRAGTORY: pharmacophore-focused design, synthesis, and evaluation of an sp<sup>3</sup>-enriched fragment library
Bührmann, M., Kallepu, S., Warmuth, J. D., Wiese, J. N., Ehrt, C., Vatheuer, H., … Rauh, D. (2023). FRAGTORY: pharmacophore-focused design, synthesis, and evaluation of an sp3-enriched fragment library. Journal of Medicinal Chemistry, 66(9), 6297-6314. https://doi.org/10.1021/acs.jmedchem.3c00187
 

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