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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
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
Ym1 protein crystals promote type 2 immunity
Heyndrickx, I., Deswarte, K., Verstraete, K., Verschueren, K. H. G., Smole, U., Aegerter, H., … Lambrecht, B. N. (2024). Ym1 protein crystals promote type 2 immunity. eLife, 12, RP90676 (17 pp.). https://doi.org/10.7554/eLife.90676
Fragment-based screening targeting an open form of the SARS-CoV-2 main protease binding pocket
Huang, C. Y., Metz, A., Lange, R., Artico, N., Potot, C., Hazemann, J., … Mac Sweeney, A. (2024). Fragment-based screening targeting an open form of the SARS-CoV-2 main protease binding pocket. Acta Crystallographica Section D: Structural Biology, 80, 123-136. https://doi.org/10.1107/S2059798324000329
Structure of <em>Staphylococcus aureus </em>ClpP bound to the covalent active-site inhibitor cystargolide A
Illigmann, A., Vielberg, M. T., Lakemeyer, M., Wolf, F., Dema, T., Stange, P., … Brötz-Oesterhelt, H. (2024). Structure of Staphylococcus aureus ClpP bound to the covalent active-site inhibitor cystargolide A. Angewandte Chemie International Edition, 63(3), e202314028 (10 pp.). https://doi.org/10.1002/anie.202314028
Substrate selectivity and catalytic activation of the type III CRISPR ancillary nuclease Can2
Jungfer, K., Sigg, A., & Jinek, M. (2024). Substrate selectivity and catalytic activation of the type III CRISPR ancillary nuclease Can2. Nucleic Acids Research, 52(1), 462-473. https://doi.org/10.1093/nar/gkad1102
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
RNA oligomers at atomic resolution containing 1-methylpseudouridine, an essential building block of mRNA vaccines
Nievergelt, P., Berliat, F., McAuley, K. E., Dorgan, C. R., van Well, R. M., Thorn, A., & Spingler, B. (2024). RNA oligomers at atomic resolution containing 1-methylpseudouridine, an essential building block of mRNA vaccines. ChemMedChem. https://doi.org/10.1002/cmdc.202300600
Discovery and biochemical characterization of thermostable glycerol oxidases
Santema, L. L., Rotilio, L., Xiang, R., Tjallinks, G., Guallar, V., Mattevi, A., & Fraaije, M. W. (2024). Discovery and biochemical characterization of thermostable glycerol oxidases. Applied Microbiology and Biotechnology, 108, 61 (14 pp.). https://doi.org/10.1007/s00253-023-12883-9
An atlas of protein homo-oligomerization across domains of life
Schweke, H., Pacesa, M., Levin, T., Goverde, C. A., Kumar, P., Duhoo, Y., … Levy, E. D. (2024). An atlas of protein homo-oligomerization across domains of life. Cell, 187(4), 999-1010.e15. https://doi.org/10.1016/j.cell.2024.01.022
An artificial nickel chlorinase based on the biotin-streptavidin technology
Yu, K., Zhang, K., Jakob, R. P., Maier, T., & Ward, T. R. (2024). An artificial nickel chlorinase based on the biotin-streptavidin technology. Chemical Communications, 60(14), 1944-1947. https://doi.org/10.1039/d3cc05847f
Elucidation of the GSK3α structure informs the design of novel, paralog-selective inhibitors
Amaral, B., Capacci, A., Anderson, T., Tezer, C., Bajrami, B., Lulla, M., … Koirala, S. (2023). Elucidation of the GSK3α structure informs the design of novel, paralog-selective inhibitors. ACS Chemical Neuroscience, 14(6), 1080-1094. https://doi.org/10.1021/acschemneuro.2c00476
Targeting the alternative vitamin E metabolite binding site enables noncanonical PPAR<em>γ</em> modulation
Arifi, S., Marschner, J. A., Pollinger, J., Isigkeit, L., Heitel, P., Kaiser, A., … Merk, D. (2023). Targeting the alternative vitamin E metabolite binding site enables noncanonical PPARγ modulation. Journal of the American Chemical Society, 145(27), 14802-14810. https://doi.org/10.1021/jacs.3c03417
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
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
Se-MAG is a convenient additive for experimental phasing and structure determination of membrane proteins crystallised by the lipid cubic phase (in meso) method
Boland, C., Huang, C. Y., Shanker Kaki, S., Wang, M., Olieric, V., & Caffrey, M. (2023). Se-MAG is a convenient additive for experimental phasing and structure determination of membrane proteins crystallised by the lipid cubic phase (in meso) method. Crystals, 13(9), 1402 (20 pp.). https://doi.org/10.3390/cryst13091402
Antibiotic hyper-resistance in a class I aminoacyl-tRNA synthetase with altered active site signature motif
Brkic, A., Leibundgut, M., Jablonska, J., Zanki, V., Car, Z., Petrovic Perokovic, V., … Gruic-Sovulj, I. (2023). Antibiotic hyper-resistance in a class I aminoacyl-tRNA synthetase with altered active site signature motif. Nature Communications, 14(1), 5498 (12 pp.). https://doi.org/10.1038/s41467-023-41244-3
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
 

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