Active Filters

  • (-) Beamlines = PXII
Search Results 1 - 20 of 1,203

Pages

  • RSS Feed
Select Page
Optimizing the growth of endothiapepsin crystals for serial crystallography experiments
Beale, J. H., & Marsh, M. E. (2021). Optimizing the growth of endothiapepsin crystals for serial crystallography experiments. Journal of Visualized Experiments, 168, e61896 (30 pp.). https://doi.org/10.3791/61896
Structure-based approaches to improving selectivity through utilizing explicit water molecules: discovery of selective <em>β</em>-secretase (BACE1) inhibitors over BACE2
Fujimoto, K., Yoshida, S., Tadano, G., Asada, N., Fuchino, K., Suzuki, S., … Kusakabe, Kichi. (2021). Structure-based approaches to improving selectivity through utilizing explicit water molecules: discovery of selective β-secretase (BACE1) inhibitors over BACE2. Journal of Medicinal Chemistry, 64(6), 3075-3085. https://doi.org/10.1021/acs.jmedchem.0c01858
Structure based design of bicyclic Peptide inhibitors of RbAp48
Hart, P. 't., Hommen, P., Noisier, A., Krzyzanowski, A., Schüler, D., Porfetye, A. T., … Waldmann, H. (2021). Structure based design of bicyclic Peptide inhibitors of RbAp48. Angewandte Chemie International Edition, 60(4), 1813-1820. https://doi.org/10.1002/anie.202009749
Insulin binding to the analytical antibody sandwich pair OXI‐005 and HUI‐018: epitope mapping and binding properties
Johansson, E., Wu, X., Yu, B., Yang, Z., Cao, Z., Wiberg, C., … Poulsen, F. (2021). Insulin binding to the analytical antibody sandwich pair OXI‐005 and HUI‐018: epitope mapping and binding properties. Protein Science, 30(2), 485-496. https://doi.org/10.1002/pro.4009
Discovery of LYS006, a potent and highly selective inhibitor of leukotriene A&lt;sub&gt;4&lt;/sub&gt; hydrolase
Markert, C., Thoma, G., Srinivas, H., Bollbuck, B., Lüönd, R. M., Miltz, W., … Röhn, T. A. (2021). Discovery of LYS006, a potent and highly selective inhibitor of leukotriene A4 hydrolase. Journal of Medicinal Chemistry, 64(4), 1889-1903. https://doi.org/10.1021/acs.jmedchem.0c01955
One atom makes all the difference: Getting a foot in the door between SOS1 and KRAS
Ramharter, J., Kessler, D., Ettmayer, P., Hofmann, M. H., Gerstberger, T., Gmachl, M., … McConnell, D. B. (2021). One atom makes all the difference: Getting a foot in the door between SOS1 and KRAS. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.0c01949
Azole-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
Röhrig, U. F., Majjigapu, S. R., Reynaud, A., Pojer, F., Dilek, N., Reichenbach, P., … Zoete, V. (2021). Azole-based indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors. Journal of Medicinal Chemistry, 64(4), 2205-2227. https://doi.org/10.1021/acs.jmedchem.0c01968
BET bromodomain inhibitors regulate keratinocyte plasticity
Schutzius, G., Kolter, C., Bergling, S., Tortelli, F., Fuchs, F., Renner, S., … Kirkland, S. (2021). BET bromodomain inhibitors regulate keratinocyte plasticity. Nature Chemical Biology, 17, 280-290. https://doi.org/10.1038/s41589-020-00716-z
Functional and structural characterization of PII-like protein CutA does not support involvement in heavy metal tolerance and hints at a small-molecule carrying/signaling role
Selim, K. A., Tremiño, L., Marco-Marín, C., Alva, V., Espinosa, J., Contreras, A., … Rubio, V. (2021). Functional and structural characterization of PII-like protein CutA does not support involvement in heavy metal tolerance and hints at a small-molecule carrying/signaling role. FEBS Journal, 288(4), 1142-1162. https://doi.org/10.1111/febs.15464
Development of autotaxin inhibitors: a series of tetrazole cinnamides
Thomson, C. G., Le Grand, D., Dowling, M., Beattie, D., Elphick, L., Faller, M., … Zink, F. (2021). Development of autotaxin inhibitors: a series of tetrazole cinnamides. Bioorganic and Medicinal Chemistry Letters, 31, 127663 (7 pp.). https://doi.org/10.1016/j.bmcl.2020.127663
Discovery of diaminopyrimidine carboxamide HPK1 inhibitors as preclinical immunotherapy tool compounds
Vara, B. A., Levi, S. M., Achab, A., Candito, D. A., Fradera, X., Lesburg, C. A., … Pasternak, A. (2021). Discovery of diaminopyrimidine carboxamide HPK1 inhibitors as preclinical immunotherapy tool compounds. ACS Medicinal Chemistry Letters, 12(4), 653-661. https://doi.org/10.1021/acsmedchemlett.1c00096
Identification of potent reverse indazole inhibitors for HPK1
Yu, E. C., Methot, J. L., Fradera, X., Lesburg, C. A., Lacey, B. M., Siliphaivanh, P., … Pasternak, A. (2021). Identification of potent reverse indazole inhibitors for HPK1. ACS Medicinal Chemistry Letters, 12(3), 459-466. https://doi.org/10.1021/acsmedchemlett.0c00672
Alternative catalytic residues in the active site of Esco acetyltransferases
Ajam, T., De, I., Petkau, N., Whelan, G., Pena, V., & Eichele, G. (2020). Alternative catalytic residues in the active site of Esco acetyltransferases. Scientific Reports, 10(1), 9828 (13 pp.). https://doi.org/10.1038/s41598-020-66795-z
Discovery of LOU064 (remibrutinib), a potent and highly selective covalent inhibitor of Bruton&#039;s tyrosine kinase
Angst, D., Gessier, F., Janser, P., Vulpetti, A., Wälchli, R., Beerli, C., … Cenni, B. (2020). Discovery of LOU064 (remibrutinib), a potent and highly selective covalent inhibitor of Bruton's tyrosine kinase. Journal of Medicinal Chemistry, 63(10), 5102-5118. https://doi.org/10.1021/acs.jmedchem.9b01916
Identification of FAM181A and FAM181B as new interactors with the TEAD transcription factors
Bokhovchuk, F., Mesrouze, Y., Delaunay, C., Martin, T., Villard, F., Meyerhofer, M., … Chène, P. (2020). Identification of FAM181A and FAM181B as new interactors with the TEAD transcription factors. Protein Science, 29(2), 509-520. https://doi.org/10.1002/pro.3775
Fragment-based discovery of pyrazolopyridones as JAK1 inhibitors with excellent subtype selectivity
Borreschmidt Hansen, B., Jepsen, T. H., Larsen, M., Sindet, R., Vifian, T., Nørreskov Burhardt, M., … Ritzén, A. (2020). Fragment-based discovery of pyrazolopyridones as JAK1 inhibitors with excellent subtype selectivity. Journal of Medicinal Chemistry, 63(3), 7008-7032. https://doi.org/10.1021/acs.jmedchem.0c00359
Discovery of novel imidazopyridine GSK-3β inhibitors supported by cmputational approaches
Buonfiglio, R., Prati, F., Bischetti, M., Cavarischia, C., Furlotti, G., & Ombrato, R. (2020). Discovery of novel imidazopyridine GSK-3β inhibitors supported by cmputational approaches. Molecules, 25(9), 2163 (29 pp.). https://doi.org/10.3390/molecules25092163
&lt;em&gt;In situ&lt;/em&gt; crystallography as an emerging method for structure solution of membrane proteins: the case of CCR2A
Cheng, R., Huang, C. Y., Hennig, M., Nar, H., & Schnapp, G. (2020). In situ crystallography as an emerging method for structure solution of membrane proteins: the case of CCR2A. FEBS Journal, 287(5), 866-873. https://doi.org/10.1111/febs.15098
Novel autotaxin inhibitor for the treatment of idiopathic pulmonary fibrosis: a clinical candidate discovered using DNA-encoded chemistry
Cuozzo, J. W., Clark, M. A., Keefe, A. D., Kohlmann, A., Mulvihill, M., Ni, H., … Zhang, Y. (2020). Novel autotaxin inhibitor for the treatment of idiopathic pulmonary fibrosis: a clinical candidate discovered using DNA-encoded chemistry. Journal of Medicinal Chemistry, 63(14), 7840-7856. https://doi.org/10.1021/acs.jmedchem.0c00688
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar
DeRatt, L. G., Pietsch, E. C., Tanner, A., Shaffer, P., Jacoby, E., Wang, W., … Kuduk, S. D. (2020). A carboxylic acid isostere screen of the DHODH inhibitor Brequinar. Bioorganic and Medicinal Chemistry Letters, 30(22), 127589 (5 pp.). https://doi.org/10.1016/j.bmcl.2020.127589
 

Pages