Publications

 

Recent publications are listed below. For an extensive overview we kindly refer you to our publication repository DORA

  • Abel AC, Mühlethaler T, Dessin C, Schachtsiek T, Sammet B, Sharpe T, et al.
    Bridging the maytansine and vinca sites: Cryptophycins target β-tubulin's T5-loop
    Journal of Biological Chemistry. 2024; 300(6): 107363 (10 pp.). https://doi.org/10.1016/j.jbc.2024.107363
    DORA PSI
  • Aksu M, Kumar P, Güttler T, Taxer W, Gregor K, Mußil B, et al.
    Nanobodies to multiple spike variants and inhalation of nanobody-containing aerosols neutralize SARS-CoV-2 in cell culture and hamsters
    Antiviral Research. 2024; 221: 105778 (21 pp.). https://doi.org/10.1016/j.antiviral.2023.105778
    DORA PSI
  • Baltgalvis KA, Lamb KN, Symons KT, Wu CC, Hoffman MA, Snead AN, et al.
    Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase
    Nature. 2024; 629(8011): 435-442. https://doi.org/10.1038/s41586-024-07318-y
    DORA PSI
  • Butini S, Grether U, Jung KM, Ligresti A, Allarà M, Postmus AGJ, et al.
    Development of potent and selective monoacylglycerol lipase inhibitors. SARs, structural analysis, and biological characterization
    Journal of Medicinal Chemistry. 2024; 67(3): 1758-1782. https://doi.org/10.1021/acs.jmedchem.3c01278
    DORA PSI
  • Carney DW, Leffler AE, Bell JA, Chandrasinghe AS, Cheng C, Chang E, et al.
    Exploiting high-energy hydration sites for the discovery of potent peptide aldehyde inhibitors of the SARS-CoV-2 main protease with cellular antiviral activity
    Bioorganic and Medicinal Chemistry. 2024; 103: 117577 (27 pp.). https://doi.org/10.1016/j.bmc.2023.117577
    DORA PSI
  • DeRatt LG, Pietsch EC, Cisar JS, Jacoby E, Kazmi F, Matico R, et al.
    Discovery of alternative binding poses through fragment-based identification of DHODH inhibitors
    ACS Medicinal Chemistry Letters. 2024; 15(3): 381-387. https://doi.org/10.1021/acsmedchemlett.3c00543
    DORA PSI
  • Ferretti S, Hamon J, de Kanter R, Scheufler C, Andraos-Rey R, Barbe S, et al.
    Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers
    Nature. 2024; 629(8011): 443-449. https://doi.org/10.1038/s41586-024-07350-y
    DORA PSI
  • Gehl M, Demmer U, Ermler U, Shima S
    Mutational and structural studies of (βα)8-barrel fold methylene-tetrahydropterin reductases utilizing a common catalytic mechanism
    Protein Science. 2024; 33(6): e5018 (18 pp.). https://doi.org/10.1002/pro.5018
    DORA PSI
  • Huppertz M-C, Wilhelm J, Grenier V, Schneider MW, Falt T, Porzberg N, et al.
    Recording physiological history of cells with chemical labeling
    Science. 2024; 383(6685): 890-897. https://doi.org/10.1126/science.adg0812
    DORA PSI
  • Kageji H, Momose T, Nagamoto Y, Togashi N, Yasumatsu I, Nishikawa Y, et al.
    Synthesis, activity, and their relationships of 2,4-diaminonicotinamide derivatives as EGFR inhibitors targeting C797S mutation
    Bioorganic and Medicinal Chemistry Letters. 2024; 98: 129575 (7 pp.). https://doi.org/10.1016/j.bmcl.2023.129575
    DORA PSI
  • Kawano S, Kawada MI, Fukushima S, Arai Y, Shibata T, Miyano SW
    Antitumor activity of Tasurgratinib as an orally available FGFR1-3 inhibitor in Cholangiocarcinoma models with FGFR2-fusion
    Anticancer research. 2024; 44(6): 2393-2406. https://doi.org/10.21873/anticanres.17046
    DORA PSI
  • Kotschy J, Söldner B, Singh H, Vasa SK, Linser R
    Microsecond timescale conformational dynamics of a small-molecule ligand within the active site of a protein
    Angewandte Chemie International Edition. 2024; 63(5): e202313947 (6 pp.). https://doi.org/10.1002/anie.202313947
    DORA PSI
  • Kozicka Z, Suchyta DJ, Focht V, Kempf G, Petzold G, Jentzsch M, et al.
    Design principles for cyclin K molecular glue degraders
    Nature Chemical Biology. 2024; 20(1): 93-102. https://doi.org/10.1038/s41589-023-01409-z
    DORA PSI
  • Langer LM, Kurscheidt K, Basquin J, Bonneau F, Iermak I, Basquin C, et al.
    UPF1 helicase orchestrates mutually exclusive interactions with the SMG6 endonuclease and UPF2
    Nucleic Acids Research. 2024; 52(10): 6036-6048. https://doi.org/10.1093/nar/gkae323
    DORA PSI
  • McCarver S, Hanna L, Samant A, Thompson AA, Seierstad M, Saha A, et al.
    Structure-based optimization of selective and brain penetrant CK1δ inhibitors for the treatment of circadian disruptions
    ACS Medicinal Chemistry Letters. 2024; 15(4): 486-492. https://doi.org/10.1021/acsmedchemlett.3c00523
    DORA PSI
  • Meibom D, Wasnaire P, Beyer K, Broehl A, Cancho-Grande Y, Elowe N, et al.
    BAY-9835: discovery of the first orally bioavailable ADAMTS7 inhibitor
    Journal of Medicinal Chemistry. 2024; 67(4): 2907-2940. https://doi.org/10.1021/acs.jmedchem.3c02036
    DORA PSI
  • Porfetye AT, Stege P, Rebollido-Rios R, Hoffmann D, Schrader T, Vetter IR
    How Do molecular tweezers bind to proteins? Lessons from X-ray crystallography
    Molecules. 2024; 29(8): 1764. https://doi.org/10.3390/molecules29081764
    DORA PSI
  • Schmidt M, Grethe C, Recknagel S, Kipka GM, Klink N, Gersch M
    N-cyanopiperazines as specific covalent inhibitors of the deubiquitinating enzyme UCHL1
    Angewandte Chemie International Edition. 2024; 63(12): e202318849 (10 pp.). https://doi.org/10.1002/anie.202318849
    DORA PSI
  • Shevalev R, Bischof L, Sapegin A, Bunev A, Olga G'eva, Kantin G, et al.
    Discovery and characterization of potent spiro-isoxazole-based cereblon ligands with a novel binding mode
    European Journal of Medicinal Chemistry. 2024; 270: 116328 (10 pp.). https://doi.org/10.1016/j.ejmech.2024.116328
    DORA PSI
  • Solà Colom M, Fu Z, Gunkel P, Güttler T, Trakhanov S, Srinivasan V, et al.
    A checkpoint function for Nup98 in nuclear pore formation suggested by novel inhibitory nanobodies
    EMBO Journal. 2024; 43(11): 2198-2232. https://doi.org/10.1038/s44318-024-00081-w
    DORA PSI
  • Teuber A, Schulz T, Fletcher BS, Gontla R, Mühlenberg T, Zischinsky M-L, et al.
    Avapritinib-based SAR studies unveil a binding pocket in KIT and PDGFRA
    Nature Communications. 2024; 15(1): 63 (11 pp.). https://doi.org/10.1038/s41467-023-44376-8
    DORA PSI
  • Thoma G, Miltz W, Srinivas H, Penno CA, Kiffe M, Gajewska M, et al.
    Structure-guided elaboration of a fragment-like hit into an orally efficacious leukotriene A4 hydrolase inhibitor
    Journal of Medicinal Chemistry. 2024; 67(6): 5093-5108. https://doi.org/10.1021/acs.jmedchem.4c00290
    DORA PSI
  • Toledo-Patiño S, Goetz SK, Shanmugaratnam S, Höcker B, Farías-Rico JA
    Molecular handcraft of a well-folded protein chimera
    FEBS Letters. 2024; 598(11): 1375-1386. https://doi.org/10.1002/1873-3468.14856
    DORA PSI
  • Vulpetti A, Rondeau JM, Bellance MH, Blank J, Boesch R, Boettcher A, et al.
    Ligandability assessment of IL-1β by integrated hit identification approaches
    Journal of Medicinal Chemistry. 2024; 67: 8141-8160. https://doi.org/10.1021/acs.jmedchem.4c00240
    DORA PSI
  • Abe-Sato K, Tabuse H, Kanazawa H, Kamitani M, Endo M, Tokura S, et al.
    Structure-based optimization and biological evaluation of potent and selective MMP-7 inhibitors for kidney fibrosis
    Journal of Medicinal Chemistry. 2023; 66(21): 14653-14668. https://doi.org/10.1021/acs.jmedchem.3c01166
    DORA PSI
  • Adam S, Zheng D, Klein A, Volz C, Mullen W, Shirran SL, et al.
    Unusual peptide-binding proteins guide pyrroloindoline alkaloid formation in crocagin biosynthesis
    Nature Chemistry. 2023; 15(4): 560-568. https://doi.org/10.1038/s41557-023-01153-w
    DORA PSI
  • Alper P, Betschart C, André C, Boulay T, Cheng D, Deane J, et al.
    Discovery of the TLR7/8 antagonist MHV370 for treatment of systemic autoimmune diseases
    ACS Medicinal Chemistry Letters. 2023; 14(8): 1054-1062. https://doi.org/10.1021/acsmedchemlett.3c00136
    DORA PSI
  • Berneburg I, Stumpf M, Velten A-S, Rahlfs S, Przyborski J, Becker K, et al.
    Structure of Leishmania donovani 6-phosphogluconate dehydrogenase and inhibition by phosphine gold(I) complexes: a potential approach to leishmaniasis treatment
    International Journal of Molecular Sciences. 2023; 24(10): 8615 (20 pp.). https://doi.org/10.3390/ijms24108615
    DORA PSI
  • Blum A, Dorsch D, Linde N, Brandstetter S, Buchstaller H-P, Busch M, et al.
    Identification of M4205 - a highly selective inhibitor of KIT mutations for treatment of unresectable metastatic or recurrent gastrointestinal stromal tumors
    Journal of Medicinal Chemistry. 2023; 66(4): 2386-2395. https://doi.org/10.1021/acs.jmedchem.2c00851
    DORA PSI
  • Boland C, Huang C-Y, Shanker Kaki S, Wang M, Olieric V, Caffrey M
    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. 2023; 13(9): 1402 (20 pp.). https://doi.org/10.3390/cryst13091402
    DORA PSI
  • Bothe U, Günther J, Nubbemeyer R, Siebeneicher H, Ring S, Bömer U, et al.
    Discovery of IRAK4 Inhibitors BAY1834845 (Zabedosertib) and BAY1830839
    Journal of Medicinal Chemistry. 2023; 67: 1125-1242. https://doi.org/10.1021/acs.jmedchem.3c01714
    DORA PSI
  • Buchstaller H-P, Sala-Hojman A, Leiendecker M, Albers J, Anlauf U, Berges N, et al.
    Discovery of cycloalkyl[c]thiophenes as novel scaffolds for hypoxia-inducible factor-2α inhibitors
    Journal of Medicinal Chemistry. 2023; 66(13): 8666-8686. https://doi.org/10.1021/acs.jmedchem.3c00332
    DORA PSI
  • Bührmann M, Kallepu S, Warmuth JD, Wiese JN, Ehrt C, Vatheuer H, et al.
    FRAGTORY: pharmacophore-focused design, synthesis, and evaluation of an sp3-enriched fragment library
    Journal of Medicinal Chemistry. 2023; 66(9): 6297-6314. https://doi.org/10.1021/acs.jmedchem.3c00187
    DORA PSI
  • Chen X-R, Poudel L, Hong Z, Johnen P, Katti S, Tripathi A, et al.
    Mechanisms by which small molecules of diverse chemotypes arrest Sec14 lipid transfer activity
    Journal of Biological Chemistry. 2023; 299(2): 102861 (21 pp.). https://doi.org/10.1016/j.jbc.2022.102861
    DORA PSI
  • Claff T, Schlegel JG, Voss JH, Vaaßen VJ, Weiße RH, Cheng RKY, et al.
    Crystal structure of adenosine A2A receptor in complex with clinical candidate Etrumadenant reveals unprecedented antagonist interaction
    Communications Chemistry. 2023; 6(1): 106 (10 pp.). https://doi.org/10.1038/s42004-023-00894-6
    DORA PSI
  • Cumming JG, Kreis L, Kühne H, Wermuth R, Vercruysse M, Kramer C, et al.
    Discovery of a series of indane-containing NBTIs with activity against multidrug-resistant gram-negative pathogens
    ACS Medicinal Chemistry Letters. 2023; 14(7): 993-998. https://doi.org/10.1021/acsmedchemlett.3c00187
    DORA PSI
  • Demin S, Peschiulli A, Velter AI, Vos A, De Boeck B, Miller B, et al.
    Macrocyclic carbon-linked pyrazoles as novel inhibitors of MCL-1
    ACS Medicinal Chemistry Letters. 2023; 14(7): 955-961. https://doi.org/10.1021/acsmedchemlett.3c00141
    DORA PSI
  • Dietl A, Wellach K, Mahadevan P, Mertes N, Winter SL, Kutsch T, et al.
    Structures of an unusual 3-hydroxyacyl dehydratase (FabZ) from a ladderane-producing organism with an unexpected substrate preference
    Journal of Biological Chemistry. 2023; 299(5): 104602 (15 pp.). https://doi.org/10.1016/j.jbc.2023.104602
    DORA PSI
  • Dillenberger M, Werner A-D, Velten A-S, Rahlfs S, Becker K, Fritz-Wolf K
    Structural analysis of Plasmodium falciparum hexokinase provides novel information about catalysis due to a Plasmodium-specific insertion
    International Journal of Molecular Sciences. 2023; 24(16): 12739 (20 pp.). https://doi.org/10.3390/ijms241612739
    DORA PSI
  • Duan J, Hemschemeier A, Burr DJ, Stripp ST, Hofmann E, Happe T
    Cyanide binding to [FeFe]-hydrogenase stabilizes the alternative configuration of the proton transfer pathway
    Angewandte Chemie International Edition. 2023; 62(7): e202216903 (4 pp.). https://doi.org/10.1002/anie.202216903
    DORA PSI
  • Dunbar KL, Perlatti B, Liu N, Cornelius A, Mummau D, Chiang Y-M, et al.
    Resistance gene–guided genome mining reveals the roseopurpurins as inhibitors of cyclin-dependent kinases
    Proceedings of the National Academy of Sciences of the United States of America PNAS. 2023; 120(48): e2310522120 (10 pp.). https://doi.org/10.1073/pnas.2310522120
    DORA PSI
  • Duvall JR, Thomas JD, Bukhalid RA, Catcott KC, Bentley KW, Collins SD, et al.
    Discovery and optimization of a STING agonist platform for application in antibody drug conjugates
    Journal of Medicinal Chemistry. 2023; 66(15): 10715-10733. https://doi.org/10.1021/acs.jmedchem.3c00907
    DORA PSI
  • Ebenhoch R, Bauer M, Romig H, Gottschling D, Kley JT, Heine N, et al.
    Crystal structures of human and mouse ketohexokinase provide a structural basis for species- and isoform-selective inhibitor design
    Acta Crystallographica Section D: Structural Biology. 2023; 79(10): 871-880. https://doi.org/10.1107/S2059798323006137
    DORA PSI
  • Fedir B, Yannick M, Marco M, Patrizia F, Catherine Z, Frédéric V, et al.
    N‐terminal β‐strand in YAP is critical for stronger binding to scalloped relative to TEAD transcription factor
    Protein Science. 2023; 32(1): e4545 (13 pp.). https://doi.org/10.1002/pro.4545
    DORA PSI
  • Fischman S, Levin I, Rondeau J-M, Štrajbl M, Lehmann S, Huber T, et al.
    "Redirecting an anti-IL-1β antibody to bind a new, unrelated and computationally predicted epitope on hIL-17A"
    Communications Biology. 2023; 6(1): 997 (13 pp.). https://doi.org/10.1038/s42003-023-05369-x
    DORA PSI
  • Gehl M, Demmer U, Ermler U, Shima S
    Crystal structure of FAD-independent methylene-tetrahydrofolate reductase from Mycobacterium hassiacum
    Proteins. 2023; 91(9): 1329-1340. https://doi.org/10.1002/prot.26504
    DORA PSI
  • Goebel L, Kirschner T, Koska S, Rai A, Janning P, Maffini S, et al.
    Targeting oncogenic KRasG13C with nucleotide-based covalent inhibitors
    eLife. 2023; 12: e82184 (22 pp.). https://doi.org/10.7554/elife.82184
    DORA PSI
  • Grädler U, Schwarz D, Wegener A, Eichhorn T, Bandeiras TM, Freitas MC, et al.
    Biophysical and structural characterization of the impacts of MET phosphorylation on tepotinib binding
    Journal of Biological Chemistry. 2023; 299(11): 105328 (14 pp.). https://doi.org/10.1016/j.jbc.2023.105328
    DORA PSI
  • Guerlavais V, Sawyer TK, Carvajal L, Chang YS, Graves B, Ren J-G, et al.
    Discovery of sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-helical peptide in clinical development
    Journal of Medicinal Chemistry. 2023; 66(14): 9401-9417. https://doi.org/10.1021/acs.jmedchem.3c00623
    DORA PSI
  • Heim C, Spring A-K, Kirchgäßner S, Schwarzer D, Hartmann MD
    Cereblon neo-substrate binding mimics the recognition of the cyclic imide degron
    Biochemical and Biophysical Research Communications. 2023; 646: 30-35. https://doi.org/10.1016/j.bbrc.2023.01.051
    DORA PSI
  • Hellweg L, Edenhofer A, Barck L, Huppertz MC, Frei MS, Tarnawski M, et al.
    A general method for the development of multicolor biosensors with large dynamic ranges
    Nature Chemical Biology. 2023; 19: 1147-1157. https://doi.org/10.1038/s41589-023-01350-1
    DORA PSI
  • Hiemstra IH, Santegoets KCM, Janmaat ML, De Goeij BECG, Ten Hagen W, van Dooremalen S, et al.
    Preclinical anti-tumour activity of HexaBody-CD38, a next-generation CD38 antibody with superior complement-dependent cytotoxic activity
    EBioMedicine. 2023; 93: 104663 (19 pp.). https://doi.org/10.1016/j.ebiom.2023.104663
    DORA PSI
  • Hommel U, Hurth K, Rondeau J-M, Vulpetti A, Ostermeier D, Boettcher A, et al.
    Discovery of a selective and biologically active low-molecular weight antagonist of human interleukin-1β
    Nature Communications. 2023; 14(1): 5497 (13 pp.). https://doi.org/10.1038/s41467-023-41190-0
    DORA PSI
  • Imai Y, Suzuki R, Wakasugi D, Matsuda D, Tanaka-Yamamoto N, Ohki Y, et al.
    Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor
    Bioorganic and Medicinal Chemistry. 2023; 93: 117460 (15 pp.). https://doi.org/10.1016/j.bmc.2023.117460
    DORA PSI
  • Kalliokoski T, Kettunen H, Kumpulainen E, Kettunen E, Thieulin-Pardo G, Neumann L, et al.
    Discovery of novel methionine adenosyltransferase 2A (MAT2A) allosteric inhibitors by structure-based virtual screening
    Bioorganic and Medicinal Chemistry Letters. 2023; 94: 129450 (8 pp.). https://doi.org/10.1016/j.bmcl.2023.129450
    DORA PSI
  • Kim D, Herdeis L, Rudolph D, Zhao Y, Böttcher J, Vides A, et al.
    Pan-KRAS inhibitor disables oncogenic signalling and tumour growth
    Nature. 2023; 619(7968): 160-166. https://doi.org/10.1038/s41586-023-06123-3
    DORA PSI
  • Kompa J, Bruins J, Glogger M, Wilhelm J, Frei MS, Tarnawski M, et al.
    Exchangeable HaloTag ligands for super-resolution fluorescence microscopy
    Journal of the American Chemical Society. 2023; 145(5): 3075-3083. https://doi.org/10.1021/jacs.2c11969
    DORA PSI
  • Krasavin M, Adamchik M, Bubyrev A, Heim C, Maiwald S, Zhukovsky D, et al.
    Synthesis of novel glutarimide ligands for the E3 ligase substrate receptor Cereblon (CRBN): Investigation of their binding mode and antiproliferative effects against myeloma cell lines
    European Journal of Medicinal Chemistry. 2023; 246: 114990 (12 pp.). https://doi.org/10.1016/j.ejmech.2022.114990
    DORA PSI
  • Krieger J, Sorrell FJ, Wegener AA, Leuthner B, Machrouhi-Porcher F, Hecht M, et al.
    Systematic potency and property assessment of VHL ligands and implications on PROTAC design
    ChemMedChem. 2023; 18(8): e202200615 (11 pp.). https://doi.org/10.1002/cmdc.202200615
    DORA PSI
  • Kuhn B, Ritter M, Benz J, Kocer B, Sarie JC, Hochstrasser R, et al.
    Novel potent and highly selective DDR1 inhibitors from integrated lead finding
    Medicinal Chemistry Research. 2023; 32(7): 1400-1425. https://doi.org/10.1007/s00044-023-03066-2
    DORA PSI
  • Leit S, Greenwood J, Carriero S, Mondal S, Abel R, Ashwell M, et al.
    Discovery of a potent and selective tyrosine kinase 2 inhibitor: TAK-279
    Journal of Medicinal Chemistry. 2023; 66: 10473-10496. https://doi.org/10.1021/acs.jmedchem.3c00600
    DORA PSI
  • Liu J, Chiang H-C, Xiong W, Laurent V, Griffiths SC, Dülfer J, et al.
    A highly selective humanized DDR1 mAb reverses immune exclusion by disrupting collagen fiber alignment in breast cancer
    Journal for ImmunoTherapy of Cancer. 2023; 11(6): e006720 (14 pp.). https://doi.org/10.1136/jitc-2023-006720
    DORA PSI
  • Martinelli P, Schaaf O, Mantoulidis A, Martin LJ, Fuchs JE, Bader G, et al.
    Discovery of a chemical probe to study implications of BPTF bromodomain inhibition in cellular and in vivo experiments
    ChemMedChem. 2023; 18(6): e202200686 (8 pp.). https://doi.org/10.1002/cmdc.202200686
    DORA PSI
  • Mauxion F, Basquin J, Ozgur S, Rame M, Albrecht J, Schäfer I, et al.
    The human CNOT1-CNOT10-CNOT11 complex forms a structural platform for protein-protein interactions
    Cell Reports. 2023; 42(1): 111902 (18 pp.). https://doi.org/10.1016/j.celrep.2022.111902
    DORA PSI
  • Mesrouze Y, Gubler H, Villard F, Boesch R, Ottl J, Kallen J, et al.
    Biochemical and structural characterization of a peptidic inhibitor of the YAP:TEAD interaction that binds to the α-Helix Pocket on TEAD
    ACS Chemical Biology. 2023; 18(3): 643-651. https://doi.org/10.1021/acschembio.2c00936
    DORA PSI
  • Mhaindarkar VP, Rasche R, Kümmel D, Rudolph MG, Klostermeier D
    Structure of reverse gyrase with a minimal latch that supports ATP-dependent positive supercoiling without specific interactions with the topoisomerase domain
    Acta Crystallographica Section D: Structural Biology. 2023; 79(6): 498-507. https://doi.org/10.1107/S2059798323002565
    DORA PSI
  • Miyagi H, Suzuki M, Yasunaga M, Asada H, Iwata S, Saito J-ichi
    Structural insight into an anti-BRIL Fab as a G-protein-coupled receptor crystallization chaperone
    Acta Crystallographica Section D: Structural Biology. 2023; 79(5): 435-441. https://doi.org/10.1107/S205979832300311X
    DORA PSI
  • Nain-Perez A, Nilsson O, Lulla A, Håversen L, Brear P, Liljenberg S, et al.
    Tuning liver pyruvate kinase activity up or down with a new class of allosteric modulators
    European Journal of Medicinal Chemistry. 2023; 250: 115177 (18 pp.). https://doi.org/10.1016/j.ejmech.2023.115177
    DORA PSI
  • Ohta A, Tanada M, Shinohara S, Morita Y, Nakano K, Yamagishi Y, et al.
    Validation of a new methodology to create oral drugs beyond the rule of 5 for intracellular tough targets
    Journal of the American Chemical Society. 2023; 145(44): 24035-24051. https://doi.org/10.1021/jacs.3c07145
    DORA PSI
  • O’Dea R, Kazi N, Hoffmann-Benito A, Zhao Z, Recknagel S, Wendrich K, et al.
    Molecular basis for ubiquitin/Fubi cross-reactivity in USP16 and USP36
    Nature Chemical Biology. 2023; 19(11): 1394-1405. https://doi.org/10.1038/s41589-023-01388-1
    DORA PSI
  • Roehrig S, Ackerstaff J, Jiménez Núñez E, Teller H, Ellerbrock P, Meier K, et al.
    Design and preclinical characterization program toward Asundexian (BAY 2433334), an oral factor XIa inhibitor for the prevention and treatment of thromboembolic disorders
    Journal of Medicinal Chemistry. 2023; 66(17): 12203-12224. https://doi.org/10.1021/acs.jmedchem.3c00795
    DORA PSI
  • Rutz S, Deneka D, Dittmann A, Sawicka M, Dutzler R
    Structure of a volume-regulated heteromeric LRRC8A/C channel
    Nature Structural and Molecular Biology. 2023; 30: 52-61. https://doi.org/10.1038/s41594-022-00899-0
    DORA PSI
  • Schmeing S, Amrahova G, Bigler K, Chang JY, Openy J, Pal S, et al.
    Rationally designed stapled peptides allosterically inhibit PTBP1-RNA-binding
    Chemical Science. 2023; 14(31): 8269-8278. https://doi.org/10.1039/d3sc00985h
    DORA PSI
  • Schröder M, Leiendecker M, Grädler U, Braun J, Blum A, Wanior M, et al.
    MSC-1186, a highly selective Pan-SRPK inhibitor based on an exceptionally decorated benzimidazole-pyrimidine core
    Journal of Medicinal Chemistry. 2023; 66(1): 837-854. https://doi.org/10.1021/acs.jmedchem.2c01705
    DORA PSI
  • Selim KA, Haffner M, Mantovani O, Albrecht R, Zhu H, Hagemann M, et al.
    Carbon signaling protein SbtB possesses atypical redox-regulated apyrase activity to facilitate regulation of bicarbonate transporter SbtA
    Proceedings of the National Academy of Sciences of the United States of America PNAS. 2023; 120(8): e2205882120 (11 pp.). https://doi.org/10.1073/pnas.2205882120
    DORA PSI
  • Sellner H, Chapeau E, Furet P, Voegtle M, Salem B, Le Douget M, et al.
    Optimization of a class of dihydrobenzofurane analogs toward orally efficacious YAP-TEAD protein-protein interaction inhibitors
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