Publications

Publications RG Hausch

Pubmed Citation collection

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125.Marrone L, Di Giacomo V, Malasomma C, Vecchione MA, Hausch F, Cacace M, D’Esposito L, Tufano M, D’Arrigo P, Romano MF, et al. Exploring the potential of selective FKBP51 inhibitors on melanoma: an investigation of their in vitro and in vivo effects. Cell Death Discov. 2025;11:138. doi (link): 10.1038/s41420-025-02430-y.
124.Repity ML, Deutscher RCE, Hausch F. Nondegradative Synthetic Molecular Glues Enter the Clinic. ChemMedChem. 2025; do (link)i: 10.1002/cmdc.202500048.
123. Quist-Lokken I, Tilseth M, Andersson-Rusch C, Hanif MA, Walz M, Moen JFN, Vik MA, Slordahl TS, Sundan A, Hausch F, et al. Novel PROTAC to target FKBP12: the potential to enhance bone morphogenetic protein activity and apoptosis in multiple myeloma. Haematologica. 2025; doi (link): 10.3324/haematol.2024.287047.
122. Deutscher RCE, Meyners C, Repity ML, Sugiarto WO, Kolos JM, Maciel EVS, Heymann T, Geiger TM, Knapp S, Lermyte F, et al. Discovery of fully synthetic FKBP12-mTOR molecular glues. Chem Sci. 2025; doi (link): 10.1039/D4SC06917J.
121. Spiske M, Meyners C, Bauder M, Repity M, Brudy C, Sugiarto WO, Achaq H, Geiger TM, Hausch F. Conformationally Restricted Macrocycles as Improved FKBP51 Inhibitors Enabled by Systematic Linker Derivatization. Angew Chemie Int Ed. 2025; doi (link): 10.1002/anie.202418511.
120. Krysenko S, Emani CS, Bäuerle M, Oswald M, Kulik A, Meyners C, Hillemann D, Merker M, Prosser G, Wohlers I, et al. GlnA3 Mt is able to glutamylate spermine but it is not essential for the detoxification of spermine in Mycobacterium tuberculosis. Federle MJ, editor. J Bacteriol. 2025; doi (link): 10.1128/jb.00439-24.
119. Buffa V, Walz C, Meyners C, Zheng M, Sugiarto WO, Repity M, Achaq H, Cica M, Brudy C, Spiske M, et al. Conformational Plasticity and Binding Affinity Enhancement Controlled by Linker Derivatization in Macrocycles. Angew Chemie Int Ed. 2025; doi (link): 10.1002/anie.202418512.
118. Walz C, Spiske M, Walter M, Keller B-L, Mezler M, Hoft C, Pohlki F, Vukelić S, Hausch F. Macrocyclization as a Strategy for Kinetic Solubility Improvement: A Comparative Analysis of Matched Molecular Pairs. J Med Chem. 2025; doi (link): 10.1021/acs.jmedchem.4c01822.
117. Gnatzy MT, Hartmann S, Hausch F. Development of a Class A/B Hybrid GPCR System for the Proximity-Assisted Screening of GPCR Ligands. ACS Chem Biol. 2025;20:172–178. doi (link): 10.1021/acschembio.4c00658.

2024

116. Lohr T, Herbst C, Bzdyl NM, Jenkins C, Scheuplein NJ, Sugiarto WO, Whittaker JJ, Guskov A, Norville I, Hellmich UA, et al. High Affinity Inhibitors of the Macrophage Infectivity Potentiator Protein from Trypanosoma cruzi , Burkholderia pseudomallei , and Legionella pneumophila ─A Comparison. ACS Infect Dis. 2024;10:3681–3691. doi (link): 10.1021/acsinfecdis.4c00553.
115. Dreizler JK, Meyners C, Hausch F. Toward Dual Targeting of Catalytic and Gatekeeper Pockets in Cyclophilins Using a Macrocyclic Scaffold. ACS Med Chem Lett. 2024;15:2012–2018. doi (link): 10.1021/acsmedchemlett.4c00427.
114. Brudy C, Walz C, Spiske M, Dreizler JK, Hausch F. The Missing Link(er): A Roadmap to Macrocyclization in Drug Discovery. J Med Chem. 2024; doi (link): 10.1021/acs.jmedchem.4c01163.
113. Mareczek L, Mueller LK, Halstenberg L, Geiger TM, Walz M, Zheng M, Hausch F. Use of Poly(vinyl alcohol) in Spray-Dried Dispersions: Enhancing Solubility and Stability of Proteolysis Targeting Chimeras. Pharmaceutics. 2024;16:924. doi (link): 10.3390/pharmaceutics16070924.
112. Buffa V, Meyners C, Sugiarto WO, Bauder M, Gaali S, Hausch F. 1,4‐Pyrazolyl‐containing SAFit‐analogues are selective FKBP51 inhibitors with improved ligand efficiency and drug‐like profile. ChemMedChem. 2024; doi (link): 10.1002/cmdc.202400264.
111. Krajczy P, Meyners C, Repity M, Hausch F. Structure‐Based Design of Ultrapotent Tricyclic Ligands for FK506‐Binding proteins. Chem – A Eur J. 2024; doi (link): 10.1002/chem.202401405.
110. Hartmann J, Bajaj T, Otten J, Klengel C, Ebert T, Gellner A-K, Junglas E, Hafner K, Anderzhanova EA, Tang F, et al. SKA2 regulated hyperactive secretory autophagy drives neuroinflammation-induced neurodegeneration. Nat Commun. 2024;15:2635. doi (link): 10.1038/s41467-024-46953-x.
109. Wiedemann C, Whittaker JJ, Pérez Carrillo VH, Goretzki B, Dajka M, Tebbe F, Harder J-M, Krajczy PR, Joseph B, Hausch F, et al. Legionella pneumophila macrophage infectivity potentiator protein appendage domains modulate protein dynamics and inhibitor binding. Int J Biol Macromol. 2023;252:126366. doi (link): 10.1016/j.ijbiomac.2023.126366.
108. Stransky F, Kostrz D, Follenfant M, Pomplun S, Meyners C, Strick T, Hausch F, Gosse C. Use of DNA forceps to measure receptor-ligand dissociation equilibrium constants in a single-molecule competition assay. 2024. p. 51–82. Available from here
107. Schäfer SC, Voll AM, Bracher A, Ley S V., Hausch F. Antascomicin B stabilizes FKBP51-Akt1 complexes as a molecular glue. Bioorg Med Chem Lett. 2024;104:129728. doi (link): 10.1016/j.bmcl.2024.129728.
106. Charalampidou A, Nehls T, Meyners C, Gandhesiri S, Pomplun S, Pentelute BL, Lermyte F, Hausch F. Automated Flow Peptide Synthesis Enables Engineering of Proteins with Stabilized Transient Binding Pockets. ACS Cent Sci. 2024; doi (link): 10.1021/acscentsci.3c01283.

2023

105. Lerma Romero JA, Meyners C, Rupp N, Hausch F, Kolmar H. A protein engineering approach toward understanding FKBP51 conformational dynamics and mechanisms of ligand binding. Protein Eng Des Sel. 2023;36. doi (link): 10.1093/protein/gzad014.
104. Geiger TM, Walz M, Meyners C, Kuehn A, Dreizler JK, Sugiarto WO, Maciel E, Zheng M, Lermyte F, Hausch F. Discovery of a Potent PROTAC Enables Targeting of FKBP51’s Scaffolding Functions. Angew Chemie Int Ed. 2023; doi (link): 10.1002/anie.202309706.
103. Baischew A, Engel S, Taubert MC, Geiger TM, Hausch F. Large-scale, in-cell photocrosslinking at single-residue resolution reveals the molecular basis for glucocorticoid receptor regulation by immunophilins. Nat Struct Mol Biol. 2023; doi (link): 10.1038/s41594-023-01098-1.
102. Purder PL, Meyners C, Sugiarto WO, Kolos J, Löhr F, Gebel J, Nehls T, Dötsch V, Lermyte F, Hausch F. Deconstructing Protein Binding of Sulfonamides and Sulfonamide Analogues. JACS Au. 2023; doi (link): 10.1021/jacsau.3c00241.
101. Wedel S, Hahnefeld L, Schreiber Y, Namendorf C, Heymann T, Uhr M, Schmidt M V., de Bruin N, Hausch F, Thomas D, et al. SAFit2 ameliorates paclitaxel-induced neuropathic pain by reducing spinal gliosis and elevating pro-resolving lipid mediators. J Neuroinflammation. 2023;20:149. doi (link): 10.1186/s12974-023-02835-5.
100. Deutscher R, Karagöz MS, Purder P, Kolos J, Meyners C, Sugiarto WO, Krajczy P, Tebbe F, Geiger T, Ünal C, et al. [4.3.1] Bicyclic FKBP ligands inhibit Legionella pneumophila infection by LpMip‐dependent and LpMip independent mechanisms. ChemBioChem. 2023; doi (link): 10.1002/cbic.202300442.
99. Knaup FH, Meyners C, Sugiarto WO, Wedel S, Springer M, Walz C, Geiger TM, Schmidt M, Sisignano M, Hausch F. Structure-Based Discovery of a New Selectivity-Enabling Motif for the FK506-Binding Protein 51. J Med Chem. 2023; doi (link): 10.1021/acs.jmedchem.3c00249.
98. Quist-Løkken I, Andersson-Rusch C, Kastnes MH, Kolos JM, Jatzlau J, Hella H, Olsen OE, Sundan A, Knaus P, Hausch F, et al. FKBP12 is a major regulator of ALK2 activity in multiple myeloma cells. Cell Commun Signal. 2023;21:25. doi (link): 10.1186/s12964-022-01033-9.
97. 1. Baischew A, Engel S, Geiger TM, Taubert MC, Hausch F. Structural and biochemical insights into FKBP51 as a Hsp90 co‐chaperone. J Cell Biochem. 2023; doi (link): 10.1002/jcb.30384.
96. Buffa V, Knaup FH, Heymann T, Springer M, Schmidt M V., Hausch F. Analysis of the Selective Antagonist SAFit2 as a Chemical Probe for the FK506-Binding Protein 51. ACS Pharmacol Transl Sci. 2023; doi (link): 10.1021/acsptsci.2c00234.

2022

95. Berthold EJ, Ma-Lauer Y, Chakraborty A, von Brunn B, Hilgendorff A, Hatz R, Behr J, Hausch F, Staab-Weijnitz CA, von Brunn A. Effects of immunophilin inhibitors and non-immunosuppressive analogs on coronavirus replication in human infection models. Front Cell Infect Microbiol. 2022;12. doi (link): 10.3389/fcimb.2022.958634
94. Wedel S, Mathoor P, Rauh O, Heymann T, Ciotu CI, Fuhrmann DC, Fischer MJM, Weigert A, de Bruin N, Hausch F, et al. SAFit2 reduces neuroinflammation and ameliorates nerve injury-induced neuropathic pain. J Neuroinflammation. 2022;19 doi (link): 10.1186/s12974-022-02615-7
93. Lerma Romero JA, Meyners C, Christmann A, Reinbold LM, Charalampidou A, Hausch F, Kolmar H. Binding pocket stabilization by high-throughput screening of yeast display libraries. Front Mol Biosci. 2022;9. doi (link): 10.3389/fmolb.2022.1023131
92. Wedel S, Hahnefeld L, Alnouri MW, Offermanns S, Hausch F, Geisslinger G, Sisignano M. The FKBP51 Inhibitor SAFit2 Restores the Pain-Relieving C16 Dihydroceramide after Nerve Injury. Int J Mol Sci. 2022;23 doi (link): 10.3390/ijms232214274
91. Wanstrath BJ, McLean SA, Zhao Y, Mickelson J, Bauder M, Hausch F, Linnstaedt SD. Duration of Reduction in Enduring Stress-Induced Hyperalgesia Via FKBP51 Inhibition Depends on Timing of Administration Relative to Traumatic Stress Exposure. J Pain. 2022 doi (link): https://doi.org/10.1016/j.jpain.2022.02.007
90. Purder PL, Meyners C, Krysenko S, Funk J, Wohlleben W, Hausch F. Mechanism‐based design of the first GlnA4‐specific inhibitors. ChemBioChem 2022; doi (link): https://doi.org/10.1002/cbic.202200312
89. Geiger TM, Schäfer SC, Dreizler JK, Walz M, Hausch F. Clues to molecular glues. Curr Res Chem Biol. 2022; 2: 100018. doi (link): https://doi.org/10.1016/j.crchbi.2021.100018

2021

88. Kolos JM, Pomplun S, Jung S, Rieß B, Purder PL, Voll AM, Merz S, Gnatzy M, Geiger TM, Quist-Løkken I, Jatzlau J, Knaus P, Holien T, Bracher A, Meyners C, Czodrowski P, Krewald V, Hausch F. Picomolar FKBP inhibitors enabled by a single water-displacing methyl group in bicyclic [4.3.1] aza-amides. Chem Sci. 2021; 12: 14758–14765. doi (link): https://doi.org/10.1039/d1sc04638a
87. Taubert MC, Hausch F. Break Away: FKBP12 sequestration as a target for increasing BMP activity. Cell Chem Biol. 2021; 28: 1253–1255. doi (link): https://doi.org/10.1016/j.chembiol.2021.08.015
86. Nehls T, Heymann T, Meyners C, Hausch F, Lermyte F. Fenton-Chemistry-Based Oxidative Modification of Proteins Reflects Their Conformation. Int J Mol Sci. 2021; 22: 9927. doi (link): https://doi.org/10.3390/ijms22189927
85. Martinelli S, Anderzhanova EA, Bajaj T, Wiechmann S, Dethloff F, Weckmann K, Heinz DE, Ebert T, Hartmann J, Geiger TM, Döngi M, Hafner K, Pöhlmann ML, Jollans L, Philipsen A, Schmidt S V., Schmidt U, Maccarrone G, Stein V, Hausch F, Turck CW, Schmidt M V., Gellner A-K, Kuster B, Gassen NC. Stress-primed secretory autophagy promotes extracellular BDNF maturation by enhancing MMP9 secretion. Nat Commun. 2021; 12: 4643. doi (link): https://doi.org/10.1038/s41467-021-24810-5
84. Knaup FH, Meyners C, Charalampidou A, Krajczy P, Purder PL, Ross T, Hausch F. Med Chem Remote: The Frontiers in Medicinal Chemistry 2021. ChemMedChem. 2021; 16: 2411–2416. doi (link): https://doi.org/10.1002/cmdc.202100355
83. Bailus BJ, Scheeler SM, Simons J, Sanchez MA, Tshilenge K-T, Creus-Muncunill J, Naphade S, Lopez-Ramirez A, Zhang N, Lakshika Madushani K, Moroz S, Loureiro A, Schreiber KH, Hausch F, Kennedy BK, Ehrlich ME, Ellerby LM. Modulating FKBP5/FKBP51 and autophagy lowers HTT (huntingtin) levels. Autophagy. 2021; 17: 4119–4140. doi (link): https://doi.org/10.1080/15548627.2021.1904489
82. Gnatzy MT, Geiger TM, Kuehn A, Gutfreund N, Walz M, Kolos JM, Hausch F. Development of NanoBRET‐Binding Assays for FKBP‐Ligand Profiling in Living Cells. ChemBioChem. 2021; 22: 2257–2261. doi (link): https://doi.org/10.1002/cbic.202100113
81. Voll AM, Meyners C, Taubert MC, Bajaj T, Heymann T, Merz S, Charalampidou A, Kolos J, Purder PL, Geiger TM, Wessig P, Gassen NC, Bracher A, Hausch F. Macrocyclic FKBP51 Ligands Define a Transient Binding Mode with Enhanced Selectivity. Angew Chemie Int Ed. 2021; 60: 13257–13263. doi (link): https://doi.org/10.1002/anie.202017352
80. Bauder M, Meyners C, Purder PL, Merz S, Sugiarto WO, Voll AM, Heymann T, Hausch F. Structure-Based Design of High-Affinity Macrocyclic FKBP51 Inhibitors. J Med Chem. 2021; 64: 3320–3349. doi (link): https://doi.org/10.1021/acs.jmedchem.0c02195

2020

79. Connelly KL, Wolsh CC, Barr JL, Bauder M, Hausch F, Unterwald EM. Sex differences in the effect of the FKBP5 inhibitor SAFit2 on anxiety and stress-induced reinstatement following cocaine self-administration. Neurobiol Stress. 2020; 13: 100232. doi (link): https://doi.org/10.1016/j.ynstr.2020.100232
78. Jagtap PKA, Kubelka T, Soni K, Will CL, Garg D, Sippel C, Kapp TG, Potukuchi HK, Schorpp K, Hadian K, Kessler H, Lührmann R, Hausch F, Bach T, Sattler M. Identification of phenothiazine derivatives as UHM-binding inhibitors of early spliceosome assembly. Nat Commun. 2020; 11: 5621. doi (link): https://doi.org/10.1038/s41467-020-19514-1
77. Schraut K, Kalnytska O, Lamp D, Jastroch M, Eder M, Hausch F, Gassen NC, Moore S, Nagaraj N, Lopez JP, Chen A, Schmidt M V. Loss of the psychiatric risk factor SLC6A15 is associated with increased metabolic functions in primary hippocampal neurons. Eur J Neurosci. 2021; 53: 390–401. doi (link): https://doi.org/10.1111/ejn.14990
76. Savarese AM, Ozburn AR, Metten P, Schlumbohm JP, Hack WR, LeMoine K, Hunt H, Hausch F, Bauder M, Crabbe JC. Targeting the Glucocorticoid Receptor Reduces Binge‐Like Drinking in High Drinking in the Dark (HDID‐1) Mice. Alcohol Clin Exp Res. 2020; 44: 1025–1036. doi (link): https://doi.org/10.1111/acer.14318
75. Bischoff M, Mayer P, Meyners C, Hausch F. Enantioselective Synthesis of a Tricyclic, sp 3 ‐Rich Diazatetradecanedione: an Amino Acid‐Based Natural Product‐Like Scaffold. Chem – A Eur J. 2020; 26: 4677–4681. doi (link): https://doi.org/10.1002/chem.201905144
74. Feng X, Sippel C, Knaup FH, Bracher A, Staibano S, Romano MF, Hausch F. A Novel Decalin-Based Bicyclic Scaffold for FKBP51-Selective Ligands. J Med Chem. 2020; 63: 231–240. doi (link): https://doi.org/10.1021/acs.jmedchem.9b01157

2019

73. D’Arrigo P, Digregorio M, Romano S, Tufano M, Rea A, Hausch F, Dedobbeleer M, Vigorito V, Russo S, Bauder M, Rogister B, Romano MF. The splicing FK506-binding protein-51 isoform plays a role in glioblastoma resistance through programmed cell death ligand-1 expression regulation. Cell Death Discov. 2019; 5: 137. doi (link): https://doi.org/10.1038/s41420-019-0216-0
72. Tietze D, Kaufmann D, Tietze AA, Voll A, Reher R, König G, Hausch F. Structural and Dynamical Basis of G Protein Inhibition by YM-254890 and FR900359: An Inhibitor in Action. J Chem Inf Model. 2019; 59: 4361–4373. doi (link): https://doi.org/10.1021/acs.jcim.9b00433
71. Hähle A, Geiger TM, Merz S, Meyners C, Tianqi M, Kolos J, Hausch F. FKBP51 and FKBP12.6—Novel and tight interactors of Glomulin. Picard D, editor. PLoS One. 2019; 14: e0221926. doi (link): https://doi.org/10.1371/journal.pone.0221926
70. König L, Kalinichenko LS, Huber SE, Voll AM, Bauder M, Kornhuber J, Hausch F, Müller CP. The selective FKBP51 inhibitor SAFit2 reduces alcohol consumption and reinstatement of conditioned alcohol effects in mice. Addict Biol. 2020; 25. doi (link): https://doi.org/10.1111/adb.12758
69. Krysenko S, Matthews A, Okoniewski N, Kulik A, Girbas MG, Tsypik O, Meyners CS, Hausch F, Wohlleben W, Bera A. Initial Metabolic Step of a Novel Ethanolamine Utilization Pathway and Its Regulation in Streptomyces coelicolor M145. Søgaard-Andersen L, editor. MBio. 2019; 10. doi (link): https://doi.org/10.1128/mbio.00326-19
68. Zannas AS, Jia M, Hafner K, Baumert J, Wiechmann T, Pape JC, Arloth J, Ködel M, Martinelli S, Roitman M, Röh S, Haehle A, Emeny RT, Iurato S, Carrillo-Roa T, Lahti J, Räikkönen K, Eriksson JG, Drake AJ, Waldenberger M, Wahl S, Kunze S, Lucae S, Bradley B, Gieger C, Hausch F, Smith AK, Ressler KJ, Müller-Myhsok B, Ladwig K-H, Rein T, Gassen NC, Binder EB. Epigenetic upregulation of FKBP5 by aging and stress contributes to NF-κB–driven inflammation and cardiovascular risk. Proc Natl Acad Sci. 2019; 116: 11370–11379. doi (link): https://doi.org/10.1073/pnas.1816847116
67. Jagtap PKA, Asami S, Sippel C, Kaila VRI, Hausch F, Sattler M. Selective Inhibitors of FKBP51 Employ Conformational Selection of Dynamic Invisible States. Angew Chemie Int Ed. 2019; 58: 9429–9433. doi (link): https://doi.org/10.1002/anie.201902994
66. Hähle A, Merz S, Meyners C, Hausch F. The Many Faces of FKBP51. Biomolecules. 2019; 9: 35. doi (link): https://doi.org/10.3390/biom9010035

2018

65. Kolos JM, Voll AM, Bauder M, Hausch F. FKBP Ligands—Where We Are and Where to Go? Front Pharmacol. 2018; 9. doi (link): https://doi.org/10.3389/fphar.2018.01425
64. Pöhlmann ML, Häusl AS, Harbich D, Balsevich G, Engelhardt C, Feng X, Breitsamer M, Hausch F, Winter G, Schmidt M V. Pharmacological Modulation of the Psychiatric Risk Factor FKBP51 Alters Efficiency of Common Antidepressant Drugs. Front Behav Neurosci. 2018; 12. doi (link): https://doi.org/10.3389/fnbeh.2018.00262
63. Sidibeh CO, Pereira MJ, Abalo XM, J Boersma G, Skrtic S, Lundkvist P, Katsogiannos P, Hausch F, Castillejo-López C, Eriksson JW. FKBP5 expression in human adipose tissue: potential role in glucose and lipid metabolism, adipogenesis and type 2 diabetes. Endocrine. doi (link): 2018; 62: 116-128. https://doi.org/10.1007/s12020-018-1674-5
62. Pomplun S, Sippel C, Hähle A, Tay D, Shima K, Klages A, Ünal CM, Rieß B, Toh HT, Hansen G, Yoon HS, Bracher A, Preiser P, Rupp J, Steinert M, Hausch F. Chemogenomic Profiling of Human and Microbial FK506-Binding Proteins. J Med Chem. 2018; 61:3660–3673. doi (link): https://doi.org/10.1021/acs.jmedchem.8b00137
61. Maiarù M, Morgan OB, Mao T, Breitsamer M, Bamber H, Pöhlmann M, Schmidt M V., Winter G, Hausch F, Géranton SM. The stress regulator FKBP51: a novel and promising druggable target for the treatment of persistent pain states across sexes. Pain. 2018; 159: 1224–1234. doi (link): https://doi.org/10.1097%2Fj.pain.0000000000001204

2017

60. Balsevich G, Häusl AS, Meyer CW, Karamihalev S, Feng X, Pöhlmann ML, Dournes C, Uribe-Marino A, Santarelli S, Labermaier C, Hafner K, Mao T, Breitsamer M, Theodoropoulou M, Namendorf C, Uhr M, Paez-Pereda M, Winter G, Hausch F, Chen A, Tschöp MH, Rein T, Gassen NC, Schmidt M V. Stress-responsive FKBP51 regulates AKT2-AS160 signaling and metabolic function. Nat Commun. 2017; 8: 1725. doi (link): https://doi.org/10.1038/s41467-017-01783-y
59. D’Arrigo P, Russo M, Rea A, Tufano M, Guadagno E, Del Basso De Caro ML, Pacelli R, Hausch F, Staibano S, Ilardi G, Parisi S, Romano MF, Romano S. A regulatory role for the co-chaperone FKBP51s in PD-L1 expression in glioma. Oncotarget. 2017; 8: 68291–68304. doi (link): https://doi.org/10.18632%2Foncotarget.19309
58. Hausch F. Cryo‐EM Structures of Class B GPCR Reveal the Activation Mechanism. Angew Chemie Int Ed. 2017; 56: 12412–12414. doi (link): https://doi.org/10.1002/anie.201707200
57. Schuster M, Schnell L, Feigl P, Birkhofer C, Mohr K, Roeder M, Carle S, Langer S, Tippel F, Buchner J, Fischer G, Hausch F, Frick M, Schwan C, Aktories K, Schiene-Fischer C, Barth H. The Hsp90 machinery facilitates the transport of diphtheria toxin into human cells. Sci Rep. 2017; 7: 613. doi (link): https://doi.org/10.1038/s41598-017-00780-x
56. Richers J, Pöthig A, Herdtweck E, Sippel C, Hausch F, Tiefenbacher K. Synthesis and Neurotrophic Activity Studies of Illicium Sesquiterpene Natural Product Analogues. Chem – A Eur J. 2017; 23: 3178–3183. doi (link): https://doi.org/10.1002/chem.201605362

2016

55. Gaali S, Feng X, Hähle A, Sippel C, Bracher A, Hausch F. Rapid, Structure-Based Exploration of Pipecolic Acid Amides as Novel Selective Antagonists of the FK506-Binding Protein 51. J Med Chem. 2016; 59: 2410–2422. doi (link): https://doi.org/10.1021/acs.jmedchem.5b01355
54. Maiarù M, Tochiki KK, Cox MB, Annan L V., Bell CG, Feng X, Hausch F, Géranton SM. The stress regulator FKBP51 drives chronic pain by modulating spinal glucocorticoid signaling. Sci Transl Med . 2016; 8. doi (link): https://doi.org/10.1126/scitranslmed.aab3376
53. Kirmeier T, Gopalakrishnan R, Gormanns V, Werner AM, Cuboni S, Rudolf GC, Höfner G, Wanner KT, Sieber SA, Schmidt U, Holsboer F, Rein T, Hausch F. Azidobupramine, an Antidepressant-Derived Bifunctional Neurotransmitter Transporter Ligand Allowing Covalent Labeling and Attachment of Fluorophores. Hashimoto K, editor. PLoS One. 2016; 11: e0148608. doi (link): https://doi.org/10.1371/journal.pone.0148608
52. Feng X, Pomplun S, Hausch F. Recent Progress in FKBP Ligand Development. Curr Mol Pharmacol. 2015; 9: 27–36. doi (link): https://doi.org/10.2174/1874467208666150519113313

2015

51. Feng X, Sippel C, Bracher A, Hausch F. Structure–Affinity Relationship Analysis of Selective FKBP51 Ligands. J Med Chem. 2015; 58: 7796–7806. doi (link): https://doi.org/10.1021/acs.jmedchem.5b00785
50. Romano S, Xiao Y, Nakaya M, D’Angelillo A, Chang M, Jin J, Hausch F, Masullo M, Feng X, Romano MF, Sun S-C. FKBP51 employs both scaffold and isomerase functions to promote NF-κB activation in melanoma. Nucleic Acids Res. 2015; 43: 6983–6993. doi (link): https://doi.org/10.1093/nar/gkv615
49. Hartmann J, Wagner K V., Gaali S, Kirschner A, Kozany C, Ruhter G, Dedic N, Hausl AS, Hoeijmakers L, Westerholz S, Namendorf C, Gerlach T, Uhr M, Chen A, Deussing JM, Holsboer F, Hausch F, Schmidt M V. Pharmacological Inhibition of the Psychiatric Risk Factor FKBP51 Has Anxiolytic Properties. J Neurosci. 2015; 35: 9007–9016. doi (link): https://doi.org/10.1523/JNEUROSCI.4024-14.2015
48. Navarro G, Quiroz C, Moreno-Delgado D, Sierakowiak A, McDowell K, Moreno E, Rea W, Cai N-S, Aguinaga D, Howell LA, Hausch F, Cortes A, Mallol J, Casado V, Lluis C, Canela EI, Ferre S, McCormick PJ. Orexin-Corticotropin-Releasing Factor Receptor Heteromers in the Ventral Tegmental Area as Targets for Cocaine. J Neurosci. 2015 Apr 29; 35: 6639–6653. doi (link): https://doi.org/10.1523/JNEUROSCI.4364-14.2015
47. Hausch F. FKBPs and their role in neuronal signaling. Biochim Biophys Acta – Gen Subj. 2015; 1850: 2035–2040. doi (link): https://doi.org/10.1016/j.bbagen.2015.01.012
46. Kohl C, Wang X-D, Grosse J, Fournier C, Harbich D, Westerholz S, Li J-T, Bacq A, Sippel C, Hausch F, Sandi C, Schmidt M V. Hippocampal neuroligin-2 links early-life stress with impaired social recognition and increased aggression in adult mice. Psychoneuroendocrinology. 2015; 55: 128–143. doi (link): https://doi.org/10.1016/j.psyneuen.2015.02.016
45. Riebold M, Theodoropoulou M, Kozany C, Hausch F, Stalla G, Paez-Pereda M. C-terminal Hsp90 inhibitors restore glucocorticoid sensitivity in an experimental model for Cushing’s disease. Exp Clin Endocrinol Diabetes. 2014; 122. doi: 10.1055/s-0034-1372049
44. Gaali S, Kirschner A, Cuboni S, Hartmann J, Kozany C, Balsevich G, Namendorf C, Fernandez-Vizarra P, Sippel C, Zannas AS, Draenert R, Binder EB, Almeida OFX, Rühter G, Uhr M, Schmidt M V, Touma C, Bracher A, Hausch F. Selective inhibitors of the FK506-binding protein 51 by induced fit. Nat Chem Biol. 2015; 11:33–37. doi (link): https://doi.org/10.1038/nchembio.1699
43. Pomplun S, Wang Y, Kirschner A, Kozany C, Bracher A, Hausch F. Rationales Design und asymmetrische Synthese potenter neuritotropher Liganden für FK506‐bindende Proteine (FKBPs). Angew Chemie. 2015; 127. doi: 10.1002/ange.201408776.

2014

42. Cuboni S, Devigny C, Hoogeland B, Strasser A, Pomplun S, Hauger B, Höfner G, Wanner KT, Eder M, Buschauer A, Holsboer F, Hausch F. Loratadine and Analogues: Discovery and Preliminary Structure–Activity Relationship of Inhibitors of the Amino Acid Transporter B 0 AT2. J Med Chem. 2014; 57: 9473–9479. doi (link): https://doi.org/10.1021/jm501086v
41. Bischoff M, Sippel C, Bracher A, Hausch F. Stereoselective Construction of the 5-Hydroxy Diazabicyclo[4.3.1]decane-2-one Scaffold, a Privileged Motif for FK506-Binding Proteins. Org Lett. 2014; 16: 5254–5257. doi (link): https://doi.org/10.1021/ol5023195
40. Labermaier C, Kohl C, Hartmann J, Devigny C, Altmann A, Weber P, Arloth J, Quast C, Wagner K V., Scharf SH, Czibere L, Widner-Andrä R, Brenndörfer J, Landgraf R, Hausch F, Jones KA, Müller MB, Uhr M, Holsboer F, Binder EB, Schmidt M V. A Polymorphism in the Crhr1 Gene Determines Stress Vulnerability in Male Mice. Endocrinology. 2014; 155: 2500–2510. doi (link): https://doi.org/10.1210/en.2013-1986
39. Cuboni S, Hausch F. Schnappschuss von Antidepressiva bei der Arbeit: die Struktur von Neurotransmittertransporter-Proteinen. Angew Chemie. 2014; 126: 5108–5109. doi (link): https://doi.org/10.1002/ange.201310567
38. Albu S, Romanowski CPN, Letizia Curzi M, Jakubcakova V, Flachskamm C, Gassen NC, Hartmann J, Schmidt M V., Schmidt U, Rein T, Holsboer F, Hausch F, Paez-Pereda M, Kimura M. Deficiency of FK506-binding protein (FKBP) 51 alters sleep architecture and recovery sleep responses to stress in mice. J Sleep Res. 2014; 23: 176–185. doi (link): https://doi.org/10.1111/jsr.12112

2013

37. Hausch F. Strukturen der G-Protein-gekoppelten Rezeptoren der Klasse B: Perspektiven für die Arzneimittelforschung. Angew Chemie. 2013; 125: 13017–13019. doi (link): https://doi.org/10.1002/ange.201307542
36. Bracher A, Kozany C, Hähle A, Wild P, Zacharias M, Hausch F. Crystal Structures of the Free and Ligand-Bound FK1–FK2 Domain Segment of FKBP52 Reveal a Flexible Inter-Domain Hinge. J Mol Biol. 2013; 425: 4134–4144. doi (link): https://doi.org/10.1016/j.jmb.2013.07.041
35. Hausch F, Kozany C, Theodoropoulou M, Fabian A-K. FKBPs and the Akt/mTOR pathway. Cell Cycle. 2013; 12: 2366–2370. doi (link): https://doi.org/10.4161/cc.25508
34. Quast C, Cuboni S, Bader D, Altmann A, Weber P, Arloth J, Röh S, Brückl T, Ising M, Kopczak A, Erhardt A, Hausch F, Lucae S, Binder EB. Functional Coding Variants in SLC6A15, a Possible Risk Gene for Major Depression. Liu C, editor. PLoS One. 2013; 8: e68645. doi (link): https://doi.org/10.1371/journal.pone.0068645
33. Wang Y, Kirschner A, Fabian A-K, Gopalakrishnan R, Kress C, Hoogeland B, Koch U, Kozany C, Bracher A, Hausch F. Increasing the Efficiency of Ligands for FK506-Binding Protein 51 by Conformational Control. J Med Chem. 2013; 56: 3922–3935. doi (link): https://doi.org/10.1021/jm400087k
32. Fabian A-K, März A, Neimanis S, Biondi RM, Kozany C, Hausch F. InterAKTions with FKBPs – Mutational and Pharmacological Exploration. Porter J, editor. PLoS One. 2013; 8: e57508. doi (link): https://doi.org/10.1371/journal.pone.0057508
31. März AM, Fabian A-K, Kozany C, Bracher A, Hausch F. Large FK506-Binding Proteins Shape the Pharmacology of Rapamycin. Mol Cell Biol. 2013; 33: 1357–1367. doi (link): https://doi.org/10.1128/MCB.00678-12

2012

30. Hausch F, Holsboer F. Die sieben Säulen der molekularen Pharmakologie: GPCR-Forschung mit Chemie-Nobelpreis geehrt. Angew Chemie. 2012; 124: 12338–12341. doi (link): https://doi.org/10.1002/ange.201208565
29. Hausch F, Holsboer F. Snapshot of an activated peptide receptor. Nature. 2012; 490: 492–493. doi (link): https://doi.org/10.1038/nature11634
28. Hartmann J, Wagner K V., Dedic N, Marinescu D, Scharf SH, Wang X-D, Deussing JM, Hausch F, Rein T, Schmidt U, Holsboer F, Müller MB, Schmidt M V. Fkbp52 heterozygosity alters behavioral, endocrine and neurogenetic parameters under basal and chronic stress conditions in mice. Psychoneuroendocrinology. 2012; 39: 2009–2021. doi (link): https://doi.org/10.1016/j.psyneuen.2012.04.017
27. Schmidt M V., Paez-Pereda M, Holsboer F, Hausch F. The Prospect of FKBP51 as a Drug Target. ChemMedChem. 2012; 7: 1351–1359. doi (link): https://doi.org/10.1002/cmdc.201200137
26. Gopalakrishnan R, Kozany C, Wang Y, Schneider S, Hoogeland B, Bracher A, Hausch F. Exploration of Pipecolate Sulfonamides as Binders of the FK506-Binding Proteins 51 and 52. J Med Chem. 2012; 55: 4123–4131. doi (link): https://doi.org/10.1021/jm201747c
25. Gopalakrishnan R, Kozany C, Gaali S, Kress C, Hoogeland B, Bracher A, Hausch F. Evaluation of Synthetic FK506 Analogues as Ligands for the FK506-Binding Proteins 51 and 52. J Med Chem. 2012; 55: 4114–4122. doi (link): https://doi.org/10.1021/jm201746x
24. Hartmann J, Wagner K V., Liebl C, Scharf SH, Wang X-D, Wolf M, Hausch F, Rein T, Schmidt U, Touma C, Cheung-Flynn J, Cox MB, Smith DF, Holsboer F, Müller MB, Schmidt M V. The involvement of FK506-binding protein 51 (FKBP5) in the behavioral and neuroendocrine effects of chronic social defeat stress. Neuropharmacology. 2012; 62: 332–339. doi (link): https://doi.org/10.1016/j.neuropharm.2011.07.041

2011

23. Touma C, Gassen NC, Herrmann L, Cheung-Flynn J, Büll DR, Ionescu IA, Heinzmann J-M, Knapman A, Siebertz A, Depping A-M, Hartmann J, Hausch F, Schmidt M V., Holsboer F, Ising M, Cox MB, Schmidt U, Rein T. FK506 Binding Protein 5 Shapes Stress Responsiveness: Modulation of Neuroendocrine Reactivity and Coping Behavior. Biol Psychiatry. 2011; 70: 928–936. doi (link): https://doi.org/10.1016/j.biopsych.2011.07.023
22. Gaali S, Gopalakrishnan R, Wang Y, Kozany C, Hausch F. The Chemical Biology of Immunophilin Ligands. Curr Med Chem. 2011; 18: 5355–5379. doi (link): https://doi.org/10.2174/092986711798194342
21. Gräber M, Janczyk W, Sperl B, Elumalai N, Kozany C, Hausch F, Holak TA, Berg T. Selective Targeting of Disease-Relevant Protein Binding Domains by O -Phosphorylated Natural Product Derivatives. ACS Chem Biol. 2011; 6: 1008–1014. doi (link): https://doi.org/10.1021/cb2001796
20. Devigny C, Perez-Balderas F, Hoogeland B, Cuboni S, Wachtel R, Mauch CP, Webb
KJ, Deussing JM, Hausch F.Biomimetic screening of class-B G protein-coupled receptors. J Am Chem Soc. 2011; 133: 8927-33. doi (link): https://doi.org/10.1021/ja200160s
19. Bracher A, Kozany C, Thost A-K, Hausch F. Structural characterization of the PPIase domain of FKBP51, a cochaperone of human Hsp90. Acta Crystallogr Sect D Biol Crystallogr. 2011; 67: 549–559. doi (link): https://doi.org/10.1107/S0907444911013862
18. Paez-Pereda M, Hausch F, Holsboer F.Corticotropin releasing factor receptor antagonists for major depressive disorder. Expert Opin Investig Drugs. 2011; 20: 519-35. doi (link): https://doi.org/10.1517/13543784.2011.565330.

2010

17. Gaali S, Kozany C, Hoogeland B, Klein M, Hausch F. Facile synthesis of a fluorescent cyclosporin a analogue to study cyclophilin 40 and cyclophilin 18 ligands.ACS Med Chem Lett. 2010;1: 536-9. doi (link): https://doi.org/10.1021/ml1001272
16. Hausch F. Protein Targeting with Small Molecules: Chemical Biology Techniques and Applications. Edited by Hiroyuki Osada. ChemBioChem. 2010; 11: 434–435. doi (link): https://doi.org/10.1002/cbic.200900770

2009

15. Kozany C, März A, Kress C, Hausch F.Fluorescent probes to characterise FK506-binding proteins. Chembiochem. 2009; 10: 1402-10. doi (link): https://doi.org/10.1002/cbic.200800806
14. Laenger A, Lang-Rollin I, Kozany C, Zschocke J, Zimmermann N, Ruegg J, Holsboer F, Hausch F, Rein T. (2009) XAP2 inhibits glucocorticoid receptor activity in mammalian cells. FEBS Lett, 589, 1493-8.

2008

13. Hausch F, Becker CFW. EMBL Conference on Chemical Biology 2008. ChemBioChem. 2008; 9: 3083–3086. doi (link): https://doi.org/10.1002/cbic.200800711
12. Hausch F. Betablocker in Aktion: die Struktur des β2-Adrenozeptors im Kristall. Angew Chemie. 2008; 120: 3360–3362. doi (link): https://doi.org/10.1002/ange.200705971

2005

11. Hausch F, Jaeschke A. (2005) Trendbericht Organische Chemie 2004: Biokombinatorische Chemie. Nachrichten aus der Chemie, 53, 251-72.

2004

10. Middendorp O, Lüthi U, Hausch F, Barberis A. Searching for the most effective screening system to identify cell-active inhibitors of beta-secretase.Biol Chem. 2004; 385: 481-5. doi (link): https://doi.org/10.1515/BC.2004.056

2003

9. Hausch F, Halttunen T, Mäki M, Khosla C. Design, synthesis, and evaluation of gluten peptide analogs as selective inhibitors of human tissue transglutaminase. Chem Biol. 2003;10:225-31. doi (link): https://doi.org/10.1016/S1074-5521(03)00045-0
8. Frauendorf C, Hausch F, Röhl I, Lichte A, Vonhoff S, Klussmann S. Internal 32P-labeling of L-deoxyoligonucleotides.Nucleic Acids Res. 2003; 31: e34. doi (link): https://doi.org/10.1093/nar/gng034

2002

7. Shan L, Molberg Ø, Parrot I, Hausch F, Filiz F, Gray GM, Sollid LM, Khosla C. Structural basis for gluten intolerance in celiac sprue. Science. 2002; 297: 2275-9. doi (link): https://doi.org/10.1126/science.1074129
6. Hausch F, Shan L, Santiago NA, Gray GM, Khosla C. Intestinal digestive resistance of immunodominant gliadin peptides.Am J Physiol Gastrointest Liver Physiol. 2002; 283: G996-G1003. doi (link): https://doi.org/10.1152/ajpgi.00136.2002

2001

5. Hausch F, Jäschke A. Multifunctional dinucleotide analogs for the generation of complex RNA conjugates. Tetrahedron. 2001; 57: 1261–1268. doi (link): https://doi.org/10.1016/S0040-4020(00)01114-5

2000

4. Hausch F, Jäschke A. Multifunctional DNA conjugates for the in vitro selection of new catalysts. Nucleic Acids Res. 2000; 28: E35. doi (link): https://doi.org/10.1093%2Fnar%2F28.8.e35

1999

3. Jäschke A, Frauendorf C, Hausch F. In Vitro Selected Oligonucleotides as Tools in Organic Chemistry. Synlett.; 1999; 6: 825–833. doi: 10.1055/s-1999-2726

1998

2. Hausch F, Jäschke A. A novel carboxy-functionalized photocleavable dinucleotide analog for the selection of RNA catalysts. Tetrahedron Lett. 1998; 39: 6157–6158. doi (link): https://doi.org/10.1016/S0040-4039(98)01265-9

1997

1. Hausch F, Jäschke A. Libraries of multifunctional RNA conjugates for the selection of new RNA catalysts.Bioconjug Chem. 1997; 8: 885-90. doi (link): https://doi.org/10.1021/bc9701151