Publications

2019
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. 2019 Jun 7:e12758.
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. MBio. 2019 May 21;10(3). pii: e00326-19.
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 KH, 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 U S A. 2019 Jun 4;116(23):11370-11379.
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 Chem Int Ed Engl. 2019 May 17. doi: 10.1002/anie.201902994.
66. Hähle A, Merz S, Meyners C, Hausch F. The Many Faces of FKBP51. Biomolecules. 2019 Jan 21;9(1). pii: E35.

Publications

2018
65. Kolos JM, Voll AM, Bauder M, Hausch F. FKBP Ligands-Where We Are and Where to Go? Front Pharmacol. 2018 Dec 5;9:1425.
64. Pöhlmann ML, Häusl AS, Harbich D, Balsevich G, Engelhardt C, Feng X, Breitsamer M, Hausch F, Winter G, Schmidt MV. Pharmacological Modulation of the Psychiatric Risk Factor FKBP51 Alters Efficiency of Common Antidepressant Drugs. Front Behav Neurosci. 2018 Nov 12;12:262.
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. 2018 Oct;62(1):116-128.
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. Chemogenomisches Profiling von humanen und mikrobiellen FK506-bindenden ProteinenJ Med Chem. 2018 Apr 26;61(8):3660-3673.
61. Maiarù M, Morgan OB, Mao T, Breitsamer M, Bamber H, Pöhlmann M, Schmidt MV, 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 Jul;159(7):1224-1234.
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 MV (2017) Stress-responsive FKBP51 regulates AKT2-AS160 signaling and metabolic function.
Nat Commun. 23;8(1)
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. (2017) A regulatory role for the co-chaperone FKBP51s in PD-L1 expression in glioma. Oncotarget 68291-68304
58. Hausch F. (2017) Cryo-EM Structures of Class B GPCR Reveal the Activation Mechanism. Angew Chem Int Ed Engl.12412-12414.
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 (2017) The Hsp90 machinery facilitates the transport of diphtheria toxin into human cells. Sci Rep 7, 613
56. Richers J, Pöthig A, Herdtweck E, Sippel C, Hausch F, Tiefenbacher K (2017) Synthesis and Neurotrophic Activity Studies of Illicium Sesquiterpene Natural Product Analogues. Chemistry, 23, 3178-83

2016
55. Gaali S, Feng X, Haehle A, Sippel C, Bracher A, Hausch F(2016) Rapid, structure-based exploration of pipecolic acid amides as novel selective antagonists of the FK506-binding protein 51. J Med Chem, 59, 2410-22.
54. Maiaru M, Tochiki KK, Cox MB, Annan AV, Bell CG, Feng X, Hausch F, Geranton S (2016) The stress regulator FKBP51 drives chronic pain by modulating spinal glucocorticoid signaling. Sci Transl Med, 10, 325ra19.
53. T. Kirmeier, R. Gopalakrishnan, V. Gormanns, A.M. Werner, S. Cuboni, G.C. Rudolf, G. Höfner, K.T. Wanner, S.A. Sieber, F. Holsboer, T. Rein, F. Hausch (2016) Azidobupramine, an Antidepressant-Derived Bifunctional Neurotransmitter Transporter Ligand Allowing Covalent Labeling and Attachment of Fluorophores. PLoS One, 11, e0148608.
52. Feng X, Pomplun X, Hausch F (2016) Recent progress in FKBP ligand development. Curr Mol Pharm, 9, 27-36.
 

2015
51. Feng X, Sippel C, Bracher A, Hausch F (2015) Structure-Affinity Relationship Analysis of Selective FKBP51 Ligands. J Med Chem, 58, 7796-806.
50. Romano S, Xiao Y, Nakaya M, D’Angelillo A, Chang M, Jin J, Hausch F, Romano MF, Sun S-C (2015) FKBP51 employs both scaffold and isomerase functions to promote NF-κB activation in melanoma. Nucleic Acids Res, 43, 6983-93.
49. Hartmann J, Wagner KV, Gaali S, Kirschner K, Kozany C, Rühter G, Hoeijmakers L, Westerholz S, Uhr M, Chen A, Holsboer F, Hausch F, Schmidt MV (2015) Pharmacological inhibition of the psychiatric risk factor FKBP51 has anxiolytic properties. J Neurosci, 35, 9007-16
48. Navarro G, Quiroz C, Moreno D, Sierakowiak A, McDowell K, Rea W, Moreno E, Howell LA, Hausch F, CortesA, Mallol J, Casado V, Lluis C, Canela E, Ferre S*, McCormick PJ (2015) Orexin‐CRF receptor heteromers in the ventral tegmental area as targets for cocaine. J Neurosci, 29, 6639-53.
47. Hausch F (2015) FKBPs and their role in neuronal signaling. Biochim Biophys Acta, S0304-4165.
46. Kohl C, Wang XD, Grosse J, Fournier C, Harbich D, Westerholz S, Li JT, Bacq A, Sippel C, Hausch F, Sandi C, Schmidt MV (2015) Hippocampal neuroligin-2 links early-life stress with impaired social recognition and increased aggression in adult mice. Psychoneuroendocrinology, 55, 128-43.
45. Riebold M, Kozany C, Buchfelder M, Freiburger L, Sattler M, Hausch F, Stalla GK, Paez–Pereda M (2015) C–terminal Hsp90 inhibitors restore glucocorticoid sensitivity and relieve a mouse allograft model of Cushing’s disease. Nat Med, 21, 276-80.
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 MV, Touma C, Bracher A, Hausch F (2015) Selective inhibitors for the psychiatric risk factor FKBP51 enabled by an induced-fit mechanism. Nat Chem Biol, 11, 33-37.
43. Pomplun S, Wang Y, Kirschner A, Kozany C, Bracher A, Hausch F (2015) Rationales Design und asymmetrische Synthese potenter neuritotropher Liganden für FK506-bindende Proteine. Angew Chem, 1, 352-5; Rational design and asymmetric synthesis of potent and neurotrophic FKBP ligands. Angew Chem Int Ed, 54, 345-8.

2014
42. Cuboni S, Devigny C, Hoogeland B, Straßer A, Pomplun S, Hauger B, Eder M, Buschauer A, Holsboer F, Hausch F (2014) Loratadine and analogs: Discovery and SAR of inhibitors of the amino acid transporter B0AT2. J Med Chem, 57, 9743-9.
41. Bischoff M, Sippel C, Bracher A, Hausch F (2014) Stereoselective Construction of the 5-Hydroxy Diazabicyclo-[4.3.1]decane-2-one Scaffold, a Privileged Motif for FK506-Binding Proteins. Org Lett, 16, 5254-7.
40. Labermaier C, Kohl C, Hartmann J, Devigny C, Altmann A, Weber P, Arloth J, Quast C, Wagner KV, Scharf SH, Czibere L, Widner-Andrä R, Brenndörfer J, Landgraf R, Hausch F, Jones KA, Müller MB, Uhr M, Holsboer F, Binder EB, Schmidt MV (2014) A polymorphism in the Crhr1 gene determines stress vulnerability in male mice. Endocrinology, 155, 2500-10.
39. Cuboni S, Hausch F (2014) Schnappschuss von Antidepressiva bei der Arbeit: die Struktur von Neurotransmittertransporter-Proteinen. Angew Chem, 126, 5108–9; Snapshot of Antidepressants at Work: The Structure of Neurotransmitter Transporter Proteins. Angew Chem Int Ed, 53, 5008-9.
38. Albu S, Romanowski CPN, Curzi ML, Jakubcakova V, Flachskamm C, Gassen NC, Hartmann J, Schmidt MV, Schmidt U, Rein T, Holsboer F, Hausch F, Paez-Pereda M, Kimura M (2014) Deficiency of FK506-binding protein (FKBP) 51 alters sleep architecture and recovery sleep responses to stress in mice. J Sleep Res, 23, 176-85.


2013
37. Hausch F (2013) Strukturen der G-Protein-gekoppelten Rezeptoren der Klasse B: Perspektiven für die Arzneimittelforschung. Angew Chem, 125, 13017-9; Structures of Class B G Protein-Coupled Receptors: Prospects for Drug Discovery. Angew Chem Int Ed, 52, 12785-5.
36. Bracher A, Kozany C, Hähle A, Wild P, Zacharias M, Hausch F (2013) Crystal Structures of the Free and Ligand-Bound FK1-FK2 Domain Segment of FKBP52 Reveal a Flexible Inter-Domain Hinge. J Mol Biol, 425, 4134-44.
35. Hausch F, Kozany C, Theodoropoulou M, Fabian A-K (2013) FKBPs and the Akt/mTOR pathway. Cell Cycle, 12, 2366-70.
34. Quast C, Cuboni C, Bader D,Altmann A, Weber P, Arloth J, Röh S, Brückl T, Ising M, Kopczak A, Erhardt A, Hausch F, Lucae S, Binder EB (2013) Functional coding variants in SLC6A15, a possible risk gene for major depression. PLoS One, 8, e68645.
33. Wang Y, Kirschner A, Fabian AK, Gopalakrishnan R, Kress C, Hoogeland B, Koch U, Kozany C, Bracher A, Hausch F (2013) Increasing the Efficiency of Ligands for FK506-Binding Protein 51 by Conformational Control. J Med Chem, 56, 3922-35.
32. Fabian A-F, Neimanis S, Biondi RM, März AM, Kozany C, Hausch F (2013) InterAKTions with FKBPs – Mutational and pharmacological exploration. PLoS One, 8, e57508.
31. März AM, Fabian A-F, Kozany C, Bracher A, Hausch F (2013) Large FK506-binding Proteins Shape the Pharmacology of Rapamycin. Mol Cell Biol, 33, 1357-67.

2012
30. Hausch F, Holsboer F. (2012) Die sieben Säulen der molekularen Pharmakologie: GPCR-Forschung mit Chemie-Nobelpreis geehrt. Angew Chem, 124, 12338-41. The Seven Pillars of Molecular Pharmacology: GPCR Research Honored with Nobel Prize for Chemistry. Angew Chem Int Ed, 51, 12172-5.
29. Hausch F, Holsboer F. (2012) Structural biology: Snapshot of an activated peptide receptor. Nature, 490, 492-3.
28. Hartmann J, Wagner KV, Dedic N, Marinescu D, Scharf SH, Wang XD, Deussing JM, Hausch F, Rein T, Schmidt U, Holsboer F, Müller MB, Schmidt MV. (2012) Fkbp52 heterozygosity alters behavioral, endocrine and neurogenetic parameters under basal and chronic stress conditions in mice. Psychoneuroendocrinology, 27, 2009-21.
27. Schmidt MV, Paez-Pereda M, Holsboer F, Hausch F. (2012) The Prospect of FKBP51 as a Drug Target. ChemMedChem, 7, 1351-9.
26. Gopalakrishnan R, Kozany C, Wang Y, Schneider S, Hoogeland B, Bracher A, Hausch F. (2012) Exploration of Pipecolate Sulfonamides as Binders of the FK506-Binding Proteins 51 and 52. J Med Chem, 55, 4123-31.
25. Gopalakrishnan R, Kozany C, Gaali S, Kress C, Hoogeland B, Bracher A, Hausch F. (2012) Evaluation of Synthetic FK506 Analogs as Ligands for the FK506-Binding Proteins 51 and 52. J Med Chem, 55, 4114-22.
24. Hartmann J, Wagner KV, Liebl C, Scharf SH, Wang XD, Wolf M, Hausch F, Rein T, Schmidt U, Touma C, Cheung-Flynn J, Cox MB, Smith DF, Holsboer F, Muller MB, Schmidt MV. (2012) The involvement of FK506-binding protein 51 (FKBP5) in the behavioral and neuroendocrine effects of chronic social defeat stress. Neuropharmacology, 62, 332-9.

2011
23. Touma C, Gassen NC, Herrmann L, Cheung-Flynn J, Büll DR, Ionescu IA, Heinzmann JM, Knapman A, Siebertz A, Depping AM, Hartmann J, Hausch F, Schmidt MV, Holsboer F, Ising M, Cox MB, Schmidt U, Rein T. (2011) FK506 Binding Protein 5 Shapes Stress Responsiveness: Modulation of Neuroendocrine Reactivity and Coping Behavior. Biol Psychiatry, 70, 928-36.
22. Gaali S, Gopalakrishnan R, Wang Y, Kozany C, Hausch F. (2011) The Chemical Biology of Immunophilin Ligands. Curr Med Chem, 18, 5355-79.
21. Graber M, Janczyk W, Sperl B, Elumalai N, Kozany C, Hausch F, Holak TA, Berg T. (2011) Selective Targeting of Disease-Relevant Protein Binding Domains by O-Phosphorylated Natural Product Derivatives. ACS Chem Biol, 6, 1008-14.
20. Devigny C, Perez-Balderas F, Hoogeland B, Cuboni S, Wachtel R, Mauch CP, Webb KJ, Deussing JM, Hausch F. (2011) Biomimetic screening of class-B g protein-coupled receptors. J Am Chem Soc, 133, 8927-33.
19. Bracher A, Kozany C, Thost AK, Hausch F. (2011) Structural characterization of the PPIase domain of FKBP51, a cochaperone of human Hsp90. Acta Crystallogr D Biol Crystallogr 67, 549-59.
18. Paez-Pereda M, Hausch F, Holsboer F. (2011) Corticotropin releasing factor receptor antagonists for major depressive disorder. Expert Opin Investig Drugs, 20, 519-35.

2010
17. Gaali S, Kozany C, Hoogeland B, Klein M, Hausch F. (2010) Facile Synthesis of a Fluorescent Cyclosporin A Analogue To Study Cyclophilin 40 and Cyclophilin 18 Ligands. ACS Med Chem Lett, 1, 536-539.
16. Hausch F. (2010) Protein Targeting with Small Molecules: Chemical Biology Techniques and Applications. ChemBioChem, 11, 434-5.


2009
15. Kozany C, März A, Kress C, Hausch, F. (2009) Fluorescent Probes to Characterise FK506-Binding Proteins. ChemBioChem, 10, 1402-10.
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 CF. (2008) EMBL conference on Chemical Biology 2008. ChemBioChem, 9, 3083-3086.
12. Hausch F. (2008) Betablocker in Aktion: die Struktur des β2-Adrenozeptors im Kristall. Angew Chem, 120, 3360-2. Betablockers at work: the crystal structure of the beta2-adrenergic receptor. Angew Chem Int Ed, 47, 3314-6.

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. (2004) Searching for the most effective screening system to identify cell-active inhibitors of beta-secretase. Biol Chem, 385, 481-5.

2003
9. Hausch F, Haltunnen T, Mäki M, Khosla C. (2003) Design, synthesis, and evaluation of gluten peptide analogs as selective inhibitors of human tissue transglutaminase. Chem Biol, 10, 225-31.
8. Frauendorf C+, Hausch F+, Rohl I, Lichte A, Vonhoff S, Klussmann S. (2003) Internal 32P-labeling of L-deoxyoligonucleotides. Nucleic Acids Res, 31, e34. (+ equal contributions)

2002
7. Shan L, Molberg O, Parrot I, Hausch F, Filiz F, Gray GM, Sollid LM, Khosla C. (2002) Structural basis for gluten intolerance in celiac sprue. Science, 297, 2275-9.
6. Hausch F, Shan L, Santiago A, Gray GM, Khosla C. (2002) Intestinal digestive resistance of immunodominant gliadin peptides. Am J Physiol Gastrointest Liver Physiol, 283, G996-G1003.

2001
5. Hausch F, Jäschke A. (2001) Multifunctional dinucleotide analogs for the generation of complex RNA conjugates. Tetrahedron, 57, 1261-8.

2000
4. Hausch F, Jäschke A. (2000) Multifunctional DNA conjugates for the in vitro selection of new catalysts. Nucleic Acids Res, 28, e35.

1999
3. Jäschke A, Frauendorf C, Hausch F. (1999) In Vitro Selected Oligonucleotides as Tools in Organic Chemistry. Synlett, 6, 825-33.

1998
2. Hausch F, Jäschke A. (1998) A novel carboxy-functionalized photocleavable dinucleotide analog for the selection of RNA catalysts. Tetrahedron Lett, 39, 6157-8.

1997
1. Hausch F, Jäschke A. (1997) Libraries of multifunctional RNA conjugates for the selection of new RNA catalysts. Bioconjugate Chem, 8, 885-90.

Accepted patents:
8. Y. Wang, F. Hausch; Bicyclic aza-amides for treatment of psychiatric disorders; Max-Planck-Gesellschaft, US14/416,604 (granted 23.5.2016).
7. F. Hausch, F. Perez-Balderas; Screening method for GPCR ligands; Max-Planck-Gesellschaft, US8623606 (granted 7.1.2014).
6. L. Shan, C. Khosla, F. Hausch, G. Gray. Enzyme Treatment of Foodstuffs for Celiac Sprue. Stanford University, AU2008202964 (granted 16.6.2011).
5. F. Hausch, G. Gray, L. Shan, C. Khosla. Methods for diagnosing celiac sprue and reagents useful therein. Stanford University, US7923532 (12.4.2011).
4. C. Khosla, F. Hausch; Drug Therapy for Celiac Sprue; Stanford University, US7605150 (granted 20.10.2009).
3. F. Hausch, L. Shan, G. Gray, C. Khosla. Enzyme Treatment of Foodstuffs for Celiac Sprue. Stanford University, US7303871 (4.12.2007), AU2003215272 (4.3.2008), US7910541 (22.3.2011), EP1572127 (13.4.2011), US7928056 (19.4.2011), US7943312 (17.5.2011), US8962545 (24.2.2015).
2. F. Hausch, A. Jäschke. (2006) Multiplex sequence variation analysis of DNA samples by mass spectrometry. Bruker Saxonia Analytik GmbH, Germany, DE10015797 (2.2.2006), EP1138782 (20.10.2010).
1. T. Wenzel, T. Fröhlich, A. Jäschke, M. Kostrzewa, F. Hausch. Mutation analysis by mass spectrometry using photolytically cleavable primers. Bruker Saxonia Analytik GmbH, Germany, US7160680 (9.1.2007), DE10108453 (20.10.2005).