Publications
ETH Publications (2003 – 2019)
1. Original articles
99. Kuzniewski, C. N.; Glauser, S.; Gaugaz, F. Z.; Schiess, R.; Vetterli, S.; Rodríguez-Salarichs, J.; Gertsch, J.; Redondo-Horcajo, M.; Horlacher, O. P.; Canales, A.; Jimenez-Barbero, J.; Díaz, J. F. Synthesis, Profiling and Bioactive Conformation of trans-Cyclopropyl Epothilones. Helv. Chim. Acta 2019, accepted for publication. Published online as an Accepted Article: external page http://dx.doi.org/10.1002/hlca.201900078.
98. de Asís Balaguer, F.; Mühlethaler T.; Estévez-Gallego, J.; Calvo, E.; Giménez-Abián, J. F.; Risinger, A. L.; Sorensen E. J.; Vanderwal, C. D.; Altmann, K.-H.; Mooberry, S. L.; Steinmetz, M. O.; Oliva, M. A.; Prota, A. E.; Díaz, J. F. Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands. Int. J. Mol. Sci. 2019, 20, 1392; external page http://dx.doi.org/10.3390/ijms20061392.
97. Gaugaz, F. Z.; Chicca, A.; Redondo-Horcajo, M.; Barasoain, I.; Díaz, J. F.; Altmann, K.-H. Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate. Int. J. Mol. Sci. 2019, 20, 1113; external page https://doi.org/10.3390/ijms20051113.
96. Schrof, R.; Altmann, K.-H. Studies toward the Total Synthesis of the Marine Macrolide Salarin C. Org. Lett. 2018, 20, 7679-7683.
95. Foo, C.; Lupien, A.; Kienle, M.; Vocat A.; Benjak, A.; Sommer, R.; Lamprecht, D.; Steyn, A.; Pethe, K.; Piton, J.; Altmann, K.-H.; Cole, S.; Arylvinylpiperazine amides, a new class of potent inhibitors targeting QcrB of Mycobacterium tuberculosis. mBio 2018, 9:e01276-18. external page https://doi.org/10.1128/mBio.01276-18.
94. Häfliger, P.; Rubin, M.; Stooss, A.; Gertsch, J.; Charles R.-P.; Graff, J.; Altmann, K.-H.; Dettmer, M. S. The LAT1 inhibitor JPH203 reduces growth of thyroid carcinoma in a fully immunocompetent mouse model. J. Exp. Clin. Cancer Res. 2018, 37, 234; external page https://doi.org/10.1186/s13046-018-0907-z.
93. Menchon, G.; Prota, A. E.; Lucena-Agell, D.; Bucher, P.; Jansen, R.; Irschik, H.; Müller, R.; Paterson, I.; Díaz, J. F.; Altmann, K.-H.; Steinmetz, M. O. A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin. Nature Commun. 2018, 9, 2106. external page https://www.nature.com/articles/s41467-018-04535-8.
92. Jackson, S. M.; Manolaridis I.; Kowal, I.; Zechner, M.; Taylor N. M. I.; Bause, M.; Bauer, S.; Bartholomäus R.; Bernhardt G.; König, B.; Buschauer, A.; Stahlberg, H.; Altmann, K.-H.; Locher, K. P. Structural basis of small-molecule inhibition of human multidrug transporter ABCG2. Nature Struct. Mol. Biol. 2018, 25, 333-340.
91. Glaus, F.; Dedic, D.; Tare, P.; Nagaraja, V.; Rodrigues, L.; Ainsa, J. A.; Kunze, J.; Schneider, G.; Hartkoorn, R. C.; Cole, S. T.; Altmann, K.-H. Total Synthesis of Ripostatin B and Structure-Activity Relationship Studies on Ripostatin Analogs. J. Org. Chem. 2018, 83, 7150-7172.
90. Field, J. J.; Pera, B.; Gallego, J. E.; Calvo, E.; Rodriguez-Salarichs, J.; Saez-Calvo, G.; Zuwerra, D.; Jordi, M.; Andreu, J. M.; Prota, A. E.; Menchon, G.; Miller, J. H.; Altmann, K.-H.; Díaz, J. F. Zampanolide Binding to Tubulin Indicates Cross-Talk of Taxane Site with Colchicine and Nucleotide Sites. J. Nat. Prod. 2018, 81, 494–505.
89. Chicca, A.; Nicolussi, S.; Bartholomäus, R.; Blunder, M.; Rey, A. A.; Petrucci, V.; del Carmen Reynoso-Moreno, I.; Viveros-Paredes, J. M.; Gens, M. D.; Lutz, B.; Schioth, H. B.; Soeberdt, M.; Abels, C.; Charles, R.-P.; Altmann, K.-H.; Gertsch, J. Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake. Proc. Natl. Acad. Sci. U.S.A. 2017, 114, E5006-E5015.
88. Pillong, M.; Hiss, J. A.; Schneider, P.; Lin, Y.-C.; Posselt, G.; Pfeiffer, B.; Blatter, M.; Müller, A. T.; Bachler, S.; Neuhaus, C. S.; Dittrich, P. S.; Altmann, K.-H.; Wessler, S.; Schneider, G. Rational Design of Membrane-Pore-Forming Peptides. Small 2017, 13, n/a.
87. Stutz, K.; Müller, A. T.; Hiss, J. A.; Schneider, P.; Blatter, M.; Pfeiffer, B.; Posselt, G.; Kanfer, G.; Kornmann, B.; Wrede, P.; Altmann, K.-H.; Wessler, S.; Schneider, G. Peptide-Membrane Interaction between Targeting and Lysis. ACS Chem. Biol. 2017, 12, 2254-2259.
86. Feklistov, A.; Bae, B.; Hauver, J.; Lass-Napiorkowska, A.; Kalesse, M.; Glaus, F.; Altmann, K.-H. Heyduk, T.; Landick, R.; Darst, S. A. RNA polymerase motions during promoter melting. Science 2017, 356, 863-866.
85. Field, J. J.; Northcote, P.; Paterson, I.; Altmann, K.-H.; Miller, J. H.; Díaz, J. F. Zampanolide, a Microtubule-Stabilizing Agent, Is Active in Resistant Cancer Cells and Inhibits Cell Migration. Int. J. Mol. Sci. 2017, 18, 971; external page https://doi.org/10.3390/ijms18050971
84. Bieri, R.; Scherr, N.; Ruf, M.-T.; Dangy, J.-P.; Gersbach, P.; Gehringer, M.; Altmann, K.-H.; Pluschke, G. The Macrolide Toxin Mycolactone Promotes Bim-Dependent Apoptosis in Buruli Ulcer through Inhibition of mTOR. ACS Chemical Biology 2017, 12, 1297-1307.
83. Jantsch, A.; Nieto, L.; Gertsch, J.; Rodriguez-Salarichs, J.; Matesanz, R.; Jimenez-Barbero, J.; Diaz, J. F.; Canales, A.; Altmann, K.-H. Synthesis, biological profiling and determination of the tubulin-bound conformation of 12-aza-epothilones (azathilones). Molecules 2016, 21, 1010/1-1010/26.
82. Schneider, G.; Reker, D.; Chen, T.; Hauenstein, K.; Schneider, P.; Altmann, K.-H. Deorphaning the Macromolecular Targets of the Natural Anticancer Compound Doliculide. Angew. Chem. Int. Ed. 2016, 55, 12408-12411.
81. Wullschleger, C. W.; Li, J.; Edenharter, A.; Altmann, K.-H. Studies towards the Synthesis of Leiodolide A. Synlett 2016, 27, 2726-2730.
80. Dangy, J.-P.; Scherr, N.; Gersbach, P.; Hug, M. N.; Bieri, R.; Huber, S.; Bomio, C.; Li, J.; Altmann, K.-H.; Pluschke, G. Antibody-Mediated Neutralization of the Exotoxin Mycolactone, the Main Virulence Factor Produced by Mycobacterium ulcerans. PLoS Negl. Trop. Dis. 2016, 10, e0004808.
79. Foerster, F.; Chen, T.; Altmann, K.-H.; Vollmar, A. M. Actin-binding doliculide causes premature senescence in p53 wild type cells. Bioorg. Med. Chem. 2016, 24, 123-129.
78. Brütsch, T. M.; Bucher, P.; Altmann, K.-H. Total Synthesis and Biological Assessment of Mandelalide A. Chem. Eur. J. 2016, 22, 1292–1300.
77. Foerster, F.; Chen, T.; Altmann, K.-H.; Vollmar, A. M. Actin-binding doliculide causes premature senescence in p53 wild type cells. Bioorg. Med. Chem. 2016, 24, 123-129.
76. Pera, B.; Calvo-Vidal, M. N.; Ambati, S.; Jordi, M.; Kahn, A.; Diaz, J. F.; Fang, W.; Altmann, K.-H.; Cerchietti, L.; Moore, M. A. S. High affinity and covalent-binding microtubule stabilizing agents show activity in chemotherapy-resistant acute myeloid leukemia cells. Cancer Lett. 2015, 368, 97-104.
75. Lin, Y.-C.; Lim, Y. F.; Russo, E.; Schneider, P.; Bolliger, L.; Edenharter, A.; Altmann, K.-H.; Halin, C.; Hiss, J. A.; Schneider, G. Multidimensional Design of Anticancer Peptides. Angew. Chem. Int. Ed. 2015, 54, 10370-10374.
74. Perna, A. M.; Rodrigues, T.; Schmidt, T. P.; Boehm, M.; Stutz, K.; Reker, D.; Pfeiffer, B.; Altmann, K.-H.; Backert, S.; Wessler, S.; Schneider, G. Fragment-Based De Novo Design Reveals a Small-Molecule Inhibitor of Helicobacter Pylori HtrA. Angew. Chem. Int. Ed. 2015, 54, 10244-10248.
73. Chen, T.; Altmann, K.-H. Directed hydrogenations and an Ireland-Claisen rearrangement linked to Evans-Tishchenko chemistry: The highly efficient total synthesis of the marine cyclodepsipeptide doliculide. Chem. Eur. J. 2015, 21, 8403-8407.
72. Glaus, F.; Altmann, K.-H. Total Synthesis of the Tiacumicin B (Lipiarmycin A3/Fidaxomicin) Aglycone. Angew. Chem. Int. Ed. 2015, 54, 1937-1940.
71. Prota, A. E.; Bargsten, K.; Díaz, J. F.; Marsh, M.; Cuevas, C.; Liniger, M.; Neuhaus, C.; Andreu, J. M.; Altmann, K.-H.; Steinmetz, M. O. A new tubulin-binding site and pharmacophore for microtubule-destabilizing anticancer drugs. Proc. Natl. Acad. Sci. USA 2014, 111, 13817-13821.
70. Gaugaz, F. Z.; Redondo-Horcajo, M.; Barasoain, I.; Díaz, J. F.; Cobos-Correa, Amanda; Kaufmann, M.; Altmann, K.-H. The Impact of Cyclopropane Configuration on the Biological Activity of Cyclopropyl-Epothilones. ChemMedChem 2014, 9, 2227-2232.
69. Marion, E.; Song, O.-R.; Christophe, T.; Babonneau, J.; Fenistein, D.; Eyer, J.; Letournel, F.; Henrion, D.; Clere, N.; Paille, V. Mycobacterial Toxin Induces Analgesia in Buruli Ulcer by Targeting the Angiotensin Pathways. Cell 2014, 157, 1565-1576.
68. Albesa-Jove, D.; Chiarelli, L. R.; Makarov, V.; Pasca, M. R.; Urresti, S.; Mori, G.; Salina, E.; Vocat, A.; Comino, N.; Mohorko, E. Rv2466c Mediates the Activation of TP053 To Kill Replicating and Non-replicating Mycobacterium tuberculosis. ACS Chem. Biol. 2014, 9, 1567-1575.
67. Foerster, F.; Braig, S.; Chen, T.; Altmann, K.-H.; Vollmar, A. M. Pharmacological characterization of actin-binding (-)-doliculide. Bioorg. Med. Chem. 2014, 22, 5117-5122.
66. Canales, A.; Nieto, L.; Rodriguez-Salarichs, J.; Sanchez-Murcia, P. A.; Coderch, C.; Cabrera, A. C.; Paterson, I.; Carlomagno, T.; Gago, F.; Andreu, J. M.; Altmann, K.-H.; Jimenez-Barbero, J.; Diaz, J. F. The molecular recognition of epothilones by microtubules and tubulin dimers revealed by biochemical and NMR approaches. ACS Chemical Biology 2014, 9, 1033-1043.
65. Prota, A. E.; Bargsten, K.; Northcote, P. T.; Marsh, N.; Altmann, K.-H.; Miller, J. H.; Díaz, J. F.; Steinmetz, M. O. Structural basis of microtubule stabilization by laulimalide and peloruside A. Angew. Chem. Int. Ed. 2014, 53, 1621-1625.
64. Hartkoorn, R. C.; Pojer, F.; Read, J. A.; Gingell, H.; Neres, J.; Horlacher, O. P.; Altmann, K.-H.. Cole, S. T. Pyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhA. Nat. Chem. Biol. 2014, 10, 96-98.
63. Evensen, L.; Odlo, K.; Micklem, D. R, Littlewood-Evans, A.; Wood, J.; Kuzniewski, C.; Altmann, K.-H.; Hansen, T. V.; Lorens, J. B. Contextual Compound Screening for Improved Therapeutic Discovery. ChemBioChem 2013, 14, 2512-2518.
62. Liniger, M.; Estermann, K.; Altmann, K.-H. Total Synthesis of Hygrolines and Pseudohygrolines. J. Org. Chem. 2013, 78, 11066-11070.
61. Wullschleger, C. W.; Gertsch, J.; Altmann, K.-H. Synthesis and Biological Activity of 7,8,9-Trideoxy- and 7R Des-THP-Peloruside A. Chemistry Eur. J. 2013, 19, 13105-13111.
60. Neuhaus, C.; Liniger, M.; Stieger, M.; Altmann, K.-H. RCAM-based Total Synthesis of the Tubulin Inhibitor WF-1360F. Angew. Chem. Int. Ed. 2013, 52, 5866-5870.
59. Scherr, N.; Gersbach, P.; Dangy, J.-P.; Bomio, C.; Li, J.; Altmann, K.-H.; Pluschke, G. Structure-Activity Relationship Studies on the Macrolide Exotoxin Mycolactone of Mycobacterium ulcerans. PLOS Neglect. Trop. D. 2013, accepted for publication.
58. Pfeiffer, B.; Speck-Gisler, S.; Barandun, L.; Senft, U.; de Groot, C.; Lehmann, I.; Ganci, W.; Gertsch, J.; Altmann, K.-H. Total Synthesis and Configurational Assignment of the Marine Natural Product Haliclamide. J. Org. Chem. 2013, 78, 2553-2563.
57. Prota, A. E.; Bargsten, K.; Zurwerra, D.; Field, J. J.; Díaz, J. F.; Altmann, K.-H.; Steinmetz, M. O. Molecular Mechanism of Action of Microtubule-Stabilizing Anticancer Agents. Science 2013, 339, 587-590.
56. Horlacher, O.; Haartkorn, R.; Cole, S.; Altmann, K.-H. Synthesis and Antimycobacterial Activity of 2,1-Dihydropyridomycins. ACS Med. Chem. Lett. 2013, 4, 264-268.
55. Hartkoorn, R. C.; Sala, C.; Neres, J.; Pojer, F.; Magnet, S.; Mukherjee, R.; Uplekar, S.; Boy-Roettger, S.; Altmann, K.-H.; Cole, S. T. Towards a new tuberculosis drug: pyridomycin – nature’s isoniazid. EMBO Mol. Med. 2012, 4, 1032-1042.
54. Johannes, M.; Altmann, K.-H. A Ring-Closing Metathesis-based Approach to the Synthesis of (+)-Tetrabenazine. Org. Lett. 2012, 14, 3752-3755.
53. Zurwerra, D.; Glaus, F.; Betschart, L.; Schuster, J.; Gertsch, J.; Ganci, W.; Altmann, K.-H. Total Synthesis of (-)-Zampanolide and Structure–Activity Relationship Studies on (-)-Dactylolide Derivatives. Chem. Eur. J. 2012, 18, 16868-16883.
52. Field, J. J.; Pera, B.; Calvo, E.; Canales, A.; Zurwerra, D.; Trigili, C.; Rodríguez‐Salarichs, J.; Matesanz, R.; Kanakkanthara, A.; Wakefield, St. J.; Singh, A. J.; Jiménez‐Barbero, J.; Northcote, P.; Miller, J. H.; López, J. A.; Hamel, E.; Barasoain, I.; Altmann, K.-H.; Díaz, J. F. Zampanolide, a potent new microtubule stabilizing agent, covalently reacts with the taxane luminal site in both tubulin a,b‐heterodimers and microtubules. Chem. Biol. 2012, 19, 686-698.
51. Glaus, F.; Altmann, K.-H. Total Synthesis of the Bacterial RNA Polymerase Inhibitor Ripostatin B. Angew. Chem. Int. Ed. 2012, 51, 3405-3409.
50. Hartenfeller, M.; Eberle, M.; Meier, P.; Nieto-Oberhuber, C.; Altmann, K.-H.; Schneider, G.; Jacoby, E.; Renner, S. Probing the Bioactivity-Relevant Chemical Space of Robust Reactions and Common Molecular Building Blocks. J. Chem. Inf. Mod. 2012, 52, 1167-1178.
49. Geppert, T.; Bauer, S.; Hiss, J. A.; Conrad, E.; Reutlinger, M.; Schneider, P.; Weisel, M.; Pfeiffer, B.; Altmann, K.-H.; Waibler, Z.; Schneider, G. Immunosuppressive Small Molecule Discovered by Structure-Based Virtual Screening for Inhibitors of Protein-Protein Interactions. Angew. Chem. Int. Ed. 2012, 51, 258-261.
48. Hartenfeller, M.; Eberle, M.; Meier, P.; Nieto-Oberhuber, C.; Altmann, K.-H.; Schneider, G.; Jacoby, E.; Renner, S.; A Collection of Robust Organic Synthesis Reactions for In Silico Molecule Design. J. Chem. Inf. Mod. 2011, 51, 3093-3098.
47. Gersbach, P.; Jantsch, A.; Feyen, F.; Scherr, N.; Dangy, J.-P.; Pluschke, G.; Altmann, K.-H. A Ring-Closing Metathesis (RCM)-Based Approach to Mycolactones A/B. Chemistry Eur. J. 2011, 17, 13017-13031.
46. Nievergelt, A.; Marazzi, J.; Schoop, R.; Altmann, K.-H.; Gertsch, J. Ginger Phenylpropanoids Inhibit IL-1b and Prostanoid Secretion and Disrupt Arachidonate-Phospholipid Remodeling by Targeting Phospholipases A2. J. Immunol.; 2011, 187, 4140-4150.
45. Schuehly, W.; Paredes, J. M. V.; Kleyer, J.; Huefner, A.; Anavi-Goffer, S.; Raduner, S.; Altmann, K.-H.; Gertsch, J. Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB2 Receptor Inverse Agonists. Chem. Biol. 2011, 18, 1053-1064.
44. Schiess, R.; Gertsch, J.; Schweizer, W. B.; Altmann, K.-H. Stereoselective Synthesis of 12,13-Cyclopropyl-Epothilone B and Side-Chain-Modified Variants. Org. Lett. 2011, 13, 1436-1439.
43. Liniger, M.; Neuhaus, C.; Hofmann, T.; Fransioli-Ignazio, L.; Jordi, M.; Drueckes, P.; Trappe, J.; Fabbro, D.; Altmann, K.-H. Kinase Inhibition by Deoxy Analogs of the Resorcylic Lactone L-783277. ACS Med. Chem. Lett. 2011, 2, 22-27.
42. Erdelyi, M.; Navarro-Vazquez, A.; Pfeiffer, B.; Kuzniewski, C. N.; Felser, A.; Widmer, T.; Gertsch, J.; Pera, B.; Diaz, J. F.; Altmann, K.-H.; T. Carlomagno, T. The Binding Mode of Side Chain- and C3-Modified Epothilones to Tubulin. ChemMedChem 2010, 5, 911-920.
41. Nievergelt, A.; Huonker, P.; Schoop, R.; Altmann, K.-H. Identification of serotonin 5-HT1A receptor partial agonists in ginger. Bioorg. Med. Chem. 2010, 18, 3345-3351.
40. Kopp, S.; Baur, R.; Sigel, E.; Moehler, H.; Altmann, K.-H. Highly Potent Modulation of GABAA Receptors by Valerenic Acid Derivatives. ChemMedChem 2010, 5, 678-681.
39. Zurwerra, D.; Gertsch, J.; Altmann, K.-H. Synthesis of (-)-Dactylolide and 13-Desmethylene-(-)-dactylolide and Their Effects on Tubulin. Org. Lett. 2010, 12, 2302-2305.
38. Leonti, M.; Casu, L.; Raduner, S.; Cottiglia, F.; Floris, C.; Altmann, K.-H.; Gertsch, J. Falcarinol is a covalent cannabinoid CB1 receptor antagonist and induces pro-allergic effects in skin. Biochem. Pharmacol. 2010, 79, 1815-1826.
37. Wullschleger, C. W.; Gertsch, J.; Altmann, K.-H.; Stereoselective Synthesis of a Monocyclic Peloruside A Analogue. Org. Lett. 2010, 12, 1120-112.
36. Forli, S.; Manetti, F.; Altmann, K.-H.; Botta, M. Evaluation of Novel Epothilone Analogues by means of a Common Pharmacophore and a QSAR Pseudoreceptor Model for Taxanes and Epothilones. ChemMedChem 2010, 5, 35-40.
35. Lawnicka, H.; Kowalewicz-Kulbat, M.; Sicinska, P.; Altmann, K.-H.; Hofmann, T.; Stepien, H. Resorcylic acid lactone L-783,277 inhibits the growth of the human adrenal cancer cell line H295R in vitro. Int. J. Immunopathol. Pharmacol. 2009, 22, 889-895.
34. Gollner, A.; Altmann, K.-H.; Gertsch, J.; Mulzer, J. Synthesis and biological evaluation of a des-dihydropyran laulimalide analog. Tetrahedron Lett. 2009, 50, 5790-5792.
33. Passarella, D.; Comi, D.; Cappelletti, G.; Cartelli, D.; Gertsch, J.; Quesada, A. R.; Borlak, J.; Altmann, K.-H. Synthesis and biological evaluation of epothilone A dimeric compounds. Bioorg. Med. Chem. 2009, 17, 7435-7440.
32. Gertsch, J.; Feyen, F.; Bützberger, A.; Gerber, B.; Pfeiffer, B.; Altmann, K.-H. Making Epothilones Fluoresce: Design, Synthesis, and Biological Characterization of a Fluorescent N12-Aza-Epothilone (Azathilone). ChemBioChem, 2009, 2513-2521.
31. Chicca, A.; Raduner, S.; Pellati, F.; Strompen, T.; Altmann, K.-H.; Schoop, R.; Gertsch, J. Synergistic immunomopharmacological effects of N-alkylamides in Echinacea purpurea herbal extracts. Int. Immunopharmacol. 2009, 9, 850-858.
30. Dietrich, S.; Lindauer, R.; Stierlin, C.; Gertsch, J.; Matesanz, R.; Notararigo, S.; Díaz, J. F.; Altmann, K.-H. Epothilone Analogs with Benzimidazole and Quinoline Side Chains: Chemical Synthesis, Antiproliferative Activity, and Interactions with Tubulin. Chem. Eur. J. 2009, 10144-10157.
29. Gollner, A.; Altmann, K.-H.; Gertsch, J.; Mulzer, J. Laulimalide Family: Total Synthesis and Biological Evaluation of Neolaulimalide, Isolaulimalide, Laulimalide and a Nonnatural Analogue. Chem. Eur. J. 2009, 15, 5979-5997.
28. Pfeiffer, B.; Hauenstein, K.; Merz, P.; Gertsch, J.; Altmann, K.-H. Synthesis and SAR of C12-C13-oxazoline derivatives of epothilone A. Bioorg. Med. Chem. Lett. 2009, 19, 3760-3763.
27. Kopp, S.; Schweizer, W. B.; Altmann, K.-H. Total synthesis of valerenic acid. Synlett 2009, 1769-1772.
26. Markt, P.; Feldmann, C.; Rollinger, J. M.; Raduner, S.; Schuster, D.; Kirchmair, J.; Distinto, S.; Spitzer, G. M.; Wolber, G.; Laggner, C.; Altmann, K.-H.; Langer, T.; Gertsch, J. Discovery of Novel CB2 Receptor Ligands by a Pharmacophore-Based Virtual Screening Workflow. J. Med. Chem. 2009, 52, 369-378.
25. Benke, D.; Barberis, A.; Kopp, S.; Altmann, K.-H.; Schubiger, M.; Vogt, K. E.; Rudolph, U.; Moehler, H. GABAA receptors as in vivo substrate for the anxiolytic action of valerenic acid, a major constituent of valerian root extracts. Neuropharmacology 2009, 56, 174-181.
24. Gertsch, J.; Meier, S.; Müller, M.; Altmann, K.-H. Differential effects of natural product microtubule stabilizers on microtubule assembly: single agent and combination studies with taxol, epothilone B, and discodermolide. ChemBioChem 2009, 10, 166-175.
23. Hamel, C.; Prusov, E.; Gertsch, J.; Altmann, K.-H. Total synthesis of blumiolide C. Angew. Chem. Int Ed. 2008, 47, 10081-10084.
22. Gertsch, J.; Leonti, M.; Raduner, S.; Racz, I.; Chen,J.–Z.; Xie, X.-Q.; Altmann, K.-H.; M. Karsak, M.; Zimmer, A.; Beta-caryophyllene is a dietary cannabinoid. Proc. Natl. Acad. Sci. USA, 2008, 105, 9099-9104.
21. Feyen, F.; Jantsch, A.; Hauenstein, K.; Pfeiffer, B.; Altmann, K.-H. Synthesis of 12-aza analogs of epothilones and (E)-9,10-dehydroepothilones. Tetrahedron 2008, 64, 7920-7928.
20. Hofmann, T.; Altmann, K.-H.; Total Synthesis of the Resorcylic Lactone-based Kinase Inhibitor L-783277. Synlett 2008, 1500-1504.
19. Kuzniewski, C. N.; Gertsch, J.; Wartmann, M.; Altmann, K.-H. Total Synthesis of Hypermodified Epothilone Analogs with Potent in vitro Antitumor Activity. Org. Lett. 2008, 10, 1183-1186.
18. Erdélyi, M.; Pfeiffer, B.; Hauenstein, K.; Fohrer, J.; Altmann, K.-H.; Carlomagno, T. The Conformational Preferences of Natural and C3-Modified Epothilones in Aqueous Solution. J. Med. Chem. 2008, 51, 1469-1473.
17. Gertsch, J.; Meier, S.; Tschopp, N.; Altmann, K.-H. New tubulin inhibitors from plants: A critical assessment. Chimia 2007, 61, 368-372.
16. Raduner, S.; Bisson, W.; Abagyan, R.; Altmann, K.-H.; Gertsch, J. Self-Assembling Cannabinomimetics: Supramolecular Structures of N-Alkyl Amides. J. Nat. Prod. 2007, 70, 1010-1015.
15. Feyen, F.; Jantsch, A.; Altmann, K.-H. Synthetic Studies on Mycolactones: Synthesis of the Mycolactone Core Structure through Ring-Closing Olefin Metathesis. Synlett 2007, 415-418.
14. Feyen, F.; Gertsch, J.; Wartmann, M.; Altmann, K.-H. Design and synthesis of 12-aza-epothilones (azathilones) – Non-natural natural products with potent anticancer activity. Angew. Chem. Int. Ed. 2006, 45, 5880-5885.
13. Cachoux, F.; Isarno, T.; Wartmann, M.; Altmann, K.-H. Total synthesis and biological assessment of cyclopropane-based epothilone analogues - modulation of drug efflux through polarity adjustments. Synlett 2006, 1384-1388.
12. Pallan, P. S.; von Matt, P.; Wilds, C. J.; Altmann, K.-H.; Egli, M. RNA-Binding Affinities and Crystal Structure of Oligonucleotides Containing Five-Atom Amide-Based Backbone Structures. Biochemistry 2006, 45, 8048-8057.
11. Raduner, S.; Majewska, A.; Chen, J.-Z.; Xie, X-Q.; Hamon, J.; Faller, B.; Altmann, K.-H.; Gertsch, J. Alkylamides from Echinacea Are a New Class of Cannabinomimetics: cannabinoid type 2 receptor-dependent and -independent immunomodulatory effects. J. Biol. Chem. 2006, 281, 14192-14206.
10. Bold, G.; Wojeik, S.; Caravatti, G.; Lindauer, R.; Stierlin, C.; Gertsch, J.; Wartmann, M.; Altmann, K.-H. Structure-activity relationships in side-chain-modified epothilone analogues. How important is the position of the nitrogen atom? ChemMedChem 2006, 1, 37-40.
09. Cachoux, F.; Isarno, T.; Wartmann, M.; Altmann, K.-H. Total synthesis and biological assessment of benzimidazole-based analogues of epothilone A: Ambivalent effects on cancer cell growth inhibition. ChemBioChem 2006, 7, 54-57.
08. Cachoux, F.; Isarno, T.; Wartmann, M.; Altmann, K.-H. Scaffolds for microtubule inhibition through extensive modification of the epothilone template. Angew. Chem. Int. Ed. 2005, 44, 7469-7473.
07. O'Reilly, T.; McSheehy, P. M. J.; Wenger, F.; Hattenberger, M.; Muller, M.; Vaxelaire, J.; Altmann, K.-H.; Wartmann, M. Patupilone (epothilone B, EPO906) inhibits growth and metastasis of experimental prostate tumors in vivo. Prostate 2005, 65, 231-240.
06. O’Reilly, T.; M. Wartmann, M.; Maira, S.-M.; Hattenberger, M.; Vaxelaire, J.; Muller, M.; Buchdunger, E.; Altmann, K.-H.; McSheehy, P. J. M. Patupilone (Epothilone B, EPO906) and imatinib (STI571, Glivec®) in combination display enhanced antitumour activity in vivo against experimental rat C6 glioma. Cancer Chemother. Pharmcol. 2005, 55, 307-317.
05. Cachoux, F.; Schaal, F.; Teichert, A.; Wagner, T.; Altmann, K.-H. Synthesis of 4-aza Epothilone D Analogs. Synlett 2004, 2709-2712.
04. End, N.; Furet, F.; van Campenhout, N.; Wartmann, M.; Altmann, K.-H. Total Synthesis and Biological Evaluation of a C(10)/C(12)-Phenylene-bridged Analog of Epothilone D. Chem. & Biodiversity 2004, 1, 1771-1784.
03. Schinzer, D.; Böhm, O.; Altmann, K.-H.; Wartmann, M. Synthesis and biological evaluation of furano-epothilone C. Synlett 2004, 1375-1378.
02. Koch, G.; Loiseleur, O.; Fuentes, D.; Jantsch, A.; Altmann, K.-H. Total synthesis of 26-fluoro-epothilone B. Synlett 2004, 693-697.
01. Furet, P.; Bold, G.; Hofmann, F.; Manley, P.; Meyer, T.; Altmann, K.-H. Identification of a New Chemical Class of Potent Angiogenesis Inhibitors Based on Conformational Considerations and Database Searching. Bioorg. Med. Chem. Lett. 2003, 13, 2967–297.
2. Review articles
15. Altmann, K.-H. Drugs from the oceans: marine natural products as leads for drug discovery. Chimia 2017, 71, 646-652.
14. Dong, M.; Pfeiffer, B.; Altmann, K.-H. Recent developments in natural product-based drug discovery for tuberculosis. Drug Discov. Today 2017, 22, 585-591.
13. Gehringer, M.; Altmann, K.-H. The chemistry and biology of mycolactones. Beilstein J. Org. Chem. 2017, 13, 1596-1660.
12. Betschart, L.; Altmann, K.-H. Xenicane Natural Products: Biological Activity and Total Synthesis. Curr. Pharm. Des. 2015, 21, 5467-5488.
11. Field, J. J.; Calvo, E.; Northcote, P. T.; Miller, J. H.; Altmann, K.-H.; Díaz, J. F. Methods for studying microtubule binding site interactions: zampanolide as a covalent binding agent. Methods in Cell Biology 2013, 115, 303-325.
10. Altmann, K.-H.; Gaugaz, F. Z.; Schiess, R. Diversity through semisynthesis: The chemistry and biological activity of semisynthetic epothilone derivatives. Molecular Diversity 2011, 15, 383-399.
09. Pfeiffer, B.; Kuzniewski, C. N.; Wullschleger, C.; Altmann, K.-H. Macrolide-Based Microtubule-Stabilizing Agents – Chemistry and Structure–Activity Relationships. Top. Curr. Chem. 2009, 86, 1-72.
08. Feyen, F.; Cachoux, F.; Gertsch, J.; Wartmann, M.; Altmann, K.-H. Epothilones as Lead Structures for the Synthesis-Based Discovery of New Chemotypes for Microtubule Stabilization. Acc. Chem. Res.; 2008, 41, 21-31.
07. Mulzer, J.; Altmann, K.-H.; Höfle, G.; Müller, R.; Prantz, K. Epothilones ‚ A fascinating family of microtubule stabilizing antitumor agents. Compt. Rend.; 2008, 11, 1336-1368.
06. Hofmann, T.; Altmann, K.-H. Resorcylic Acid Lactones as New Lead Structures for Kinase Inhibition. Compt. Rend.; 2008, 11, 1318-1335.
05. Altmann, K.-H.; Gertsch, J. Anticancer drugs from nature – Natural products as a unique source of new microtubule-stabilizing agents. Nat. Prod. Rep. 2007, 24, 327-357.
04. Altmann, K.-H.; Pfeiffer, B.; Arseniyadis, S.; Pratt, B. A.; Nicolaou, K. C. The chemistry and biology of epothilones – the wheel keeps turning. ChemMedChem 2007, 2, 396-423.
03. Gertsch, J.; Raduner, S.; Altmann, K.-H. New natural noncannabinoid ligands for cannabinoid type-2 (CB2) receptors. J. Recept. Sig. Transd. 2006, 26, 709-730.
02. Altmann, K.-H. Recent developments in the chemical biology of epothilones. Curr. Pharm. Des. 2005, 11, 1595-1613.
01. Altmann, K.-H. The Merger between Medicinal Chemistry and Natural Product Synthesis: On the Chemistry and Chemical Biology of Epothilones. Org. Bioorg. Chem. 2004, 2, 2137-2152.
3. Book Chapters
09. Altmann, K.-H., Brütsch, T., Glauser, S. On the Chemistry and Biology of Dactylolide and Zampanolide. In: Chemical Biology of Natural Products, G. M. Cragg, D. J. Newman, P. Grothaus, Eds.; CRC Press, 2017, pp. 555-599.
08. Schiess, R.; Altmann, K.-H. Epothilones. In: RSC Drug Discovery Series 2015, 40 (Macrocycles in Drug Discovery), 78-108.
07. Altmann, K.-H.; Schinzer, D. Chemistry and biology of epothilones. In: Methods and Principles in Medicinal Chemistry 2014, 60 (Natural Products in Medicinal Chemistry), 83-125.
06. Pfeiffer, B.; Gaugaz, F. Z.; Schiess, R.; Altmann, K.-H. Epothilones as Lead Structures for New Anticancer Drugs. In: Drug Discovery from Natural Products, O. Genilloud, F. Vicente, Eds.; RSC Publishing, 2012, pp. 339-373.
05. Altmann, K.-H. Clinical Studies with Epothilones. In: The Epothilones: An Outstanding Family of Anti-Tumor Agents, Progr. Chem. Org. Nat. Prod. 90, A. D. Kinghorn, H. Falk, J. Kobayashi, Eds.; Springer Wien New York, 2009, pp. 221-238.
04. Altmann, K.-H. Preclinical Pharmacology and Structure-Activity Studies of Epothilones. In: The Epothilones: An Outstanding Family of Anti-Tumor Agents, Progr. Chem. Org. Nat. Prod. Vol. 90, A. D. Kinghorn, H. Falk, J. Kobayashi, Eds.; Springer Wien New York, 2009, pp. 157-220.
03. Altmann, K.-H. Semisynthetic Derivatives of Epothilones. In: The Epothilones: An Outstanding Family of Anti-Tumor Agents, Progr. Chem. Org. Nat. Prod. 90, A. D. Kinghorn, H. Falk, J. Kobayashi, Eds.; Springer Wien New York, 2009, pp. 135-156.
02. Altmann K.-H.; Memmert K. Epothilones as lead structures for new anticancer drugs--pharmacology, fermentation, and structure-activity-relationships. In: Progress in Drug Research. Fortschritte der Arzneimittelforschung. Progres des Recherches Pharmaceutiques, F. Petersen, R. Amstutz, Eds.; 2008, 66, pp. 275-334.
01. Altmann, K.-H. The chemistry and biology of epothilones - lead structures for the discovery of improved microtubule inhibitors. In: Medicinal Chemistry of Bioactive Natural Products, X.-T. Liang, W.-S. Fang, Eds.; John Wiley & Sons, Inc.; Hoboken, N. J, 2006, pp. 1-34.
4. Other Relevant Publications
08. Altmann, K.-H. Tumor targeting with small molecule-drug conjugates (SMDCs) - can they be better than ADCs? Chimia 2018, 72, 154-155. (Highlight article).
07. Altmann, K.-H. Bioorg. Med. Chem. 2014, 22, 5038-5039. (Editorial as guest editor of a Symposium-in-Print issue on “The cytoskeleton and its interactions with small molecules”).
06. Glaus, F.; Altmann, K.-H. Total synthesis of the myxobacterial macrolide ripostatin B. Chimia 2013, 67, 227-230. (Invited paper based on a Prize-winning oral presentation of F. Glaus at the Fall Meeting of the SCS 2012).
05. Zurwerra, D.; Wullschleger, C. W.; Altmann, K.-H. Treasures from the Sea: Discovery and Total Synthesis of Ammosamides.”Angew. Chem. Int. Ed. 2010, 49, 6936-6938. (Highlight article).
04. Anthoine Dietrich, S.; Riediker, L.; Gertsch, J.; Altmann, K.-H. Synthesis and biological activity of new functionalized epothilones for prodrug design and tumor targeting. Chimia 2010, 64, 136-139. (Invited paper based on a Prize-winning oral presentation of S. Anthoine Dietrich at the Fall Meeting of the SCS 2009).
03. Altmann, K.-H.; Cachoux, F.; Feyen, F.; Gertsch, J.; Kuzniewski, C. N.; Wartmann, M. Natural products as leads for anticancer drug discovery: discovery of new chemotypes of microtubule stabilizers through reengineering of the epothilone scaffold. Chimia 2010, 64, 8-13. (Invited paper based on a lecture at the Frontiers in Bioorganic Chemistry meeting, Basel, Feb. 2009).
02. Altmann, K.-H.; Neri, D. Curr. Opin. Chem. Biol. 2009, 13, 231-234. (Editorial as guest editors of a journal issue on Next Generation Therapeutics).
01. Altmann, K.-H.; Buchner, J.; Kessler, H.; Diederich, F.; Kräutler, B.; Lippard, S.; Liskamp, R.; Müller, K.; Nolan, E. M.; Samori, B.; Schneider, G.; Schreiber, S. L. Schwalbe, H.; Toniolo, C.; van Boeckel, C. A. A.; Waldmann, H.; Walsh, C. T. The state of the art of chemical biology. ChemBioChem 2009, 10, 16-29. (Editorial on occasion of the 10th anniversary of ChemBioChem).