Karl-Heinz Altmann

ETH Zürich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, HCl H405, Vladimir-Prolog-Weg 4, CH-8093, Zürich, Switzerland.

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September 2020

Synthesis and Biological Evaluation of Endocannabinoid Uptake Inhibitors Derived from WOBE437.

Authors:

Patrick Mäder Ruben Bartholomäus Simon Nicolussi Alice Baumann Melanie Weis Andrea Chicca Mark Rau Ana Catarina Simão Jürg Gertsch Karl-Heinz Altmann

ChemMedChem 2021 Jan 26;16(1):145-154. Epub 2020 May 26.

Department of Chemistry and Applied Biosciences, ETH Zürich HCI H405, Vladimir-Prelog-Weg 4, 8093, Zürich, Switzerland.

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January 2021

Ammonia uptake by transmembrane pH gradient poly(isoprene)-block-poly(ethylene glycol) polymersomes.

Authors:

Aaron C Schmidt Erik R Hebels Charlotte Weitzel Barbara Stoessel Yinyin Bao Karl-Heinz Altmann Jean-Christophe Leroux

Soft Matter 2020 Mar;16(11):2725-2735

Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Zurich, 8093 Zurich, Switzerland.

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March 2020

Synthesis and Structure-Activity Relationship Studies of C2-Modified Analogs of the Antimycobacterial Natural Product Pyridomycin.

Authors:

Maryline Kienle Patrick Eisenring Barbara Stoessel Oliver P Horlacher Samuel Hasler Gwénaëlle van Colen Ruben C Hartkoorn Anthony Vocat Stewart T Cole Karl-Heinz Altmann

J Med Chem 2020 02 21;63(3):1105-1131. Epub 2020 Jan 21.

Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences , ETH Zürich , 8093 Zurich , Switzerland.

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February 2020

Taxanes convert regions of perturbed microtubule growth into rescue sites.

Authors:

Ankit Rai Tianyang Liu Simon Glauser Eugene A Katrukha Juan Estévez-Gallego Ruddi Rodríguez-García Wei-Shuo Fang J Fernando Díaz Michel O Steinmetz Karl-Heinz Altmann Lukas C Kapitein Carolyn A Moores Anna Akhmanova

Nat Mater 2020 03 9;19(3):355-365. Epub 2019 Dec 9.

Cell Biology, Neurobiology and Biophysics, Department of Biology, Faculty of Science, Utrecht University, Utrecht, the Netherlands.

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March 2020

Total Synthesis of the Endocannabinoid Uptake Inhibitor Guineensine and SAR Studies.

Authors:

Ruben Bartholomäus Simon Nicolussi Alice Baumann Mark Rau Ana Catarina Simão Jürg Gertsch Karl-Heinz Altmann

ChemMedChem 2019 09 23;14(17):1590-1596. Epub 2019 Aug 23.

Department of Chemistry and Applied Biosciences, ETH Zürich, HCI H405, Vladimir-Prelog-Weg 4, 8093, Zürich, Switzerland.

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September 2019

Configurationally Stabilized Analogs of Exotoxins Mycolactones A and B Reveal the Importance of Side Chain Geometry for Mycolactone Virulence.

Authors:

Matthias Gehringer Patrick Mäder Philipp Gersbach Bernhard Pfeiffer Nicole Scherr Jean-Pierre Dangy Gerd Pluschke Karl-Heinz Altmann

Org Lett 2019 08 11;21(15):5853-5857. Epub 2019 Jul 11.

Swiss Federal Institute of Technology (ETH) Zürich , Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences , Vladimir-Prelog-Weg 4 , 8093 Zürich , Switzerland.

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August 2019

Crystal Structure of the Cyclostreptin-Tubulin Adduct: Implications for Tubulin Activation by Taxane-Site Ligands.

Authors:

Francisco de Asís Balaguer Tobias Mühlethaler Juan Estévez-Gallego Enrique Calvo Juan Francisco Giménez-Abián April L Risinger Erik J Sorensen Christopher D Vanderwal Karl-Heinz Altmann Susan L Mooberry Michel O Steinmetz María Ángela Oliva Andrea E Prota J Fernando Díaz

Int J Mol Sci 2019 Mar 20;20(6). Epub 2019 Mar 20.

Structural and Chemical Biology Department. Centro de Investigaciones Biológicas, CSIC, Ramiro de Maeztu 9, 28040 Madrid, Spain.

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March 2019

Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate.

Authors:

Fabienne Zdenka Gaugaz Andrea Chicca Mariano Redondo-Horcajo Isabel Barasoain J Fernando Díaz Karl-Heinz Altmann

Int J Mol Sci 2019 Mar 5;20(5). Epub 2019 Mar 5.

ETH Zürich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, 8093 Zürich, Switzerland.

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March 2019

Studies toward the Total Synthesis of the Marine Macrolide Salarin C.

Authors:

Raffael Schrof Karl-Heinz Altmann

Org Lett 2018 12 26;20(23):7679-7683. Epub 2018 Nov 26.

Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences , ETH Zürich , Vladimir-Prelog-Weg 4 , CH-8093 Zürich , Switzerland.

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December 2018

Arylvinylpiperazine Amides, a New Class of Potent Inhibitors Targeting QcrB of Mycobacterium tuberculosis.

Authors:

Caroline S Foo Andréanne Lupien Maryline Kienle Anthony Vocat Andrej Benjak Raphael Sommer Dirk A Lamprecht Adrie J C Steyn Kevin Pethe Jérémie Piton Karl-Heinz Altmann Stewart T Cole

mBio 2018 10 9;9(5). Epub 2018 Oct 9.

Global Health Institute, École Polytechnique Fédérale de Lausanne, Lausanne, Switzerland

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October 2018

Primary resistance mechanism of the canine distemper virus fusion protein against a small-molecule membrane fusion inhibitor.

Authors:

David Kalbermatter Neeta Shrestha Nadine Ader-Ebert Michael Herren Pascal Moll Richard K Plemper Karl-Heinz Altmann Johannes P Langedijk Flavio Gall Urs Lindenmann Rainer Riedl Dimitrios Fotiadis Philippe Plattet

Virus Res 2019 01 5;259:28-37. Epub 2018 Oct 5.

Division of Experimental and Clinical Research, Vetsuisse Faculty, University of Bern, CH-3001, Bern, Switzerland. Electronic address:

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January 2019

The LAT1 inhibitor JPH203 reduces growth of thyroid carcinoma in a fully immunocompetent mouse model.

Authors:

Pascal Häfliger Julien Graff Matthias Rubin Amandine Stooss Matthias S Dettmer Karl-Heinz Altmann Jürg Gertsch Roch-Philippe Charles

J Exp Clin Cancer Res 2018 Sep 21;37(1):234. Epub 2018 Sep 21.

Institute of Biochemistry and Molecular Medicine, and Swiss National Center of Competence in Research (NCCR) TransCure, University of Bern, Bühlstrasse 28, CH-3012, Bern, Switzerland.

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September 2018

A fluorescence anisotropy assay to discover and characterize ligands targeting the maytansine site of tubulin.

Authors:

Grégory Menchon Andrea E Prota Daniel Lucena-Agell Pascal Bucher Rolf Jansen Herbert Irschik Rolf Müller Ian Paterson J Fernando Díaz Karl-Heinz Altmann Michel O Steinmetz

Nat Commun 2018 05 29;9(1):2106. Epub 2018 May 29.

Laboratory of Biomolecular Research, Division of Biology and Chemistry, Paul Scherrer Institut, Villigen PSI, 5232, Switzerland.

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May 2018

Tumor Targeting with Small Molecule-Drug Conjugates (SMDCs) - Can They be Better than ADCs?

Authors:

Karl-Heinz Altmann

Chimia (Aarau) 2018 Mar;72(3):154-155

ETH Zurich, Department of Chemistry and Applied Biosciences, HCI H405, Vladimir-Prelog-Weg 4, CH-8093 Zurich;, Email:

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March 2018

Structural basis of small-molecule inhibition of human multidrug transporter ABCG2.

Authors:

Scott M Jackson Ioannis Manolaridis Julia Kowal Melanie Zechner Nicholas M I Taylor Manuel Bause Stefanie Bauer Ruben Bartholomaeus Guenther Bernhardt Burkhard Koenig Armin Buschauer Henning Stahlberg Karl-Heinz Altmann Kaspar P Locher

Nat Struct Mol Biol 2018 04 2;25(4):333-340. Epub 2018 Apr 2.

Institute of Molecular Biology and Biophysics, Department of Biology, ETH Zurich, Zurich, Switzerland.

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April 2018

Total Synthesis of Ripostatin B and Structure-Activity Relationship Studies on Ripostatin Analogs.

Authors:

Florian Glaus Darija Dedić Priyanka Tare Valakunja Nagaraja Liliana Rodrigues José Antonio Aínsa Jens Kunze Gisbert Schneider Ruben C Hartkoorn Stewart T Cole Karl-Heinz Altmann

J Org Chem 2018 07 29;83(13):7150-7172. Epub 2018 Mar 29.

Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences , ETH Zürich , 8092 Zürich , Switzerland.

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July 2018

Drugs from the Oceans: Marine Natural Products as Leads for Drug Discovery.

Authors:

Karl-Heinz Altmann

Chimia (Aarau) 2017 Oct;71(10):646-652

Department of Chemistry and Applied Biosciences Institute of Pharmaceutical Sciences Vladimir-Prelog-Wag 4 HCI H 405 CH-8093 Zurich;, Email:

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October 2017

Zampanolide Binding to Tubulin Indicates Cross-Talk of Taxane Site with Colchicine and Nucleotide Sites.

Authors:

Jessica J Field Benet Pera Juan Estévez Gallego Enrique Calvo Javier Rodríguez-Salarichs Gonzalo Sáez-Calvo Didier Zuwerra Michel Jordi José M Andreu Andrea E Prota Grégory Ménchon John H Miller Karl-Heinz Altmann J Fernando Díaz

J Nat Prod 2018 03 12;81(3):494-505. Epub 2017 Oct 12.

Centro de Investigaciones Biológicas (CIB) , CSIC , Madrid 28048 , Spain.

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March 2018

The chemistry and biology of mycolactones.

Authors:

Matthias Gehringer Karl-Heinz Altmann

Beilstein J Org Chem 2017 11;13:1596-1660. Epub 2017 Aug 11.

Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zürich, Vladimir-Prelog-Weg 4, 8093 Zürich, Switzerland.

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August 2017

Rational Design of Membrane-Pore-Forming Peptides.

Authors:

Max Pillong Jan A Hiss Petra Schneider Yen-Chu Lin Gernot Posselt Bernhard Pfeiffer Markus Blatter Alex T Müller Simon Bachler Claudia S Neuhaus Petra S Dittrich Karl-Heinz Altmann Silja Wessler Gisbert Schneider

Small 2017 10 11;13(40). Epub 2017 Aug 11.

Department of Chemistry and Applied Biosciences, ETH Zurich, 8093, Zurich, Switzerland.

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October 2017

Peptide-Membrane Interaction between Targeting and Lysis.

Authors:

Katharina Stutz Alex T Müller Jan A Hiss Petra Schneider Markus Blatter Bernhard Pfeiffer Gernot Posselt Gil Kanfer Benoît Kornmann Paul Wrede Karl-Heinz Altmann Silja Wessler Gisbert Schneider

ACS Chem Biol 2017 09 8;12(9):2254-2259. Epub 2017 Aug 8.

Department of Chemistry and Applied Biosciences, Swiss Federal Institute of Technology (ETH) , Vladimir-Prelog-Weg 4, 8093 Zurich, Switzerland.

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September 2017

Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake.

Authors:

Andrea Chicca Simon Nicolussi Ruben Bartholomäus Martina Blunder Alejandro Aparisi Rey Vanessa Petrucci Ines Del Carmen Reynoso-Moreno Juan Manuel Viveros-Paredes Marianela Dalghi Gens Beat Lutz Helgi B Schiöth Michael Soeberdt Christoph Abels Roch-Philippe Charles Karl-Heinz Altmann Jürg Gertsch

Proc Natl Acad Sci U S A 2017 06 5;114(25):E5006-E5015. Epub 2017 Jun 5.

Institute of Biochemistry and Molecular Medicine, National Centre of Competence in Research NCCR TransCure, University of Bern, 3012 Bern, Switzerland;

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June 2017

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