Horst Kessler

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Horst Kessler (2010)

Horst Kessler (born April 5, 1940 in Suhl ) is a German chemist and professor at the Technical University of Munich .

Life

Horst Kessler was born as the son of Walter and Gertrude Kessler, b. Heym, born. He attended school in Suhl from 1946 to 1958 and studied chemistry at the University of Leipzig from 1958 to 1961 . Then he moved to the University of Tübingen , where he worked as an academic student of Eugen Müller preparing his thesis in 1963 and 1966 with the work catalyzed copper salt reactions of diazomethane with aromatics doctorate was. Three years later he was in Organic Chemistry with a thesis on the detection of internal molecular motions by NMR spectroscopy habilitation . He was briefly a university lecturer in Tübingen before he was appointed to the chair for organic chemistry at the University of Frankfurt am Main in 1971 . In 1989 he moved to the Technical University of Munich as Professor of Organic Chemistry and Biochemistry , where he was also Dean of the Faculty of Chemistry, Biology and Geosciences from 1994 to 1996 . Visiting professorships took him to Dalhousie University , Halifax in 1975 , to the University of Tokyo in 1985 , to the University of Wisconsin – Madison in 1988 , to Technion , Haifa in 1990 , to the University of Texas at Austin in 1997 and to the Hebrew University of Jerusalem in 1998 . Since October 2008 he has been Carl von Linde Professor (Emeritus Professor of Excellence) at the Institute for Advanced Study (IAS) at the Technical University of Munich.

In 1964 Kessler married Elke Wiebach, with whom he has three children.

plant

Kessler works in the field of bio-organic chemistry and nuclear magnetic resonance spectroscopy (NMR). With NMR spectroscopy he has succeeded in determining the structure of medically important macromolecules in aqueous solutions, such as cyclosporine , tacrolimus , phallotoxin , substance P and sirolimus . He also devoted himself to cyclic peptides , which can be used as drugs, for coating implants or for molecular imaging. Target structures are e.g. B. the so-called integrins , whose function is essential for all multicellular organisms, because they tell the cells in which cell structure they are. The different integrin subtypes are therefore responsible for many functions in the healthy organism and also play a major role in almost all types of cancer.

With Ernest Eliel and Gerhard Binsch he introduced the term topomerization and topomer in 1971 .

Selection of scientific publications

Kessler has published 766 scientific papers to date and is the inventor or co-inventor of 36 patents.

  • H. Kessler: Detection of Hindered Rotation and Inversion by NMR Spectroscopy , Angew. Chem. Int. Ed. 1970, 9, 219-235. Intramolecular mobility by NMR spectroscopy; many works from the early period are listed here.
  • H. Kessler: Conformation and Biological Activity of Cyclic Peptides , Angew. Chem. Int. Ed. 1982, 21, 512–523.– First presentation of the importance of conformationally restricted peptides (cyclization) for super activity and selectivity. This is a commonly used principle today.
  • HR Loosli, H. Kessler, H. Oschkinat, HP Weber, TJ Petcher, A. Widmer: The Conformation of Cyclosporin A in the Crystal and in Solution , Helv. Chim. Acta 1985, 68, 682–704.– First NOE-based structure (simultaneous and independent of Kurt Wüthrich's small protein BUSI).
  • F. Hagn, L. Eisoldt, J. Hardy, C. Vendrely, M. Coles, T. Scheibel, H. Kessler: A highly conserved spider silk domain acts as a molecular switch that controls fiber assembly , Nature 2010, 465, 239 –242.– NMR-based structure elucidation of the C-terminal domain of spider silk. She explains how the spider manages to store a protein in high concentration and then in less than a second produces the spider silk, which is 5 times stronger than a steel rope of the same strength.
  • C. Mas-Moruno, F. Rechenmacher, H. Kessler: Cilengitide: the first anti-angiogenic small molecule drug candidate. Design, synthesis and clinical evaluation, Anti-Cancer Agents , Medicinal Chemistry 2010, 10, 753–768.– Description of the design, synthesis and biological application of the drug Cilengitide, a cyclic pentapeptide that is highly active and selective to the integrin αvβ3 binds.
  • U. Hersel, C. Dahmen, H. Kessler: RGD modified polymers: biomaterials for stimulated cell adhesion and beyond; Biomaterials 2003, 24, 4385–4415.– Use of RGD peptides for coating biomaterials.
  • S. Neubauer, F. Rechenmacher, AJ Beer, F. Curnis, K. Pohle, C. D´Alessandria, H.-J. Wester, U. Reuning, A. Corti, M. Schwaiger, H. Kessler: Selective imaging of the angiogenic relevant integrins α5β1 and αvβ3 , Angew Chem. Int. Ed. 2013, 52, 11656-11659.
  • OV Maltsev, U. Kiran Marelli, TG Kapp, FS Di Leva, S. Di Maro, M. Nieberler, U. Reuning, M. Schwaiger, E. Novellino, L. Marinelli, H. Kessler: Stable Peptides Instead of Stapled Peptides : Highly Potent αvβ6-Selective Integrin Ligands , Angew. Chem. Int. Ed. 2016, 55, 1535–1538.– Selective recognition of integrins, which are expressed on different tumors, with the help of positron emission tomography (PET).
  • E. Biron, J. Chatterjee, O. Ovadia, D. Langenegger, J. Brueggen, D. Hoyer, H. Schmid, R. Jelinek, C. Gilon, A. Hoffman, H. Kessler: Improving Oral Bioavailability of Peptides by Multiple N-Methylation: Somatostatin Analogues , Angew. Chem Int. Ed. 2008, 47 (14), 2595-2599.– First conversion of a bioactive, but not orally available peptide into an orally available bioactive peptide by means of multiple N -methylation.
  • M. Weinmüller, F. Rechenmacher, U. Kiran Marelli, F. Reichart, TG Kapp, AFBräder, FS Di Leva, L. Marinelli, E. Novellino, JM Muñoz ‑ Félix, K. Hodivala ‑ Dilke, A. Schumacher, J. Fanous, C. Gilon, A. Hoffman, H. Kessler: Overcoming the lack of oral availability of cyclic hexapeptides: Design of a new selective and orally available ligand for the integrin αvβ3 , Angew. Chem. Int. Ed. 2017, 56, 16405–16409.– Targeted design of an orally available biologically active RGD peptide.

Awards and honors

Kessler has been a member of the Bavarian Academy of Sciences since 1996 and of the German Academy of Sciences Leopoldina since 2002 .

  • 2009 Honorary Member of the Nuclear Magnetic Resonance Society in India
  • 2010 honorary member of the specialist group magnetic resonance spectroscopy of the GDCh
  • 2012 Akabori Memorial Award from the Japanese Peptide Society
  • 2013 Roche-Meienhofer Award
  • 2015 Endowed Murray Goodman Lecture
  • 2015 Bruce Merrifield Award from the American Peptide Society

literature

Web links

Individual evidence

  1. ↑ Life data, publications and academic family tree of Horst C. Kessler at academictree.org, accessed on February 15, 2018.
  2. ↑ C. Mas-Moruno, F. Rechenmacher, H. Kessler: Cilengitide: The First Anti-Angiogenic Small Molecule Drug Candidate. Design, Synthesis and Clinical Evaluation In: Anti-Cancer Agents in Medicinal Chemistry ; 10, 2010, pp. 753-768, PMID 21269250 .
  3. ↑ Binsch, Eliel, Kessler, A Nomenclature for Intramolecular Exchange Processes, Angewandte, Chemie, Volume 83, 1971, p. 618.
  4. ↑ Member entry of Horst Kessler (with picture and CV) at the German Academy of Natural Scientists Leopoldina , accessed on July 15, 2016.
personal data
SURNAME Kessler, Horst
BRIEF DESCRIPTION German chemist
DATE OF BIRTH April 5, 1940
PLACE OF BIRTH Suhl