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Group leader

Univ.-Prof. Dr. Dr. h.c. Holger Stark
Institute for Pharmaceutical and Medicinal Chemistry
Heinrich-Heine-University
Universitätsstraße 1
40225 Düsseldorf

Holger Stark is pharmacist by education and made his PhD in Medicinal Chemistry under the supervision of Prof. W. Schunack at the Free University of Berlin, Germany, in 1991 on newly designed prodrugs (BF2.94). During his habilitation at the same university he worked on neurotransmitter ligands, mainly at dopamine and histamine receptor subtypes for the central nervous system. In 2000 he became full professor at the Goethe University in Frankfurt, Germany and went in 2013 to the Heinrich-Heine-University in Düsseldorf, Germany where he has his actual position.

He is founded some start-up companies on cancer therapeutics (Warburg Glycomed, PSites Pharma) and has received several prices for his successful research as well as for teaching. He received in 2016 a honorate docorate from the University of Nis, Serbia. On more than 370 book contributions, original papers, reviews and patents he has focused on neurotransmitter as well as on lipid signaling research. The developments of novel pharmacological tools for imaging and of ligands with designed selectivity are some of the highlights. He is co-inventor of pitolisant (Wakix®), the first histamine H3 receptor antagonist with market approval and has prepared some back-up (pre)clinical candidates in different leads for various targets. From 2004 - 2019 Holger Stark was editor-in-chief of the Archiv der Pharmazie – Chemistry in Life Sciences, one of the oldest journals on Medicinal Chemistry.

Specific Projects
  • Histamine receptor subtype ligands (H3R, H4R)
  • Dopamine receptor subtype ligands (D2R, D3R)
  • Sphingosin cascade modulators at different levels
  • Arachidonic acid modulators
  • Multiple targeting with selected profiles
  • Labeling for visualization (fluorescence, PET etc.)
  • Preclinical profiling of promising candidates
Selected Publications
  1. A. Alachkar, S. K. Ohja, A. Sadeq, A. Adem, A. Frank, H. Stark, and B. Sadek. Experimental Models for Discovery of Novel Anticonvulsant Drugs: Focus on Pentylentetrazole-Induced Seizures and Associated Memory Deficits. Curr. Pharm. Des. 2020;26(15):1693-1711.doi:  10.2174/1381612826666200131105324. PubMed
  2. L. Stank, A. Frank, S. Hagenow, and H. Stark. Talipexole Variations as Novel Bitopic Dopamine D2 and D3 Receptor Ligands.  MedChemComm. 2019, 10, 1926-1929. MedChemComm
  3. A. Frank, F. Meza-Arriagada, C. O. Salas, C. Espinosa-Bustos, and H. Stark. Nature-inspired Pyrrolo[2,3-d]pyrimidines Targeting the Histamine H3 Receptor. 2019 Jul 15;27(14):3194-3200.doi: 10.1016/j.bmc.2019.05.042. PubMed
  4. L. C. Pullen, M. Picone, L. Tan, C. Johnston, and H. Stark. Cognitive Improvements in Children with Prader-Willi Syndrome Following Pitolisant Treatment – Patient Reports. J. Pediatr. Pharmacol. Ther. 2019, 24(2), 166-171. (open access). doi: 10.5863/1551-6776-24.2.166. PubMed
  5. D. Reiner and H. Stark. Ligand Binding Kinetics at Histamine H3 Receptors by Fluorescence-Polarization with Real-time Monitoring. Eur. J. Pharmacol. 2019 Apr 5;848:112-120. doi: 10.1016/j.ejphar.2019.01.041. PubMed
  6. A. P. Morris, T. H. Le, H. Wu, A. Akbarov, P. J. van der Most, G. Hemani, G. D. Smith, A. Mahajan, K. J. Gaulton, G. N. Nadkarni, A. Valladares-Salgado, N. Wacher-Rodarte, J. C. Mychaleckyj, N. D. Dueker, X. Guo, Y. Hai, J. Haessler, Y. Kamatani, A. M. Stilp, G. Zhu, J. P. Cook, J. Arnlov, S. H. Blanton, M. H. de Borst, E. P. Bottinger, T. A. Buchanan, S. Cechova, F. J. Charchar, P.-L. Chu, J. Damman, J. Eales, A. G. Gharavi, V. Giedraitis, A. C. Heath, E. Ipp, K. Kiryluk, M. Kubo, A. Larsson, C. M. Lindgren, Y. Lu, P. A. F. Madden, H. J. Mattix-Kramer, G. W. Montgomery, G. J. Papanicolaou, L. J. Raffel, R. L. Sacco, E. Sanchez, H. Stark, J. Sundstrom, K. D. Taylor, A. H. Xiang, A. Zivkovic, L. Lind, E. Ingelsson, N. G. Martin, J. B. Whitfield, J. Cai, C. C. Laurie, Y. Okada, K. Matsuda, C. Kooperberg, Y.-D. I. Chen, T. Rundek, S. S. Rich, R. J. F. Loos, E. J. Parra, M. Cruz, J. I. Rotter, H. Snieder, M. Tomaszewski, B. D. Humphreys, and N. Franceschini, on behalf of the Continental Origins and Genetic Epidemiology Network (COGENT) Kidney Consortium. Trans-ethnic Kidney Function Association Study Reveals Putative Causal Genes and Effects on Kidney-specific Disease Aetiologies. Nat. Commun. 2019 Jan 3;10(1):29.doi: 10.1038/s41467-018-07867-7. PubMed
  7. P. Chazot, M. Cowart, H. Fukui, C. R. Ganellin, R. Gutzmer, H. L. Haas, S. J. Hill, R. Hills, R. Leurs, R. Levi, S. Liu, P. Panula, W. Schunack, J.-C. Schwartz, R. Seifert, N. P. Shankley, H. Stark, R. Thurmond, H. Timmerman, and J. M. Young. Histamine Receptors (Version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide to Pharmacology CITE. 2019; 2019 (4). IUPHAR/BPS Guide to Pharmacology
  8. A. Frank, D. J. Kiss, G. J. Keserü, and H. Stark. Binding Kinetics of Cariprazine and Aripiprazole at the Dopamine D3 Receptor. Sci. Rep. 2018 Aug 21;8(1):12509.doi: 10.1038/s41598-018-30794-y. PubMed
  9. Ó. M. Bautista-Aguilera, S. Hagenow, A. Palomino-Antolin, V. Farré-Alins, L. Ismaili, P.-L. Joffrin, M. L. Jimeno, O. Soukup, J. Janockova, L. Kalinowsky, E. Proschak, I. Iriepa, I. Moraleda, J. S. Schwed, A. R. Martinez, F. López-Muñoz, M. Chioua, J. Egea*, R. R. Ramsay, J. Marco-Contelles*, and H. Stark*. Multitarget-Directed Ligands Combining Cholinesterase and Monoamine Oxidase Inhibition with Histamine H3R Antagonism for Neurodegenerative Diseases. Angew. Chem. Int. Ed. 2017 Oct 2;56(41):12765-12769.doi: 10.1002/anie.201706072. PubMed
  10. D. Vogt and H. Stark. Therapeutic Strategies and Pharmacological Tools Influencing S1P Signaling and Metabolism. Med. Res. Rev. 2017 Jan;37(1):3-51. doi: 10.1002/med.21402. PubMed
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