Mu.Ta.Lig - COST ACTION CA15135

Prof. Christa MÜLLER

14 June 2016


General information

Name: Christa Elisabeth
Surname: Müller
Cell phone number with international prefix: +49 175 296 4872
Country: Germany
Affiliation: University of Bonn, PharmaCenter Bonn, Pharmaceutical Institute, Pharmaceutical Chemistry I, An der Immenburg 4, 53121 Bonn, Germany
Gender: F
Year of the PhD title: 1988
Personal web page:
Previous COST participation: No


List of 10 selected publications within last 5 years

1. Sanjay Bhattarai, Marianne Freundlieb, Jan Pippel, Anne Meyer, Aliaa Abdelrahman, Amelie Fiene, Sang-Yong Lee, Herbert Zimmermann, Gennady G. Yegutkin, Norbert Sträter, Ali El-Tayeb, Christa E. Müller; a-Methylene-ADP (AOPCP) derivatives and analogues: development of potent and selective ecto-5’-nucleotidase (CD73) inhibitors. J. Med. Chem. 2015, 58, 6248-6263.
2. Christa E. Müller; Medicinal chemistry of P2X receptors: Allosteric modulators.

Curr. Med. Chem. 2015, 22, 929-941.

3. Thorsten Gnad, Saskia Scheibler, Ivar von Kügelgen, Camilla Scheele, Ana Kilić, Anja Glöde, Linda S. Hoffmann, Laia Reverte-Salisa, Philipp Horn, Samet Mutlu, Ali El-Tayeb, Mathias Kranz, Winnie Deuther-Conrad, Peter Brust, Martin E. Lidell, Matthias J. Betz, Sven Enerbäck, Jürgen Schrader, Gennady G. Yegutkin, Christa E. Müller, Alexander Pfeifer; Adenosine activates brown adipose tissue and recruits beige adipocytes via A2A receptors. Nature 2014, 516, 395-399.
4. Jin Zhang, Kaihua Zhang, Zhan-Guo Gao, Silvia Paoletta, Dandan Zhang, Gye Won Han, Tingting Li, Limin Ma, Wenru Zhang, Christa E. Müller, Huaiyu Yang, Hualiang Jiang, Vadim Cherezov, Vsevolod Katritch, Kenneth A. Jacobson, Raymond C. Stevens, Beili Wu, Qiang Zhao;
Agonist-bound structure of the human P2Y12 receptor. Nature 2014, 509, 119-122.
5. Kaihua Zhang, Jin Zhang, Zhan-Guo Gao, Dandan Zhang, Lan Zhu, GyeWon Han, Steven M. Moss, Silvia Paoletta, Evgeny Kiselev, Weizhen Lu, Gustavo Fenalti, Wenru Zhang, Christa E. Müller, Huaiyu Yang, Hualiang Jiang, Vadim Cherezov, Vsevolod Katritch, Kenneth A. Jacobson, Raymond C. Stevens, Beili Wu, Qiang Zhao; Structure of the human P2Y12 receptor in complex with an antithrombotic drug. Nature 2014, 509, 115-118.
6. Dominik Thimm, Mario Funke, Anne Meyer, Christa E. Müller; 6-Bromo-8-(4-[3H]methoxy­benzamido)-4-oxo-4H-chromene-2-carboxylic acid: a powerful tool for studying orphan G protein-coupled receptor GPR35. J. Med. Chem. 2013, 56, 7084−7099.
7. Viktor Rempel, Nicole Volz, Franziska Gläser, Martin Nieger, Stefan Bräse, Christa E. Müller;
Antagonists for the orphan G protein-coupled receptor GPR55 based on a coumarin scaffold. J. Med. Chem. 2013, 56, 4798-4810.
 Mario Funke, Dominik Thimm, Anke C. Schiedel, Christa E. Müller; 8-Benzamidochromen-4-one-2-carboxylic acids – potent and selective agonists for the orphan G protein-coupled receptor GPR35. J. Med. Chem. 2013, 56, 5182-5197.
9. Anne Stößel, Miriam Schlenk, Sonja Hinz, Petra Küppers, Jag Heer, Michael Gütschow, Christa E. Müller; Dual targeting of adenosine A2A receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones; J. Med. Chem. 2013, 56, 4580-4596.
10. Younis Baqi, Christa E. Müller; Synthesis of alkyl- and aryl-amino-substituted anthraquinone derivatives by microwave-assisted copper(0)-catalyzed Ullmann coupling reactions. Nat. Protocols 2010, 5, 945-953.


Main skills and expertise (up to 5)

1.      Synthesis of heterocyclic compounds, nucleosides and nucleotides
2.      Assay development, e.g., for G protein-coupled receptors and enzymes (ectonucleotidases, phosphatases, kinases)
3.      Molecular biology: expression of proteins in mammalian and insect cells; mutagenesis
4.      Drug development
5.      Prodrugs, fluorescent labeled compounds, radioligands, caged compounds


Main equipment/facilities available in the participants’ lab (up to 5)

1.      NMR 500 + 600 MHz
2.      LCMS instruments (Q-Tof, triple quadrupole), capillary electrophoresis instruments
3.      Professionally organized proprietary compound library with liquid handling system
4.      Synthesis labs, cell culture, radioactive lab, molecular biology lab
5.      qPCR, fluorimeters, high throughput screening station

Short personal activity proposal for the COST Action CA15135 (max 1000 characters)

Projects on the development of multi-target drugs


Alzheimer’s and Parkinson’s disease

We will continue our project on the development of compounds that block adenosine A2A receptors and inhibit monoamine oxidase B (MAO-B) for the treatment of Parkinson’s and Alzheimer’s disease. Additional effects on other relevant targets are investigated, e.g. A1 receptor blockade, COMT inhibition etc.


Immunotherapy of cancer

Another project focuses on the development of dual A2A/A2B receptor antagonists for the immunotherapy of cancer. The first selective A2A antagonists are in clinical trials for this indication. Dual A2A/A2B antagonists are expected to are more effective in reversing the inhibition of the immune system and in fighting cancer cells.




Work Group preference: score from 1 (preferred) to 4 (not preferred)

Work Group of the CA15135 COST Action Score
WG1: Development of new chemical entities x
WG2: Selection of biological targets and assessment of biological data x
WG3: Development of chemical databases x
WG4: Development of Computational methods for multiple ligand design and discovery