The target landscape of clinical kinase drugs

Author:

Klaeger Susan123ORCID,Heinzlmeir Stephanie123ORCID,Wilhelm Mathias1ORCID,Polzer Harald234,Vick Binje235ORCID,Koenig Paul-Albert6ORCID,Reinecke Maria123,Ruprecht Benjamin1,Petzoldt Svenja123,Meng Chen1,Zecha Jana123,Reiter Katrin234ORCID,Qiao Huichao1,Helm Dominic1ORCID,Koch Heiner123,Schoof Melanie1,Canevari Giulia7,Casale Elena7,Depaolini Stefania Re7,Feuchtinger Annette8,Wu Zhixiang1ORCID,Schmidt Tobias1ORCID,Rueckert Lars9,Becker Wilhelm9ORCID,Huenges Jan9,Garz Anne-Kathrin2310,Gohlke Bjoern-Oliver2311ORCID,Zolg Daniel Paul1,Kayser Gian12ORCID,Vooder Tonu131415ORCID,Preissner Robert2311,Hahne Hannes1,Tõnisson Neeme1415ORCID,Kramer Karl1,Götze Katharina2310,Bassermann Florian2310ORCID,Schlegl Judith16ORCID,Ehrlich Hans-Christian9ORCID,Aiche Stephan9ORCID,Walch Axel8,Greif Philipp A.234,Schneider Sabine1718ORCID,Felder Eduard Rudolf7ORCID,Ruland Juergen236ORCID,Médard Guillaume1ORCID,Jeremias Irmela2519,Spiekermann Karsten234ORCID,Kuster Bernhard1231820ORCID

Affiliation:

1. Chair of Proteomics and Bioanalytics, Technical University of Munich (TUM), Freising, Germany.

2. German Cancer Consortium (DKTK), Heidelberg, Germany.

3. German Cancer Research Center (DKFZ), Heidelberg, Germany.

4. Department of Internal Medicine III, University Hospital, Ludwig-Maximilians-Universität (LMU) München, Munich, Germany.

5. Department of Apoptosis in Hematopoietic Stem Cells, Helmholtz Center Munich, German Center for Environmental Health (HMGU), Munich, Germany.

6. Institut für Klinische Chemie und Pathobiochemie, TUM, Munich, Germany.

7. Oncology, Nerviano Medical Sciences Srl, Milan, Italy.

8. Research Unit Analytical Pathology, Helmholtz Zentrum München, Neuherberg, Germany.

9. SAP SE, Potsdam, Germany.

10. Department of Medicine III, Klinikum rechts der Isar, TUM, Munich, Germany.

11. Structural Bioinformatics Group, Charité-Universitätsmedizin, Berlin, Germany.

12. Institute of Surgical Pathology, University Medical Center Freiburg, Faculty of Medicine, University of Freiburg, Freiburg, Germany.

13. Center of Thoracic Surgery, Krefeld, Germany.

14. Estonian Genome Center, University of Tartu, Tartu, Estonia.

15. Tartu University Hospital, Tartu, Estonia.

16. SAP SE, Walldorf, Germany.

17. Department of Chemistry, TUM, Garching, Germany.

18. Center For Integrated Protein Science Munich (CIPSM), Munich, Germany.

19. Department of Pediatrics, Dr von Hauner Children’s Hospital, LMU, Munich, Germany.

20. Bavarian Biomolecular Mass Spectrometry Center (BayBioMS), TUM, Freising, Germany.

Abstract

An atlas for drug interactions Kinase inhibitors are an important class of drugs that block certain enzymes involved in diseases such as cancer and inflammatory disorders. There are hundreds of kinases within the human body, so knowing the kinase “target” of each drug is essential for developing successful treatment strategies. Sometimes clinical trials can fail because drugs bind more than one target. Yet sometimes off-target effects can be beneficial, and drugs can be repurposed for treatment of additional diseases. Klaeger et al. performed a comprehensive analysis of 243 kinase inhibitors that are either approved for use or in clinical trials. They provide an open-access resource of target summaries that could help researchers develop better drugs, understand how existing drugs work, and design more effective clinical trials. Science , this issue p. eaan4368

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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