Editorial: An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2

Joachim Jose (1) , Marc Le-Borgne (2) , Lorenzo Pinna , Mathias Montenarh (3)

1 WWU - Westfälische Wilhelms-Universität Münster = University of Münster
2 B2MC - Molécules bioactives et chimie médicinale
3 Saarland University [Saarbrücken]

participated. After the opening lecture by Lorenzo A. Pinna, Padova, Italy, entitled Exploring the CK2 Paradox: Restless, Dangerous, Dispensable, the scientists reported their latest research on the structural characterization of CK2, hence leading directly to the development of CK2 inhibitors. The driving force behind the development of inhibitors is their use in the treatment of various diseases, which was the next topic of the conference. New findings on protein kinase CK2 were addressed in the following session. The final topic of the conference addressed the role of CK2 in differentiation and development. Lorenzo A. Pinna reminded everybody that the original name " casein kinase " was changed to protein kinase CK2 nearly 20 years ago, because casein did not appear to be among the natural substrates of CK2 [1]. Furthermore, CK2 has now been validated as a " druggable " kinase, which is targeted, in particular, in cancer cells. The most exciting news in this field was the establishment of viable CK2α −/− ,α' −/− cells by CRISPR/cas9 technology and the subsequent phosphoproteome analysis of these non-neoplastic CK2α −/− ,α' −/− cells. Various crystallographic structures of the full-length as well as truncated version of CK2α are already published. The group of Karsten Niefind analysed CK2α and CK2α' in complex with ATP-competitive inhibitors [2]. This structural information not only provided further information about the ATP binding pocket, the interaction of individual residues in the polypeptide chain of both catalytic subunits with the inhibitors, and structural deformation of the enzymes, but also offered new elements for the design of more selective and potent inhibitors. Starting approximately at the beginning of this century, there is an increasing list of inhibitors of CK2 comprising different chemical entities. Some of these are natural products, or compounds identified in drug libraries as well as molecules identified by an in silico approach, followed by chemical synthesis. Georgio Cozza compiled these different approaches to find more potent inhibitors of human CK2 [3]. Some of these approaches are based on crystallographic information about CK2 alone or in complex with an inhibiting compound. History has shown that inhibitors, which were considered initially to be CK2 specific, later on turned out to target multiple kinases. It is now clear

Domaines: Chimie thérapeutique; Biochimie, Biologie Moléculaire; Biologie cellulaire; Cancer

Joachim Jose, Marc Le-Borgne, Lorenzo Pinna, Mathias Montenarh. Editorial: An Updated View on an Emerging Target: Selected Papers from the 8th International Conference on Protein Kinase CK2. Pharmaceuticals, 2017, Pharmaceuticals, 10 ((2)33), pp.33 - 33. ⟨10.3390/ph10020033⟩. ⟨hal-01683242⟩