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Second-generation CK2α inhibitors targeting the αD pocket.

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Iegre J, Brear P, De Fusco C, Yoshida M, Mitchell SL, Rossmann M, Carro L, Sore HF, Hyvönen M, Spring DR
OpenAccess logo Chem Sci 9 3041-3049 (2018)

Cited: 17 times
EuropePMC logo PMID: 29732088

Abstract

CK2 is a critical cell cycle regulator that also promotes various anti-apoptotic mechanisms. Development of ATP-non-competitive inhibitors of CK2 is a very attractive strategy considering that the ATP binding site is highly conserved among other kinases. We have previously utilised a pocket outside the active site to develop a novel CK2 inhibitor,

Articles - 6ehk mentioned but not cited (2)

  1. Second-generation CK2α inhibitors targeting the αD pocket. Iegre J, Brear P, De Fusco C, Yoshida M, Mitchell SL, Rossmann M, Carro L, Sore HF, Hyvönen M, Spring DR. Chem Sci 9 3041-3049 (2018)
  2. Proposed Allosteric Inhibitors Bind to the ATP Site of CK2α. Brear P, Ball D, Stott K, D'Arcy S, Hyvönen M. J Med Chem 63 12786-12798 (2020)


Reviews citing this publication (2)

  1. Targeting Protein Kinases in Blood Cancer: Focusing on CK1α and CK2. Spinello Z, Fregnani A, Quotti Tubi L, Trentin L, Piazza F, Manni S. Int J Mol Sci 22 3716 (2021)
  2. Recent Advances in the Discovery of CK2 Allosteric Inhibitors: From Traditional Screening to Structure-Based Design. Chen X, Li C, Wang D, Chen Y, Zhang N. Molecules 25 E870 (2020)

Articles citing this publication (13)

  1. Efficient development of stable and highly functionalised peptides targeting the CK2α/CK2β protein-protein interaction. Iegre J, Brear P, Baker DJ, Tan YS, Atkinson EL, Sore HF, O' Donovan DH, Verma CS, Hyvönen M, Spring DR. Chem Sci 10 5056-5063 (2019)
  2. 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 1. Identification of an Allosteric Binding Site. Bestgen B, Krimm I, Kufareva I, Kamal AAM, Seetoh WG, Abell C, Hartmann RW, Abagyan R, Cochet C, Le Borgne M, Engel M, Lomberget T. J Med Chem 62 1803-1816 (2019)
  3. Diacritic Binding of an Indenoindole Inhibitor by CK2α Paralogs Explored by a Reliable Path to Atomic Resolution CK2α' Structures. Lindenblatt D, Nickelsen A, Applegate VM, Hochscherf J, Witulski B, Bouaziz Z, Marminon C, Bretner M, Le Borgne M, Jose J, Niefind K. ACS Omega 4 5471-5478 (2019)
  4. 2-Aminothiazole Derivatives as Selective Allosteric Modulators of the Protein Kinase CK2. 2. Structure-Based Optimization and Investigation of Effects Specific to the Allosteric Mode of Action. Bestgen B, Kufareva I, Seetoh W, Abell C, Hartmann RW, Abagyan R, Le Borgne M, Filhol O, Cochet C, Lomberget T, Engel M. J Med Chem 62 1817-1836 (2019)
  5. From a MMP2/CK2 multitarget approach to the identification of potent and selective MMP13 inhibitors. Pastor M, Zapico JM, Coderch C, Maslyk M, Panchuk R, de Pascual-Teresa B, Ramos A. Org Biomol Chem 17 916-929 (2019)
  6. Identification and Biological Evaluation of CK2 Allosteric Fragments through Structure-Based Virtual Screening. Li C, Zhang X, Zhang N, Zhou Y, Sun G, Zhao L, Zhong R. Molecules 25 E237 (2020)
  7. Mining anion-aromatic interactions in the Protein Data Bank. Kuzniak-Glanowska E, Glanowski M, Kurczab R, Bojarski AJ, Podgajny R. Chem Sci 13 3984-3998 (2022)
  8. A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1. Tsuyuguchi M, Nakaniwa T, Sawa M, Nakanishi I, Kinoshita T. Acta Crystallogr F Struct Biol Commun 75 515-519 (2019)
  9. Crystal structure of the Rho-associated coiled-coil kinase 2 inhibitor belumosudil bound to CK2α. Brear P, Hyvönen M. Acta Crystallogr F Struct Biol Commun 78 348-353 (2022)
  10. Mechanism of CK2 Inhibition by a Ruthenium-Based Polyoxometalate. Fabbian S, Giachin G, Bellanda M, Borgo C, Ruzzene M, Spuri G, Campofelice A, Veneziano L, Bonchio M, Carraro M, Battistutta R. Front Mol Biosci 9 906390 (2022)
  11. Structural analysis of fungal pathogenicity-related casein kinase α subunit, Cka1, in the human fungal pathogen Cryptococcus neoformans. Ong BX, Yoo Y, Han MG, Park JB, Choi MK, Choi Y, Shin JS, Bahn YS, Cho HS. Sci Rep 9 14398 (2019)
  12. A fragment-based approach leading to the discovery of inhibitors of CK2α with a novel mechanism of action. Brear P, De Fusco C, Atkinson EL, Iegre J, Francis-Newton NJ, Venkitaraman AR, Hyvönen M, Spring DR. RSC Med Chem 13 1420-1426 (2022)
  13. Development of small cyclic peptides targeting the CK2α/β interface. Atkinson EL, Iegre J, D'Amore C, Brear P, Salvi M, Hyvönen M, Spring DR. Chem Commun (Camb) 58 4791-4794 (2022)


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