2009
DOI: 10.1002/med.20164
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How druggable is protein kinase CK2?

Abstract: CK2 is a pleiotropic, ubiquitous, and constitutively active protein kinase (PK), with both cytosolic and nuclear localization in most mammalian cells. The holoenzyme is generally composed of two catalytic (alpha and/or alpha') and two regulatory (beta) subunits, but the free alpha/alpha' subunits are catalytically active by themselves and can be present in cells under some circumstances. CK2 catalyzes the phosphorylation of more than 300 substrates characterized by multiple acidic residues surrounding the phos… Show more

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Cited by 61 publications
(59 citation statements)
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References 199 publications
(201 reference statements)
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“…Further studies are warranted to show evidence for patients who may potentially benefit from CK2 inhibitors. CK2 inhibitors have not been extensively developed as therapeutic agents, partly because the ATP-binding pocket of CK2 is not as druggable as some other protein kinases [44][45][46]. To date, only one small-molecule CK2 inhibitor has been entered to clinical trials as a potential anticancer drug [47].…”
Section: Discussionmentioning
confidence: 99%
“…Further studies are warranted to show evidence for patients who may potentially benefit from CK2 inhibitors. CK2 inhibitors have not been extensively developed as therapeutic agents, partly because the ATP-binding pocket of CK2 is not as druggable as some other protein kinases [44][45][46]. To date, only one small-molecule CK2 inhibitor has been entered to clinical trials as a potential anticancer drug [47].…”
Section: Discussionmentioning
confidence: 99%
“…3B). Several other cell-permeable CK2 inhibitors are available, but the majority of them are less selective than TDB and quinalizarin (39)(40)(41).…”
Section: Otub1 Is a Bona Fide Substrate For Ck2mentioning
confidence: 99%
“…[1,2] Its catalytic subunits (a and/or a') are constitutively active either with or without the regulatory b-subunits, which appear to play a role in targeting and substrate recruiting, rather than controlling catalytic activity. Furthermore, constitutively active CK2 is ubiquitous, essential, and implicated in a wide variety of important cell functions.…”
Section: Introductionmentioning
confidence: 98%