A promiscuous kinase inhibitor delineates the conspicuous structural features of protein kinase CK2a1.
ATP-analogue inhibitor
off-target kinases
protein kinase CK2
selectivity
structural comparison
Journal
Acta crystallographica. Section F, Structural biology communications
ISSN: 2053-230X
Titre abrégé: Acta Crystallogr F Struct Biol Commun
Pays: United States
ID NLM: 101620319
Informations de publication
Date de publication:
01 Jul 2019
01 Jul 2019
Historique:
received:
22
05
2019
accepted:
22
06
2019
entrez:
9
7
2019
pubmed:
10
7
2019
medline:
14
1
2020
Statut:
ppublish
Résumé
Protein kinase CK2a1 is a serine/threonine kinase that plays a crucial role in the growth, proliferation and survival of cells and is a well known target for tumour and glomerulonephritis therapies. Here, the crystal structure of the kinase domain of CK2a1 complexed with 5-iodotubercidin (5IOD), an ATP-mimetic inhibitor, was determined at 1.78 Å resolution. The structure shows distinct structural features and, in combination with a comparison of the crystal structures of five off-target kinases complexed with 5IOD, provides valuable information for the development of highly selective inhibitors.
Identifiants
pubmed: 31282872
pii: S2053230X19008951
doi: 10.1107/S2053230X19008951
pmc: PMC6613443
doi:
Substances chimiques
Protein Kinase Inhibitors
0
5-iodotubercidin
24386-93-4
CSNK2A1 protein, human
EC 2.7.11.1
Casein Kinase II
EC 2.7.11.1
Protein Serine-Threonine Kinases
EC 2.7.11.1
Tubercidin
M351LCX45Y
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
515-519Références
Acta Crystallogr D Biol Crystallogr. 2010 Jan;66(Pt 1):22-5
pubmed: 20057045
Cancer Res. 2010 Dec 15;70(24):10288-98
pubmed: 21159648
Bioorg Med Chem Lett. 2016 Feb 1;26(3):955-958
pubmed: 26733474
Methods Enzymol. 1997;276:307-26
pubmed: 27754618
Angew Chem Int Ed Engl. 2018 Jun 11;57(24):7220-7224
pubmed: 29601130
Acta Crystallogr D Biol Crystallogr. 2010 Apr;66(Pt 4):486-501
pubmed: 20383002
Acta Crystallogr D Biol Crystallogr. 2010 Feb;66(Pt 2):213-21
pubmed: 20124702
Biochem Biophys Res Commun. 2008 Dec 26;377(4):1123-7
pubmed: 18983981
Chem Sci. 2018 Feb 20;9(11):3041-3049
pubmed: 29732088
Trends Biochem Sci. 2011 Feb;36(2):65-77
pubmed: 20971646
Proc Natl Acad Sci U S A. 2005 May 24;102(21):7736-41
pubmed: 15897466
Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20198-203
pubmed: 19918057
Biochim Biophys Acta. 2008 Jan;1784(1):33-47
pubmed: 17931986
Bioorg Med Chem Lett. 2009 Jun 1;19(11):2920-3
pubmed: 19414254
Acta Crystallogr D Biol Crystallogr. 2011 Apr;67(Pt 4):355-67
pubmed: 21460454
Biochem J. 1994 Apr 1;299 ( Pt 1):123-8
pubmed: 8166629
Biochem Biophys Res Commun. 2006 Aug 4;346(3):840-4
pubmed: 16782058
Nat Struct Biol. 1999 Dec;6(12):1100-3
pubmed: 10581548
Science. 1988 Jun 17;240(4859):1648-52
pubmed: 3381086
Bioorg Med Chem Lett. 2009 Dec 1;19(23):6557-60
pubmed: 19857964
Chem Biol. 2011 Aug 26;18(8):966-75
pubmed: 21867912
J Synchrotron Radiat. 2013 Nov;20(Pt 6):974-9
pubmed: 24121351