Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity.
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
27 10 2022
27 10 2022
Historique:
pubmed:
8
10
2022
medline:
29
10
2022
entrez:
7
10
2022
Statut:
ppublish
Résumé
LIM domain kinases 1 and 2 (LIMK1 and LIMK2) regulate actin dynamics and subsequently key cellular functions such as proliferation and migration. LIMK1 and LIMK2 phosphorylate and inactivate cofilin leading to increased actin polymerization. As a result, LIMK inhibitors are emerging as a promising treatment strategy for certain cancers and neurological disorders. High-quality chemical probes are required if the role of these kinases in health and disease is to be understood. To that end, we report the results of a comparative assessment of 17 reported LIMK1/2 inhibitors in a variety of
Identifiants
pubmed: 36205722
doi: 10.1021/acs.jmedchem.2c00751
pmc: PMC9619402
doi:
Substances chimiques
Actin Depolymerizing Factors
0
Actins
0
Lim Kinases
EC 2.7.11.1
LIMKi3
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
13705-13713Subventions
Organisme : Medical Research Council
ID : MR/S005331/1
Pays : United Kingdom
Références
Drug Discov Today. 2019 Nov;24(11):2111-2115
pubmed: 31278990
Oncotarget. 2012 Jun;3(6):629-39
pubmed: 22776759
Biochem J. 2019 Nov 15;476(21):3197-3209
pubmed: 31652302
Virchows Arch. 2018 May;472(5):727-737
pubmed: 29352327
Cell. 2002 Jan 25;108(2):233-46
pubmed: 11832213
Nat Chem Biol. 2015 Aug;11(8):536-41
pubmed: 26196764
Biochim Biophys Acta. 2014 Jan;1842(1):99-106
pubmed: 24184715
Int J Cancer. 2019 Mar 15;144(6):1345-1355
pubmed: 30006972
Int J Neuropsychopharmacol. 2020 Dec 29;23(12):821-836
pubmed: 32827213
Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5671-6
pubmed: 23509247
ACS Med Chem Lett. 2014 Nov 24;6(1):84-8
pubmed: 25589936
Oncotarget. 2017 Jun 20;8(25):41749-41763
pubmed: 28445157
Med Res Rev. 2012 Sep;32(5):968-98
pubmed: 22886629
Biochim Biophys Acta. 2014 Dec;1842(12 Pt A):2500-9
pubmed: 25315299
Sci Signal. 2016 Jun 07;9(431):ra58
pubmed: 27273096
Mol Cancer. 2011 Jun 18;10:75
pubmed: 21682918
Mol Cancer Ther. 2015 Jan;14(1):246-58
pubmed: 25344584
J Int Med Res. 2012;40(3):1067-73
pubmed: 22906279
Cells. 2022 Jan 02;11(1):
pubmed: 35011704
Mol Cancer Ther. 2008 Nov;7(11):3490-8
pubmed: 19001433
Biomed Pharmacother. 2015 Feb;69:96-101
pubmed: 25661344
J Mol Med (Berl). 2007 Jun;85(6):555-68
pubmed: 17294230
Brain Inj. 2021 Mar 21;35(4):490-500
pubmed: 33523710
ACS Med Chem Lett. 2014 Aug 07;6(1):53-7
pubmed: 25589930
J Neurosci. 2006 Jun 14;26(24):6533-42
pubmed: 16775141
Nature. 1998 Jun 25;393(6687):809-12
pubmed: 9655398
Cancer Lett. 2019 Apr 28;448:182-196
pubmed: 30716360
Sci Signal. 2019 Jun 25;12(587):
pubmed: 31239325
Zebrafish. 2009 Dec;6(4):433-9
pubmed: 20047470
J Med Chem. 2009 Nov 12;52(21):6515-8
pubmed: 19831390
Cell Death Dis. 2018 Jul 3;9(7):749
pubmed: 29970879
Oncol Res. 2013;20(11):491-8
pubmed: 24063279
J Med Chem. 2015 Feb 26;58(4):1846-61
pubmed: 25621531