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The Nature of Diamino Linker and Halogen Bonding Define Selectivity of Pyrrolopyrimidine-Based LIMK1 Inhibitors

The LIM-domain kinase (LIMK) family consists of two isoforms, LIMK1 and LIMK2, which are highly homologous, making selective inhibitor development challenging. LIMK regulates dynamics of the actin cytoskeleton, thereby impacting many cellular functions including cell morphology and motility. Here, w...

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Principais autores: Daryl Ariawan, Carol Au, Esmeralda Paric, Thomas Fath, Yazi D. Ke, Michael Kassiou, Janet van Eersel, Lars M. Ittner
Format: Artigo
Sprog:Inglês
Udgivet: Frontiers Media S.A. 2021-12-01
Serier:Frontiers in Chemistry
Fag:
LIMK
kinase inhibitor
SAR
cofilin phosphorylation
actin cytoskeleton
Online adgang:https://www.frontiersin.org/articles/10.3389/fchem.2021.781213/full
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