The specificities of protein kinase inhibitors: an update.

By J. Bain, H. Mclauchlan, M. Elliott, P. Cohen. Biochemical Journal, 2003

1,434 citations recorded by the source corpus.

Subfields: Molecular Biology, Organic Chemistry, Pharmacology

View Paper: https://www.semanticscholar.org/paper/2284a5ade0905aba071e1d2bbade851754836e4e

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Citations in the corpus

Mitogen-activated protein kinase signaling in the heart: angels versus demons in a heart-breaking tale. (2010, background): “This is not a new concept, since for years the Cohen laboratory has performed detailed studies exposing the nonselectivity of reportedly selective inhibitors (20, 21, 92).”
Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer (2007, background): “…and CI-1040/PD184352) or p38 (SB203580 and SB 202190) (Davies et al., 2000), the preclinical observations made with the SP600125 JNK inhibitor are likely to be less informative regarding the biological roles of JNK, owing to the considerable off-target activity of this compound (Bain et al., 2003).”
Functional redundancy of GSK-3α and GSK-3β in wnt/β-catenin signaling shown by using an allelic series of embryonic stem cell lines (2007, background): “Moreover, GSK-3 inhibitors are prone to non-specific “off-target” effects that become more pronounced as the working concentration of inhibitor increases (Bain et al., 2003).”
Features of selective kinase inhibitors. (2005, background): “Two valuable studies have profiled many of the most commonly used kinase inhibitors against 28 protein kinases in this way [62, 63].”
A small molecule–kinase interaction map for clinical kinase inhibitors (2005, background): “Compounds must be tested experimentally against many kinases to assess molecular specificity and to identify off-target interaction”
LTP inhibits LTD in the hippocampus via regulation of GSK3beta. (2007, neutral): “2G and H), a concentration 40 times the IC 50 for inhibition of CDK2 (Bain et al., 2003).”
Mammalian MAPK signal transduction pathways activated by stress and inflammation: a 10-year update. (2012, background): “Both of these compounds have been used extensively to identify pathways in which the ERKs play a dominant role (8, 9, 54).”
A quantitative analysis of kinase inhibitor selectivity (2008, background): “dtd" [ ]> A first step toward understanding how kinase inhibitor selectivity affects biological activity is to identify and quantify potential off-target kinase interaction”
A rapid, reversible, and tunable method to regulate protein function in living cells using synthetic small molecules. (2006, positive): “However, the question of specificity remains of the utmost importance; in many cases, proteomic analysis reveals that a small-molecule regulator of protein function targets at least one, if not many, off-target proteins (Davies et al., 2000; Bain et al., 2003; Godl et al., 2003).”
A review of connectivity map and computational approaches in pharmacogenomics (2017, background): “A GSK3B/ CDK2 inhibitor has shown a dose-dependent efficacy in inhibiting Ebola infection in vitro without causing cellular toxicity in human cell lines [67].”
GSK-3α regulates production of Alzheimer's disease amyloid-β peptides (2003, methodology): “To test the hypothesis that lithium reduces Aβ production through inhibition of GSK-3, we treated CHO-APP 695 cells with the structurally unrelated GSK-3 inhibitor kenpaullon”
Targeting JNK for therapeutic benefit: from junk to gold? (2003, background): “Recently, SP-600125 was tested under different conditions against a broader range of kinases, in which it inhibited several other kinases with a similar or greater potency than the JNK”
Cell Biology of Tight Junction Barrier Regulation and Mucosal Disease (2018, background): “However, studies of MLCK were hampered by the lack of specific inhibitors, knockdown/knockout cell lines, and knockout mice, which resulted in the necessary reliance on nonspecific agents such as ML-7 (Bain et al. 2003).”