An overview of kinase downregulators and recent advances in discovery approaches

B Wang, H Wu, C Hu, H Wang, J Liu… - Signal Transduction and …, 2021 - nature.com
Since the clinical approval of imatinib, the discovery of protein kinase downregulators
entered a prosperous age. However, challenges still exist in the discovery of kinase …

The molecular events behind ferulic acid mediated modulation of IL-6 expression in LPS-activated Raw 264.7 cells

N Lampiasi, G Montana - Immunobiology, 2016 - Elsevier
Identification of new antioxidant and anti-inflammatory bioactive molecules is an important
tool for selecting effective formulations for the treatment of inflammation. The mouse …

Phytochemicals as potential IKK-β inhibitor for the treatment of cardiovascular diseases in plant preservation: terpenoids, alkaloids, and quinones

F Hua, L Shi, P Zhou - Inflammopharmacology, 2020 - Springer
Modulation of inhibitor kappa B kinase-beta (IKK-β) kinase activity could be useful for
preventing inflammation that serves an efficient role in protection against cardiovascular …

Homology modelling, vHTS, pharmacophore, molecular docking and molecular dynamics studies for the identification of natural compound-derived inhibitor of MRP3 …

F Olawale, O Iwaloye, K Olofinsan, OM Ogunyemi… - Chemical Papers, 2022 - Springer
The pivotal role of MRP3 protein in acute leukaemia and the efficacy of natural compounds
in cancer treatment have necessitated the current study to identify novel MRP3 inhibitors …

In silico drug discovery of IKK-β inhibitors from 2-amino-3-cyano-4-alkyl-6-(2-hydroxyphenyl) pyridine derivatives based on QSAR, docking, molecular dynamics and …

NEH Hammoudi, Y Benguerba, A Attoui… - Journal of …, 2022 - Taylor & Francis
The Inhibitor of IKK-β (nuclear factor kappa B kinase subunit beta), a specific modulator of
NF-κB (nuclear factor-κB), is considered a valid target to discover new active compounds for …

Rescuing the CFTR protein function: Introducing 1, 3, 4-oxadiazoles as translational readthrough inducing drugs

I Pibiri, L Lentini, R Melfi, M Tutone… - European journal of …, 2018 - Elsevier
Nonsense mutations in the CFTR gene prematurely terminate translation of the CFTR mRNA
leading to the production of a truncated protein that lacks normal function causing a more …

In silico drug design of inhibitor of nuclear factor kappa B kinase subunit beta inhibitors from 2-acylamino-3-aminothienopyridines based on quantitative structure …

JL Wang, L Li, MB Hu, B Wu, WX Fan, W Peng… - … biology and chemistry, 2019 - Elsevier
Inhibitor of nuclear factor kappa B kinase subunit beta (IKK-β), a specific regulator of nuclear
factor-κB (NF-κB), is considered a valid target to design novel candidate drugs to treat …

Exploring the readthrough of nonsense mutations by non-acidic Ataluren analogues selected by ligand-based virtual screening

I Pibiri, L Lentini, M Tutone, R Melfi, A Pace… - European Journal of …, 2016 - Elsevier
Ataluren, also known as PTC124, is a 5-(fluorophenyl)-1, 2, 4-oxadiazolyl-benzoic acid
suggested to suppress nonsense mutations by readthrough of premature stop codons in the …

[HTML][HTML] Discovery of a novel IKK-β inhibitor by ligand-based virtual screening techniques

SM Noha, AG Atanasov, D Schuster, P Markt… - Bioorganic & medicinal …, 2011 - Elsevier
Various inflammatory stimuli that activate the nuclear factor kappa B (NF-κB) signaling
pathway converge on a serine/threonine kinase that displays a key role in the activation of …

Targeting nonsense: optimization of 1, 2, 4-oxadiazole trids to rescue cftr expression and functionality in cystic fibrosis cell model systems

I Pibiri, R Melfi, M Tutone, A Di Leonardo… - International journal of …, 2020 - mdpi.com
Cystic fibrosis (CF) patients develop a severe form of the disease when the cystic fibrosis
transmembrane conductance regulator (CFTR) gene is affected by nonsense mutations …