New promise and opportunities for allosteric kinase inhibitors

X Lu, JB Smaill, K Ding - Angewandte Chemie International …, 2020 - Wiley Online Library
Drugs that function through allosteric inhibition of kinase signaling represent a promising
approach for the targeted discovery of therapeutics. The majority of developed allosteric …

The evolution of regulators of G protein signalling proteins as drug targets–20 years in the making: IUPHAR Review 21

B Sjögren - British journal of pharmacology, 2017 - Wiley Online Library
Regulators of G protein signalling (RGS) proteins are celebrating the 20th anniversary of
their discovery. The unveiling of this new family of negative regulators of G protein signalling …

Design, synthesis, and biological evaluation of MEK PROTACs

S Vollmer, D Cunoosamy, H Lv, H Feng… - Journal of Medicinal …, 2019 - ACS Publications
PROteolysis TArgeting Chimeras (PROTACs) targeting the degradation of MEK have been
designed based on allosteric MEK inhibitors. Inhibition of the phosphorylation of ERK1/2 …

Targeting compensatory MEK/ERK activation increases JAK inhibitor efficacy in myeloproliferative neoplasms

S Stivala, T Codilupi, S Brkic… - The Journal of …, 2019 - Am Soc Clin Investig
Constitutive JAK2 signaling is central to myeloproliferative neoplasm (MPN) pathogenesis
and results in activation of STAT, PI3K/AKT, and MEK/ERK signaling. However, the …

Oleanolic Acid Complexation with Cyclodextrins Improves Its Cell Bio-Availability and Biological Activities for Cell Migration

J Stelling-Férez, S López-Miranda… - International Journal of …, 2023 - mdpi.com
Wound healing is a complex process to restore skin. Plant-derived bioactive compounds
might be a source of substances for the treatment of wounds stalled in a non-resolving stage …

Oleanolic acid stimulation of cell migration involves a biphasic signaling mechanism

J Stelling-Férez, JA Gabaldón, FJ Nicolás - Scientific Reports, 2022 - nature.com
Cell migration is a critical process for wound healing, a physiological phenomenon needed
for proper skin restoration after injury. Wound healing can be compromised under …

Exploring the natural compounds in flavonoids for their potential inhibition of cancer therapeutic target MEK1 using computational methods

WM AlZahrani, SA AlGhamdi, TA Zughaibi, M Rehan - Pharmaceuticals, 2022 - mdpi.com
The Mitogen-Activated Protein Kinase (MAPK) signaling pathway plays an important role in
cancer cell proliferation and survival. MAPKs' protein kinases MEK1/2 serve as important …

The protein kinase CK1: Inhibition, activation, and possible allosteric modulation

YK Sunkari, L Meijer, M Flajolet - Frontiers in Molecular Biosciences, 2022 - frontiersin.org
Protein kinases play a vital role in biology and deregulation of kinases is implicated in
numerous diseases ranging from cancer to neurodegenerative diseases, making them a …

LY6K promotes glioblastoma tumorigenicity via CAV-1–mediated ERK1/2 signaling enhancement

NG Sastry, X Wan, T Huang, AA Alvarez… - Neuro …, 2020 - academic.oup.com
Background Lymphocyte antigen 6 complex, locus K (LY6K) is a putative oncogene in
various cancers. Elevated expression of LY6K is correlated with poor patient prognosis in …

Cytotoxic Effect of Vanicosides A and B from Reynoutria sachalinensis against Melanotic and Amelanotic Melanoma Cell Lines and in silico Evaluation for Inhibition …

I Nawrot-Hadzik, A Choromańska, R Abel… - International Journal of …, 2020 - mdpi.com
Vanicosides A and B are the esters of hydroxycinnamic acids with sucrose, occurring in a
few plant species from the Polygonaceae family. So far, vanicosides A and B have not been …