Extracellular-signal regulated kinase: A central molecule driving epithelial–mesenchymal transition in cancer
M Olea-Flores, MD Zuñiga-Eulogio… - International journal of …, 2019 - mdpi.com
Epithelial–mesenchymal transition (EMT) is a reversible cellular process, characterized by
changes in gene expression and activation of proteins, favoring the trans-differentiation of …
changes in gene expression and activation of proteins, favoring the trans-differentiation of …
ERK1/2 inhibitors: New weapons to inhibit the RAS-regulated RAF-MEK1/2-ERK1/2 pathway
Abstract The RAS-regulated RAF-MEK1/2-ERK1/2 signalling pathway is de-regulated in a
variety of cancers due to mutations in receptor tyrosine kinases (RTKs), negative regulators …
variety of cancers due to mutations in receptor tyrosine kinases (RTKs), negative regulators …
Protein degradation by in-cell self-assembly of proteolysis targeting chimeras
H Lebraud, DJ Wright, CN Johnson… - ACS central …, 2016 - ACS Publications
Selective degradation of proteins by proteolysis targeting chimeras (PROTACs) offers a
promising potential alternative to protein inhibition for therapeutic intervention. Current …
promising potential alternative to protein inhibition for therapeutic intervention. Current …
Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an …
JF Blake, M Burkard, J Chan, H Chen, KJ Chou, D Diaz… - 2016 - ACS Publications
The extracellular signal-regulated kinases ERK1/2 represent an essential node within the
RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations …
RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations …
Discovery of a bromodomain and extraterminal inhibitor with a low predicted human dose through synergistic use of encoded library technology and fragment …
CR Wellaway, D Amans, P Bamborough… - Journal of Medicinal …, 2020 - ACS Publications
The bromodomain and extraterminal (BET) family of bromodomain-containing proteins are
important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) …
important regulators of the epigenome through their ability to recognize N-acetyl lysine (KAc) …
Research progress of MEK1/2 inhibitors and degraders in the treatment of cancer
C Wang, H Wang, C Zheng, Z Liu, X Gao, F Xu… - European journal of …, 2021 - Elsevier
Mitogen-activated protein kinase kinases 1 and 2 (MEK1/2) are the crucial part of the RAS-
RAF-MEK-ERK pathway (or ERK pathway), which is involved in the regulation of various …
RAF-MEK-ERK pathway (or ERK pathway), which is involved in the regulation of various …
[HTML][HTML] Development of small molecule extracellular signal-regulated kinases (ERKs) inhibitors for cancer therapy
X Pan, J Pei, A Wang, W Shuai, L Feng, F Bu… - … Pharmaceutica Sinica B, 2022 - Elsevier
The mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase 1/2
(ERK1/2) signaling pathway is widely activated by a variety of extracellular stimuli, and its …
(ERK1/2) signaling pathway is widely activated by a variety of extracellular stimuli, and its …
Integration of Hydrogen–Deuterium Exchange Mass Spectrometry with Molecular Dynamics Simulations and Ensemble Reweighting Enables High Resolution Protein …
Hydrogen–Deuterium exchange mass spectrometry's (HDX-MS) utility in identifying and
characterizing protein–small molecule interaction sites has been established. The regions …
characterizing protein–small molecule interaction sites has been established. The regions …
Convenient Synthesis of N-Heterocycle-Fused Tetrahydro-1,4-diazepinones
K Dzedulionytė, M Veikšaitė, V Morávek… - Molecules, 2022 - mdpi.com
A general approach towards the synthesis of tetrahydro-4 H-pyrazolo [1, 5-a][1, 4] diazepin-4-
one, tetrahydro [1, 4] diazepino [1, 2-a] indol-1-one and tetrahydro-1 H-benzo [4, 5] imidazo …
one, tetrahydro [1, 4] diazepino [1, 2-a] indol-1-one and tetrahydro-1 H-benzo [4, 5] imidazo …
Fragment-based discovery of a potent, orally bioavailable inhibitor that modulates the phosphorylation and catalytic activity of ERK1/2
TD Heightman, V Berdini, H Braithwaite… - Journal of medicinal …, 2018 - ACS Publications
Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers.
Inhibitors of BRAF and MEK kinases are approved for the treatment of BRAF mutant …
Inhibitors of BRAF and MEK kinases are approved for the treatment of BRAF mutant …