BET bromodomain inhibitors
MP Schwalm, S Knapp - Current opinion in chemical biology, 2022 - Elsevier
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain
proteins that have emerged as principal regulators of linage specific gene transcription. The …
proteins that have emerged as principal regulators of linage specific gene transcription. The …
Impact of ERK5 on the Hallmarks of Cancer
Extracellular signal-regulated kinase 5 (ERK5) belongs to the mitogen-activated protein
kinase (MAPK) family that consists of highly conserved enzymes expressed in all eukaryotic …
kinase (MAPK) family that consists of highly conserved enzymes expressed in all eukaryotic …
Discovery of a selective inhibitor of doublecortin like kinase 1
Abstract Doublecortin like kinase 1 (DCLK1) is an understudied kinase that is upregulated in
a wide range of cancers, including pancreatic ductal adenocarcinoma (PDAC). However …
a wide range of cancers, including pancreatic ductal adenocarcinoma (PDAC). However …
Drug and disease signature integration identifies synergistic combinations in glioblastoma
V Stathias, AM Jermakowicz, ME Maloof… - Nature …, 2018 - nature.com
Glioblastoma (GBM) is the most common primary adult brain tumor. Despite extensive
efforts, the median survival for GBM patients is approximately 14 months. GBM therapy could …
efforts, the median survival for GBM patients is approximately 14 months. GBM therapy could …
Dual‐target inhibitors of bromodomain and extra‐terminal proteins in cancer: A review from medicinal chemistry perspectives
L Feng, G Wang, Y Chen, G He, B Liu… - Medicinal research …, 2022 - Wiley Online Library
Abstract Bromodomain‐containing protein 4 (BRD4), as the most studied member of the
bromodomain and extra‐terminal (BET) family, is a chromatin reader protein interpreting …
bromodomain and extra‐terminal (BET) family, is a chromatin reader protein interpreting …
[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 …
Two-hit wonders: The expanding universe of multitargeting epigenetic agents
AR De Lera, A Ganesan - Current Opinion in Chemical Biology, 2020 - Elsevier
Multitargeting involves the application of molecules that are deliberately intended to bind to
two or more unrelated cellular targets with high affinity. In epigenetic chemical biology and …
two or more unrelated cellular targets with high affinity. In epigenetic chemical biology and …
Clinical, genetic and pharmacological data support targeting the MEK5/ERK5 module in lung cancer
A Sánchez-Fdez, MF Re-Louhau… - NPJ Precision …, 2021 - nature.com
Despite advances in its treatment, lung cancer still represents the most common and lethal
tumor. Because of that, efforts to decipher the pathophysiological actors that may promote …
tumor. Because of that, efforts to decipher the pathophysiological actors that may promote …
Inhibition of ERK5 elicits cellular senescence in melanoma via the cyclin-dependent kinase inhibitor p21
A Tubita, Z Lombardi, I Tusa, A Lazzeretti, G Sgrignani… - Cancer research, 2022 - AACR
Melanoma is the deadliest skin cancer with a very poor prognosis in advanced stages.
Although targeted and immune therapies have improved survival, not all patients benefit …
Although targeted and immune therapies have improved survival, not all patients benefit …
The ERK5/NF-κB signaling pathway targets endometrial cancer proliferation and survival
N Diéguez-Martínez, S Espinosa-Gil, G Yoldi… - Cellular and Molecular …, 2022 - Springer
Endometrial cancer (EC) is the most common type of gynecologic cancer in women of
developed countries. Despite surgery combined with chemo-/radiotherapy regimens, overall …
developed countries. Despite surgery combined with chemo-/radiotherapy regimens, overall …