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MetabolomicsFirst-in-class MKK4 inhibitors enhance liver regeneration and prevent liver failure

Diminished hepatocyte regeneration is a key feature of acute and chronic liver diseases and after extended liver resections, resulting in the inability to maintain or restore a sufficient functional liver mass. Therapies to restore hepatocyte regeneration are lacking, making liver transplantation...

2024-09-23 | MTBLS9434 | MetaboLights
MetabolomicsHypoxia Dependent Inhibition of Glioblastoma Cell Proliferation, Invasion, and Metabolism by the Choline-Kinase Inhibitor JAS239
Background: Elevated choline kinase alpha (ChoK) levels are observed in most solid tumors, including glioblastomas (GBM), and ChoK inhibitors have demonstrated limited efficacy in GBM models. Given that hypoxia is associated with resistance to GBM therapy, we hypothesized that tumor hypoxia c...
2024-06-18 | MTBLS6212 | MetaboLights
TranscriptomicsBlockade of oncogenic IkappaB kinase activity in ABC DLBCL by small molecule BET protein inhibitors
In the activated B cell-like (ABC) subtype of diffuse large B cell lymphoma (DLBCL), NF-kappaB activity is essential for viability of the malignant cells and is sustained by constitutive activity of IkappaB kinase (IKK) in the cytoplasm. Here, we report an unexpected role for the bromodomain and ext...
ORGANISM(S): Homo sapiens 
2014-08-01 | E-GEOD-58791 | biostudies-arrayexpress
GenomicsSmall molecule inhibitors in melanoma Kenski Kong WES
Small-molecule inhibitors targeting the most commonly activated pathway in melanoma, MAPK pathway (either alone or in combination) are already given to melanoma patients for few years, and initially reduce tumour burden dramatically, eventually melanomas become resistant and tumours progress while o...
EGAS00001002863 | EGA
TranscriptomicsTumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase
Deregulated expression of MYC is a driver of colorectal carcinogenesis, necessitating novel strategies to inhibit MYC function. The ubiquitin ligase HUWE1 (HECTH9, ARFBP1, MULE) associates with both MYC and the MYC-associated protein MIZ1. We show here that HUWE1 is required for growth of colorecta...
ORGANISM(S): Homo sapiens 
2014-10-21 | E-GEOD-59223 | biostudies-arrayexpress
TranscriptomicsSynthetic lethal screening with small molecule inhibitors provides a pathway to rational combination therapies for melanoma
Recent data demonstrate that extracellular signals are transmitted through a network of proteins rather than hierarchical signaling pathways. This network model suggests why inhibition of a single component of a canonical pathway, even when targeting a mutationally activated driver of cancer, has in...
ORGANISM(S): Homo sapiens 
2012-12-06 | E-GEOD-39192 | biostudies-arrayexpress
ProteomicsChemical and phosphoproteomics illuminate the cellular mode of action of AKT inhibitors
Due to its key role in dysregulated cellular signaling in cancer, AKT has been subject to intense drug discovery efforts leading to small molecule inhibitors investigated in clinical trials, notably breast cancer. To shed more light on how these drugs exert their therapeutic effects, we integrated c...
ORGANISM(S): Homo Sapiens 
2022-01-21 | PXD015188 | panorama
TranscriptomicsTranscriptional response of Escherichia coli O157 TUV93-0 to small molecule inhibitors of TTS
The transcriptional profile of Escherichia coli O157 treated with small molecule inhibitors of type III secretion was determined. Four variations of the small molecule inhibitor were assessed for global changes in transcription by treating cells with 20uM of inhibitor or an equivalent volume of DMSO...
ORGANISM(S): Escherichia coli 
2009-08-10 | E-GEOD-10319 | biostudies-arrayexpress
ProteomicsChemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors
Protein kinases are key components in signal transduction pathways and are established drug targets in oncology. Consequently, small molecule kinase inhibitors are on the rise but often show a rather broad target spectrum, potentially leading to toxic side effects. As a result, a broad assessment of...
ORGANISM(S): Homo sapiens (Human) 
2017-03-22 | PXD003373 | Pride
Kinase inhibitor Fech Photosensitivity Chemical proteomics Ferrochelatase Vemurafenib Kinobeads 
UnknownTargeting cancer with small molecule kinase inhibitors.
Not available
S-EPMC12406740 | biostudies-literature
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