Results 101 to 110 of about 1,524,347 (353)

Measuring ligand efficacy at the mu-opioid receptor using a conformational biosensor. [PDF]

open access: yes, 2018
The intrinsic efficacy of orthosteric ligands acting at G-protein-coupled receptors (GPCRs) reflects their ability to stabilize active receptor states (R*) and is a major determinant of their physiological effects.
Livingston, Kathryn E   +4 more
core  

Thermal proteome profiling and proteome analysis using high‐definition mass spectrometry demonstrate modulation of cholesterol biosynthesis by next‐generation galeterone analog VNPP433‐3β in castration‐resistant prostate cancer

open access: yesMolecular Oncology, EarlyView.
Elevated level of cholesterol is positively correlated to prostate cancer development and disease severity. Cholesterol‐lowering drugs, such as statins, are demonstrated to inhibit prostate cancer. VNPP433‐3β interrupts multiple signaling and metabolic pathways, including cholesterol biosynthesis, AR‐mediated transcription of several oncogenes, mRNA 5′
Retheesh S. Thankan   +10 more
wiley   +1 more source

Exploration of heterogeneity and recurrence signatures in hepatocellular carcinoma

open access: yesMolecular Oncology, EarlyView.
This study leveraged public datasets and integrative bioinformatic analysis to dissect malignant cell heterogeneity between relapsed and primary HCC, focusing on intercellular communication, differentiation status, metabolic activity, and transcriptomic profiles.
Wen‐Jing Wu   +15 more
wiley   +1 more source

Machine Learning Methods as a Cost-Effective Alternative to Physics-Based Binding Free Energy Calculations

open access: yesMolecules
The rank ordering of ligands remains one of the most attractive challenges in drug discovery. While physics-based in silico binding affinity methods dominate the field, they still have problems, which largely revolve around forcefield accuracy and ...
Nupur Bansal, Ye Wang, Simone Sciabola
doaj   +1 more source

Human Cytomegalovirus glycoprotein UL16 causes intracellular sequestration of NKG2D ligands, protecting against NK cell cytotoxicity. [PDF]

open access: yes, 2003
The activating receptor, NKG2D, is expressed on a variety of immune effector cells and recognizes divergent families of major histocompatibility complex (MHC) class I-related ligands, including the MIC and ULBP proteins.
Chalupny, NJ   +6 more
core  

Escape from TGF‐β‐induced senescence promotes aggressive hallmarks in epithelial hepatocellular carcinoma cells

open access: yesMolecular Oncology, EarlyView.
Chronic TGF‐β exposure drives epithelial HCC cells from a senescent state to a TGF‐β resistant mesenchymal phenotype. This transition is characterized by the loss of Smad3‐mediated signaling, escape from senescence, enhanced invasiveness and metastatic potential, and upregulation of key resistance modulators such as MARK1 and GRM8, ultimately promoting
Minenur Kalyoncu   +11 more
wiley   +1 more source

Predicting the biological activity of selected phytochemicals in Alsophila spinulosa leaves against 4-aminobutyrate-aminotransferase: A potential antiepilepsy agents

open access: yesEclética Química
The use of medicinal plants as an alternative mean of treating various diseases has drawn the attention of several researchers. The desire to find lasting solutions to epilepsy among humans increases every day.
Oyebamiji Abel Kolawole   +10 more
doaj   +1 more source

ShcD adaptor protein drives invasion of triple negative breast cancer cells by aberrant activation of EGFR signaling

open access: yesMolecular Oncology, EarlyView.
We identified adaptor protein ShcD as upregulated in triple‐negative breast cancer and found its expression to be correlated with reduced patient survival and increased invasion in cell models. Using a proteomic screen, we identified novel ShcD binding partners involved in EGFR signaling pathways.
Hayley R. Lau   +11 more
wiley   +1 more source

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