Results 131 to 140 of about 6,763,423 (338)

Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance

open access: yesCommunications Biology, 2018
The androgen receptor is a major driver of prostate cancer and inhibition of its transcriptional activity using competitive antagonists, such as enzalutamide remains a frontline therapy for prostate cancer management.
J. Salami   +10 more
semanticscholar   +1 more source

Tonic signaling of the B‐cell antigen‐specific receptor is a common functional hallmark in chronic lymphocytic leukemia cell phosphoproteomes at early disease stages

open access: yesMolecular Oncology, EarlyView.
B‐cell chronic lymphocytic leukemia (B‐CLL) and monoclonal B‐cell lymphocytosis (MBL) show altered proteomes and phosphoproteomes, analyzed using mass spectrometry, protein microarrays, and western blotting. Identifying 2970 proteins and 316 phosphoproteins, including 55 novel phosphopeptides, we reveal BCR and NF‐kβ/STAT3 signaling in disease ...
Paula Díez   +17 more
wiley   +1 more source

The Hippocampus Is the Place to Be: Opioid Receptors and LTP

open access: yesCell Reports, 2019
Nam et al. (2019) genetically modulate the expression of astrocytic μ-opioid receptors to reveal they are necessary for drug-induced conditioned place preference.
Thomas M. Sanderson   +3 more
doaj  

Rational Drug Design and Synthesis of Molecules Targeting the Angiotensin II Type 1 and Type 2 Receptors

open access: yesMolecules, 2015
The angiotensin II (Ang II) type 1 and type 2 receptors (AT1R and AT2R) orchestrate an array of biological processes that regulate human health. Aberrant function of these receptors triggers pathophysiological responses that can ultimately lead to death.
Tahsin F. Kellici   +2 more
doaj   +1 more source

Targeted protein degradation in oncology: novel therapeutic opportunity for solid tumours?

open access: yesMolecular Oncology, EarlyView.
Current anticancer therapies are limited by the occurrence of resistance and undruggability of most proteins. Targeted protein degraders are novel, promising agents that trigger the selective degradation of previously undruggable proteins through the recruitment of the ubiquitin–proteasome machinery. Their mechanism of action raises exciting challenges,
Noé Herbel, Sophie Postel‐Vinay
wiley   +1 more source

Molecular docking: a powerful approach for structure-based drug discovery.

open access: yesCurrent Computer - Aided Drug Design, 2011
Molecular docking has become an increasingly important tool for drug discovery. In this review, we present a brief introduction of the available molecular docking methods, and their development and applications in drug discovery.
Xuanyu Meng   +3 more
semanticscholar   +1 more source

Determination of ADP/ATP translocase isoform ratios in malignancy and cellular senescence

open access: yesMolecular Oncology, EarlyView.
The individual functions of three isoforms exchanging ADP and ATP (ADP/ATP translocases; ANTs) on the mitochondrial membrane remain unclear. We developed a method for quantitatively differentiating highly similar human ANT1, ANT2, and ANT3 using parallel reaction monitoring. This method allowed us to assess changes in translocase levels during cellular
Zuzana Liblova   +18 more
wiley   +1 more source

Solubilization and Display of G Protein-Coupled Receptors on Beads for Real-Time Fluorescence and Flow Cytometric Analysis

open access: yesBioTechniques, 2000
G protein-coupled receptors (GPCR) and cellular signaling elements are prime targets for drug discovery. Sensitive realtime methods that expand the analytical capabilities for these elements can play significant roles in basic research and drug discovery.
L.A. Sklar   +5 more
doaj   +1 more source

Early metastasis is characterized by Gr1+ cell dysregulation and is inhibited by immunomodulatory nanoparticles

open access: yesMolecular Oncology, EarlyView.
Breast cancer metastasis is associated with myeloid cell dysregulation and the lung‐specific accumulation of tumor‐supportive Gr1+ cells. Gr1+ cells support metastasis, in part, through a CHI3L1‐mediated mechanism, which can be targeted and inhibited with cargo‐free, polymeric nanoparticles.
Jeffrey A. Ma   +9 more
wiley   +1 more source

Biased Receptor Signaling in Drug Discovery

open access: yesPharmacological Reviews, 2019
A great deal of experimental evidence suggests that ligands can stabilize different receptor active states that go on to interact with cellular signaling proteins to form a range of different complexes in varying quantities.
T. Kenakin
semanticscholar   +1 more source

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