Results 101 to 110 of about 178,264 (269)

The PI3Kδ inhibitor roginolisib (IOA‐244) preserves T‐cell function and activity

open access: yesMolecular Oncology, EarlyView.
Identification of novel PI3K inhibitors with limited immune‐related adverse effects is highly sought after. We found that roginolisib and idelalisib inhibit chronic lymphocytic leukemia (CLL) cells and Treg suppressive functions to similar extents, but roginolisib affects cytotoxic T‐cell function and promotion of pro‐inflammatory T helper subsets to a
Elise Solli   +7 more
wiley   +1 more source

Basroparib inhibits YAP‐driven cancers by stabilizing angiomotin

open access: yesMolecular Oncology, EarlyView.
Basroparib, a selective tankyrase inhibitor, suppresses Wnt signaling and attenuates YAP‐driven oncogenic programs by stabilizing angiomotin. It promotes AMOT–YAP complex formation, enforces cytoplasmic YAP sequestration, inhibits YAP/TEAD transcription, and sensitizes YAP‐active cancers, including KRAS‐mutant colorectal cancer, to MEK inhibition.
Young‐Ju Kwon   +4 more
wiley   +1 more source

Lactoferrin treatment activates acetylcholinesterase, decreasing acetylcholine levels in non‐small cell lung cancer (NSCLC) cell culture supernatants, inhibiting cell survival

open access: yesFEBS Open Bio, EarlyView.
Representation of the suggested mode of action of lactoferrin (Lf) in nonsmall cell lung cancer (NSCLC) A549 cells. Lf induces activation of caspase‐3 by activating p53 and AChE leading to decreased ACh concentrations. In turn, ACh signaling leads to activation of VEGF and AKT and blocking of caspase‐3.
Stuti Goel   +9 more
wiley   +1 more source

Indoleamine 2,3‐dioxygenase 1 inhibition reverses cancer‐associated fibroblast‐mediated immunosuppression in high‐grade serous ovarian cancer

open access: yesFEBS Open Bio, EarlyView.
CAF‐mediated immunosuppression in ovarian cancer is driven by IDO1, reducing T‐cell function. Inhibiting IDO1 restores T‐cell proliferation and cytotoxicity, increases cancer cell apoptosis, and may help overcome CAF‐induced immune suppression in high‐grade serous ovarian cancer. Targeting IDO1 may improve antitumor immunity.
Hyewon Lee   +3 more
wiley   +1 more source

A general model for analysis of linear and hyperbolic enzyme inhibition mechanisms

open access: yesFEBS Open Bio, EarlyView.
We developed a general enzyme kinetic model that integrates these six basic inhibition mechanism onto a single one. From this model, we deduced a general enzyme kinetic equation that through modulation of simple parameters, γ (the relative inhibitor affinity for two binding sites) and β (the reactivity of the enzyme–substrate–inhibitor complex), is ...
Rafael S. Chagas, Sandro R. Marana
wiley   +1 more source

Homologous expression and purification of human HAX‐1 for structural studies

open access: yesFEBS Open Bio, EarlyView.
This research protocol provides detailed instructions for cloning, expressing, and purifying large quantities of the intrinsically disordered human HAX‐1 protein, N‐terminally fused to a cleavable superfolder GFP, from mammalian cells. HAX‐1 is predicted to undergo posttranslational modifications and to interact with membranes, various cellular ...
Mariana Grieben
wiley   +1 more source

Thrombolytic proteins profiling: High‐throughput activity, selectivity, and resistance assays

open access: yesFEBS Open Bio, EarlyView.
We present optimized biochemical protocols for evaluating thrombolytic proteins, enabling rapid and robust screening of enzymatic activity, inhibition resistance, and fibrin affinity, stimulation, and selectivity. The outcome translates to key clinical indicators such as biological half‐life and bleeding risk. These assays streamline the development of
Martin Toul   +3 more
wiley   +1 more source

Long‐term culture of skin biopsies: maintenance of fibroblast production and competency of reprogramming

open access: yesFEBS Open Bio, EarlyView.
Skin biopsies taken from a patient with an ultra‐rare disorder as well as controls were cultured for up to 473 days. The chunks of skin were serially transferred to a new culture plate when confluent with fibroblasts. Different generations of fibroblasts were analyzed for cell and molecular properties, proliferation, and competence for reprogramming to
Sudiksha Rathan‐Kumar   +3 more
wiley   +1 more source

ATG4B is required for mTORC1‐mediated anabolic activity and is associated with clinical outcomes in non‐small cell lung cancer

open access: yesFEBS Open Bio, EarlyView.
The relationship between anabolic and catabolic processes governing lung cancer cell growth is nuanced. We show that ATG4B, an autophagy regulator, is elevated in lung cancer and that high ATG4B is associated with worse patient outcomes. Targeting ATG4B in cells reduces growth, protein synthesis, and mTORC1 activity, demonstrating a new relationship ...
Patrick J. Ryan   +6 more
wiley   +1 more source

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