Results 161 to 170 of about 358,313 (362)

Identification and Biological Evaluation of a Novel CLK4 Inhibitor Targeting Alternative Splicing in Pancreatic Cancer Using Structure‐Based Virtual Screening

open access: yesAdvanced Science, EarlyView.
Pancreatic cancer is a highly aggressive malignancy with limited treatment options. CLK4 regulates alternative splicing, contributing to cancer progression. This study establishes a computational model to identify CLK4 inhibitors, leading to compound 150441 (IC50: 21.4 nm).
Chun‐Lin Yang   +13 more
wiley   +1 more source

Structures of human plasma β–factor XIIa cocrystallized with potent inhibitors

open access: yesBlood Advances, 2018
: Activated factor XIIa (FXIIa) is a serine protease that has received a great deal of interest in recent years as a potential target for the development of new antithrombotics.
Alexey Dementiev   +6 more
doaj  

Nuclear‐Localized BCKDK Facilitates Homologous Recombination Repair to Support Breast Cancer Progression and Therapy Resistance

open access: yesAdvanced Science, EarlyView.
Under DNA damage, tumor cells rely on efficient DNA repair for survival and therapy resistance. This study has demonstrated that BCKDK localizes to breast cancer cell nuclei, where it binds to and phosphorylates RNF8, thereby blocking ubiquitin‐mediated degradation of RAD51 and enhancing HRR. A selective BCKDK inhibitor synergizes with clinical agents,
Haiying Liu   +12 more
wiley   +1 more source

Reversible High‐Affinity Binding of Coagulation Factor Xa to Zeolites Induces Accelerated Blood Coagulation

open access: yesAdvanced Science, EarlyView.
A calcium‐dependent, specific biorecognition between coagulation factor Xa (FXa) and zeolite is discovered. It alters the prothrombin activation pathway to a more efficient mechanism by mimicking the FXa/factor Va (FXa/FVa) interaction formed during the natural coagulation cascade.
Chaojie Shi   +9 more
wiley   +1 more source

A Phase‐Separated SR Protein Reprograms Host Pre‐mRNA Splicing to Enhance Disease Susceptibility

open access: yesAdvanced Science, EarlyView.
This study identifies SR30, a splicing factor, as a negative regulator of tomato immunity. During Phytophthora infestans infection, the elevated SR30 forms nuclear condensates to suppress the alternative splicing (AS) of defense‐related genes in a phase separation manner.
Dong Yan   +11 more
wiley   +1 more source

Epipolythiodioxopiperazine‐Based Natural Products: Building Blocks, Biosynthesis and Biological Activities

open access: yesChemBioChem, Volume 23, Issue 23, December 5, 2022., 2022
Housing sulfur: Certain fungi produce diketopiperazine compounds with a transannular sulfur bridge. These so‐called epipolythiodioxopiperzines are toxic by non‐specifically interacting with intracellular proteins and contribute to fungal pathogenicity. Producer strains serve as bio‐pesticides but also question safety of food fermentation.
Eva M. Huber
wiley   +1 more source

Dual Role of CRABP2 in Colorectal Cancer: Oncogenesis via Nuclear RB1 and Cytoplasmic AFG3L2/SLC25A39 Axis, While Limiting Liver Metastasis through Cytoplasmic AFG3L2/PINK1/Parkin‐Mediated Mitophagy

open access: yesAdvanced Science, EarlyView.
CRABP2 plays a dual role in colorectal cancer: it promotes proliferation and suppresses apoptosis through the nuclear CRABP2/RB1 axis and the cytoplasmic AFG3L2/SLC25A39 axis. Meanwhile, it inhibits colorectal liver metastasis via AFG3L2/PINK1/Parkin‐mediated mitophagy.
Chuanxin Tian   +14 more
wiley   +1 more source

Autocrine GDF10 Inhibits Hepatic Stellate Cell Activation via BMPR2/ALK3 Receptor to Prevent Liver Fibrosis

open access: yesAdvanced Science, EarlyView.
Liver fibrosis is a growing global health burden with no specific treatment. HSC activation is the predominant driver of liver fibrogenesis and the current focus in antifibrotic drug discovery. This study identifies autocrine GDF10 activates BMPR2/ALK3‐SMAD1/5/8‐SMAD7 pathway to counteract the TGF‐β‐SMAD2/3 pathway in HSCs, thereby inhibiting HSC ...
Yinliang Zhang   +16 more
wiley   +1 more source

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