Results 71 to 80 of about 216,066 (333)

Development and Structural Characterization of UTE‐156, a Covalent Inhibitor of the VCP/p97 AAA+ ATPase

open access: yesAdvanced Science, EarlyView.
The AAA+ ATPase Valosin‐containing protein (VCP/p97) regulates protein homeostasis by unfolding ubiquitinated substrates. Here, we describe UTE‐156, a novel irreversible covalent inhibitor that modifies Cys522 in the D2 ATPase motor domain. Although its pharmacochemical limitations preclude immediate therapeutic use, UTE‐156 serves as a valuable ...
Daniela Tamayo‐Jaramillo   +8 more
wiley   +1 more source

The cAMP-signaling cancers: Clinically-divergent disorders with a common central pathway

open access: yesFrontiers in Endocrinology, 2022
The cAMP-signaling cancers, which are defined by functionally-significant somatic mutations in one or more elements of the cAMP signaling pathway, have an unexpectedly wide range of cell origins, clinical manifestations, and potential therapeutic options.
Graeme B. Bolger
doaj   +1 more source

Cyclic AMP signalling in pancreatic islets [PDF]

open access: yes, 2010
Cyclic 3'5'AMP (cAMP) is an important physiological amplifier of glucose-induced insulin secretion by the pancreatic islet β-cell, where it is formed by the activity of adenylyl cyclases, which are stimulated by glucose, through elevation in ...
Furman, Brian   +2 more
core   +1 more source

Mammalian Glycerophosphodiester Phosphodiesterases [PDF]

open access: yesBioscience, Biotechnology, and Biochemistry, 2007
Bacterial glycerophosphodiester phosphodiesterases (GP-PDEs), GlpQ and UgpQ, are well-characterized periplasmic and cytosolic proteins that play critical roles in the hydrolysis of deacylated glycerophospholipids to glycerol phosphate and alcohol, which are utilized as major sources of carbon and phosphate.
openaire   +2 more sources

An Implantable Scaffold Sequentially Releasing STING Agonist and B7‐H3 Antibody for Bone Metastasis Immunotherapy

open access: yesAdvanced Science, EarlyView.
We developed an implantable dual‐drug depot using GelMA for bone metastasis treatment, co‐delivering MSA‐2 and αB7‐H3‐loaded CaCO3 microparticles. Sustained release from GelMA scaffold enables MSA‐2 to activate STING signaling and enhance T‐cell infiltration and activation, while sequentially released αB7‐H3 blocks MSA‐2‐induced B7‐H3 upregulation ...
Qijun Lin   +10 more
wiley   +1 more source

TDP1 deficiency sensitizes human cells to base damage via distinct topoisomerase I and PARP mechanisms with potential applications for cancer therapy [PDF]

open access: yes, 2013
Base damage and topoisomerase I (Top1)-linked DNA breaks are abundant forms of endogenous DNA breakage, contributing to hereditary ataxia and underlying the cytotoxicity of a wide range of anti-cancer agents.
Alagoz   +50 more
core   +1 more source

Phosphodiesterases and preeclampsia

open access: yesMedical Hypotheses, 2017
Antagonizing vasodilation has been considered one of the potential mechanisms underlying the pathophysiology of preeclampsia. Phosphodiesterases hydrolyze cGMP, interfering with the action of nitric oxide on vascular smooth muscle, thus causing vasoconstriction.
Anne Brandolt, Larré   +7 more
openaire   +2 more sources

Selective Phosphodiesterase 4B Inhibitors: A Review

open access: yesScientia Pharmaceutica, 2014
Phosphodiesterase 4B (PDE4B) is a member of the phosphodiesterase family of proteins that plays a critical role in regulating intracellular levels of cyclic adenosine monophosphate (cAMP) by controlling its rate of degradation.
M. Azam, N. S. Tripuraneni
semanticscholar   +1 more source

Endogenous Ceramide 24:1 Constrains Th17‐Driven Neutrophilic Inflammation by Antagonizing EP2 Signaling

open access: yesAdvanced Science, EarlyView.
Cer24:1 levels are reduced in neutrophilic asthma and inversely correlate with disease severity and airway neutrophilia. Restoring Cer24:1 suppresses pathogenic Th17 differentiation by engaging EP2 on CD4+ T cells, thereby dampening the JAK2–STAT3–RORγt axis and reducing IL‐17 production.
Huan Liu   +11 more
wiley   +1 more source

Ribonuclease L mediates the cell-lethal phenotype of double-stranded RNA editing enzyme ADAR1 deficiency in a human cell line

open access: yeseLife, 2017
ADAR1 isoforms are adenosine deaminases that edit and destabilize double-stranded RNA reducing its immunostimulatory activities. Mutation of ADAR1 leads to a severe neurodevelopmental and inflammatory disease of children, Aicardi-Goutiéres syndrome.
Yize Li   +9 more
doaj   +1 more source

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